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Pharmaceuticals Pipeline

Last update: Apr. 11, 2013

Therapeutic Area
Partner
Managed By
Compound/
Generic name
Trade name

Indication
Phase
123f
Expected Filing

1. Oncology

1. Oncology
CHU
solid tumors
4. Phase 1

Description/Summary:

A novel small molecule inhibitor to phosphatidylinositol 3-kinase (PI3K) class I.

Managed by:
4. Chugai
Partner:
Roche participation
1. Oncology
CHU
oncology
4. Phase 1

Description/Summary:

The Wilms' tumor gene WT1 is overexpressed in leukemias and various types of solid tumors, and therefore the WT1 protein may serve as target antigen for immunotherapy (WT1 vaccine) against these malignancies. Tumor immunotherapy, is the use of the immune system to reject cancer.

Managed by:
4. Chugai
Partner:
Roche participation
1. Oncology
RG7112
solid and hematological tumors
4. Phase 1

Description/Summary:

RG7112 is an oral, selective, small molecule MDM2 antagonist that inhibits binding of MDM2 to p53. MDM2 plays an important role in regulating the degradation of p53. Blocking the MDM2-p53 interaction stabilizes p53 and activates p53-mediated cell death and inhibition of cell growth.

Managed by:
2. Pharma Research and Early Development
Roche Only
1. Oncology
RG7116
solid tumors
4. Phase 1

Description/Summary:

RG7116 is a glyco-engineered humanised monoclonal antibody that is designed to inhibit the activation and signalling of HER3, a member of the Human Epidermal Growth Factor Receptor (HER) family which amplifies cell survival and proliferation signals when associated with HER2 or HER1. Through glyco-engineering HER3 MAb is designed to engage the immune system when bound to tumor cells and elicit enhanced antibody-dependent cellular cytotoxicity (ADCC).

Managed by:
2. Pharma Research and Early Development
Roche Only
1. Oncology
RG7155
solid tumors
4. Phase 1

Description/Summary:

RG7155 is a humanized monoclonal antibody targeting colony stimulating factor-1 receptor (CSF-1R) designed to inhibit the CSF-1 mediated survival of tumor-promoting ‘M2’ macrophages without affecting tumor-killing ‘M1’ macrophages.

Managed by:
2. Pharma Research and Early Development
Roche Only
1. Oncology
RG7167
solid tumors
4. Phase 1

Description/Summary:

RG7167 is a selective inhibitor of MEK, also known as mitogen activated protein kinase kinase (MAPKK). MEK is a key component of the RAS/RAF/MEK/ERK pathway, which is frequently activated in human tumors. Inappropriate activation of the MEK/ERK pathway promotes cell growth in the absence of exogenous growth factors.

Managed by:
2. Pharma Research and Early Development
Partner:
Chugai
1. Oncology
RG7204 vemurafenib
Zelboraf
metastatic melanoma, BRAF mutation positive
4. Phase 1

Description/Summary:

A phase Ib trial studying Zelboraf in combination with ipilimumab in BRAF-mutation positive metastatic melanoma is ongoing. Zelboraf is an oral, small molecule, BRAF kinase inhibitor. The BRAF protein is a key component of the RAS-RAF pathway involved in normal cell growth and survival. Mutations that keep the BRAF protein in an active state may cause excessive pathway signalling, leading to uncontrolled cell growth and survival.

Managed by:
1. Roche Group
Partner:
BMS, Plexxikon Inc., member of Daiichi Sankyo Group
1. Oncology
RG7212
solid tumors
4. Phase 1

Description/Summary:

RG7212 is a fully humanized monoclonal antibody that is designed to block TWEAK:Fn14 signaling, a pathway involved in tumorigenesis that regulates cell proliferation, survival, and migration.

Managed by:
2. Pharma Research and Early Development
Roche Only
1. Oncology
RG7221
oncology
4. Phase 1

Description/Summary:

RG7221 is a bi-specific monoclonal antibody comprised of two different heavy chains and two different light chains. One arm of the antibody binds Angiopoietin-2 (Ang2) and the other is based on bevacizumab (Avastin), binding Vascular Endothelial Growth Factor A (VEGF-A). The antibody is designed to inhibit both VEGF-A and Ang2 simultaneously to offer superior clinical benefit compared to VEGF-A inhibition alone.

Managed by:
2. Pharma Research and Early Development
Roche Only
1. Oncology
RG7304
solid tumors
4. Phase 1

Description/Summary:

RG7304 is a small molecule MEK inhibitor with a novel structure based on a coumarin skeleton. It selectively inhibited Raf1 (C-Raf), B-Raf, mutant B-Raf (V600E), and MEK1 in in vitro studies and showed a strong and broad spectrum of antitumor activities both in vitro in various tumor cell lines and in vivo in mouse xenograft models.

Managed by:
2. Pharma Research and Early Development
Partner:
Chugai
1. Oncology
RG7356
solid tumors
4. Phase 1

Description/Summary:

RG7356 is a humanized monoclonal antibody targeting CD44 designed to inhibit binding of CD44 to hyaluronic acid and thereby disrupt CD44-positive tumor cell-cell and cell-matrix interactions.

Managed by:
2. Pharma Research and Early Development
Partner:
Arius
1. Oncology
RG7388
solid and hematological tumors
4. Phase 1

Description/Summary:

RG7388 is an oral, selective, small molecule MDM2 antagonist that inhibits binding of MDM2 to p53. Blocking the MDM2-p53 interaction stabilizes p53 and activates p53-mediated cell death and inhibition of cell growth.

Managed by:
2. Pharma Research and Early Development
Roche Only
1. Oncology
RG7420
solid tumors
4. Phase 1

Description/Summary:

RG7420, a selective small molecule inhibitor of MEK, also known as mitogen activated protein kinase kinase (MAPKK), is a key component of the RAS/RAF/MEK/ERK pathway, which is frequently activated in human tumors. Inappropriate activation of the MEK/ERK pathway promotes cell growth in the absence of exogenous growth factors.

Managed by:
3. Genentech Research and Early Development
Roche Only
1. Oncology
RG7440
solid tumors
4. Phase 1

Description/Summary:

RG7440 is a small molecule pan-Akt inhibitor. The PI3K/Akt/mTOR pathway regulates cell growth and survival.

Managed by:
3. Genentech Research and Early Development
Partner:
Array BioPharma
1. Oncology
RG7446
solid tumors
4. Phase 1

Description/Summary:

Tumor immunotherapy is the use of the immune system to reject cancer.

Managed by:
3. Genentech Research and Early Development
Roche Only
1. Oncology
RG7450
prostate cancer
4. Phase 1

Description/Summary:

RG7450 (Anti-STEAP1, DSTP3086S, RG7450) is an antibody drug conjugate (ADC) that consists of a humanized monoclonal antibody directed against STEAP1, a six-transmembrane epithelial antigen of the prostate 1, conjugated to an anti-mitotic agent, monomethyl auristatin E (MMAE). STEAP1 is a membrane protein that is overexpressed in prostate cancer.

Managed by:
3. Genentech Research and Early Development
Partner:
Seattle Genetics
1. Oncology
RG7458
ovarian cancer
4. Phase 1

Description/Summary:

An antibody drug conjugate (ADC) is a monoclonal antibody that selectively delivers potent anti-cancer agents to tumor cells.

Managed by:
3. Genentech Research and Early Development
Partner:
Seattle Genetics
1. Oncology
RG7598
multiple myeloma
4. Phase 1

Description/Summary:

An antibody drug conjugate (ADC) is a monoclonal antibody that selectively delivers potent anti-cancer agents to tumor cells.

Managed by:
3. Genentech Research and Early Development
Partner:
Seattle Genetics
1. Oncology
RG7599
non-small cell lung cancer, ovarian cancer
4. Phase 1

Description/Summary:

An antibody drug conjugate (ADC) is a monoclonal antibody that selectively delivers potent anti-cancer agents to tumor cells.

Managed by:
3. Genentech Research and Early Development
Partner:
Seattle Genetics
1. Oncology
RG7600
pancreatic and ovarian cancer
4. Phase 1

Description/Summary:

An antibody drug conjugate (ADC) is a monoclonal antibody that selectively delivers potent anti-cancer agents to tumor cells.

Managed by:
3. Genentech Research and Early Development
Partner:
Seattle Genetics
1. Oncology
RG7601
relapsed or refractory chronic lymphocytic leukaemia
4. Phase 1

Description/Summary:

RG7601 is a novel small molecule Bcl-2 selective inhibitor designed to restore apoptosis, also known as programmed cell death, by blocking the function of a pro-survival Bcl-2 family protein. The Bcl-2 family proteins, which are expressed at high levels in many tumors, play a central role in regulating apoptosis and, consequently, are thought to impact tumor formation, tumor growth and resistance.

Managed by:
1. Roche Group
Partner:
Abbott, WEHI
1. Oncology
RG7602
solid tumors or lymphoma
4. Phase 1

Description/Summary:

Checkpoint kinase 1 (ChK1) is a protein kinase that regulates tumor cells’ response to DNA damage, often caused by treatment with chemotherapy. In response to DNA damage, ChK1 blocks cell cycle progression in order to allow for repair of damaged DNA. Inhibiting ChK1 in combination with chemotherapy may enhance tumor cell death by preventing these cells from recovering from DNA damage. RG7602 is a small molecule ChK1 selective inhibitor designed to prevent tumor cells from recovering from DNA damage.

Managed by:
3. Genentech Research and Early Development
Partner:
Array BioPharma
1. Oncology
RG7604
solid tumors
4. Phase 1

Description/Summary:

PI3 Kinase is an oncogene that is commonly mutated in cancer. The PI3K/Akt/mTOR pathway regulates cell growth and survival.

Managed by:
3. Genentech Research and Early Development
Roche Only
1. Oncology
RG7636
metastatic melanoma
4. Phase 1

Description/Summary:

An antibody drug conjugate (ADC) is a monoclonal antibody that selectively delivers potent anti-cancer agents to tumor cells.

Managed by:
3. Genentech Research and Early Development
Partner:
Seattle Genetics
1. Oncology
RG7666
progressive or recurrent high-grade glioma
4. Phase 1

Description/Summary:

RG7666 (GDC-0084) is a novel, oral, small molecule PI3 kinase inhibitor. PI3 Kinase is an oncogene that is commonly mutated in cancer. The PI3K/Akt/mTOR pathway regulates cell growth and survival.

Managed by:
3. Genentech Research and Early Development
Roche Only
1. Oncology
RG7741
solid tumors or lymphoma
4. Phase 1

Description/Summary:

Checkpoint kinase 1 (ChK1) is a protein kinase that regulates tumor cells' response to DNA damage, often caused by treatment with chemotherapy. In response to DNA damage, ChK1 blocks cell cycle progression in order to allow for repair of damaged DNA. Inhibiting ChK1 in combination with chemotherapy may enhance tumor cell death by preventing these cells from recovering from DNA damage. RG7741 (GDC-0575) is a small molecule ChK1 selective inhibitor designed to prevent tumor cells from recovering from DNA damage.

Managed by:
3. Genentech Research and Early Development
Roche Only
1. Oncology
RG7853
non-small cell lung cancer
4. Phase 1

Description/Summary:

RG7853 is a small molecule that is designed to inhibit anaplastic lymphoma kinase (ALK) involved in the pathology of non-small cell lung cancer.

Managed by:
2. Pharma Research and Early Development
Partner:
Chugai
1. Oncology
RG1273 pertuzumab
Perjeta
HER2-positive breast cancer neoadjuvant
3. Phase 2
2013

Description/Summary:

Pertuzumab is a humanized monoclonal antibody designed to prevent HER2 dimerisation, a process that is believed to play an important role in the growth and formation of several different cancer types. The mechanism of action of pertuzumab is thought to be complementary to Herceptin, as both bind to the HER2 receptor but on different regions. The goal of combining pertuzumab with Herceptin and chemotherapy is to determine if the combination may provide a more comprehensive blockade of HER signalling pathways.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG1273 pertuzumab
Perjeta
HER2-positive gastric cancer
3. Phase 2
post 2016

Description/Summary:

Pertuzumab is a humanized monoclonal antibody designed to prevent HER2 dimerisation, a process that is believed to play an important role in the growth and formation of several different cancer types. The mechanism of action of pertuzumab is thought to be complementary to Herceptin, as both bind to the HER2 receptor but on different regions. The goal of combining pertuzumab with Herceptin and chemotherapy is to determine if the combination may provide a more comprehensive blockade of HER signalling pathways.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG1273 pertuzumab
Perjeta
2nd line HER2-positive metastatic breast cancer
3. Phase 2
post 2014

Description/Summary:

Pertuzumab is a humanized monoclonal antibody designed to prevent HER2 dimerisation, a process that is believed to play an important role in the growth and formation of several different cancer types. The mechanism of action of pertuzumab is thought to be complementary to Herceptin, as both bind to the HER2 receptor but on different regions. The goal of combining pertuzumab with Herceptin and chemotherapy is to determine if the combination may provide a more comprehensive blockade of HER signalling pathways.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG3502 trastuzumab-DM1
Kadcyla
advanced HER2-positive gastric cancer
3. Phase 2
2015

Description/Summary:

Trastuzumab emtansine (T–DM1) is a novel antibody–drug conjugate that combines the therapeutic effect of trastuzumab (the active substance of Herceptin) with intracellular delivery of DM1, a highly potent chemotherapy agent, to specifically target HER2-positive tumors.

Managed by:
1. Roche Group
Partner:
ImmunoGen
1. Oncology
RG3502 trastuzumab-DM1
Kadcyla
early HER2-positive breast cancer
3. Phase 2

Description/Summary:

Trastuzumab emtansine (T–DM1) is a novel antibody–drug conjugate that combines the therapeutic effect of trastuzumab (the active substance of Herceptin) with intracellular delivery of DM1, a highly potent chemotherapy agent, to specifically target HER2-positive tumors.

Managed by:
1. Roche Group
Partner:
ImmunoGen
1. Oncology
RG3616 vismodegib
Erivedge
operable basal cell carcinoma
3. Phase 2

Description/Summary:

Vismodegib is an oral, small molecule targeted medicine designed to selectively inhibit abnormal signaling in the Hedgehog pathway, which is an underlying molecular driver of BCC.

Managed by:
1. Roche Group
Partner:
Curis
1. Oncology
RG3638 onartuzumab
1st line non-squamous non-small cell lung cancer
3. Phase 2

Description/Summary:

Onartuzumab, MetMAb, is a first-in-class monoclonal monovalent (one-armed) antibody designed to inhibit Met signalling in cancer cells by binding to the extracellular domain of Met, thereby blocking HGF-mediated activation. HGF/Met signalling is activated through over expression of either HGF and/or Met in tumours as well as through activating mutations in Met. Activation of Met signalling drives tumour growth and has also been linked to tumour angiogenesis and metastatic potential.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG3638 onartuzumab
1st line squamous non-small cell lung cancer
3. Phase 2

Description/Summary:

Onartuzumab, MetMAb, is a first-in-class monoclonal monovalent (one-armed) antibody designed to inhibit Met signalling in cancer cells by binding to the extracellular domain of Met, thereby blocking HGF-mediated activation. HGF/Met signalling is activated through over expression of either HGF and/or Met in tumours as well as through activating mutations in Met. Activation of Met signalling drives tumour growth and has also been linked to tumour angiogenesis and metastatic potential.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG3638 onartuzumab
Avastin-naïve recurrent glioblastoma
3. Phase 2

Description/Summary:

Onartuzumab, MetMAb, is a first-in-class monoclonal monovalent (one-armed) antibody designed to inhibit Met signalling in cancer cells by binding to the extracellular domain of Met, thereby blocking HGF-mediated activation. HGF/Met signalling is activated through over expression of either HGF and/or Met in tumours as well as through activating mutations in Met. Activation of Met signalling drives tumour growth and has also been linked to tumour angiogenesis and metastatic potential.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG3638 onartuzumab
metastatic colorectal cancer
3. Phase 2

Description/Summary:

Onartuzumab, MetMAb, is a first-in-class monoclonal monovalent (one-armed) antibody designed to inhibit Met signalling in cancer cells by binding to the extracellular domain of Met, thereby blocking HGF-mediated activation. HGF/Met signalling is activated through over expression of either HGF and/or Met in tumours as well as through activating mutations in Met. Activation of Met signalling drives tumour growth and has also been linked to tumour angiogenesis and metastatic potential.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG3638 onartuzumab
triple negative metastatic breast cancer
3. Phase 2

Description/Summary:

Onartuzumab, MetMAb, is a first-in-class monoclonal monovalent (one-armed) antibody designed to inhibit Met signalling in cancer cells by binding to the extracellular domain of Met, thereby blocking HGF-mediated activation. HGF/Met signalling is activated through over expression of either HGF and/or Met in tumours as well as through activating mutations in Met. Activation of Met signalling drives tumour growth and has also been linked to tumour angiogenesis and metastatic potential.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG7160 imgatuzumab
solid tumors
3. Phase 2
2016

Description/Summary:

Imgatuzumab (GA201, RG7160) is a novel, dual-acting humanised, immunoglobulin G1 monoclonal antibody against epidermal growth factor receptor (EGFR), which has been designed to provide enhanced antibody-dependent cellular cytotoxicity (ADCC) activity and increased immune response in combination with signalling inhibition.

Managed by:
2. Pharma Research and Early Development
Roche Only
1. Oncology
RG7204 vemurafenib
Zelboraf
papillary thyroid cancer, BRAF mutation positive
3. Phase 2
post 2016

Description/Summary:

Zelboraf is an oral, small molecule, BRAF kinase inhibitor. The BRAF protein is a key component of the RAS-RAF pathway involved in normal cell growth and survival. Mutations that keep the BRAF protein in an active state may cause excessive pathway signalling, leading to uncontrolled cell growth and survival.

Managed by:
1. Roche Group
Partner:
Plexxikon Inc., member of Daiichi Sankyo Group
1. Oncology
RG7321 pictilisib
solid tumors
3. Phase 2
2016

Description/Summary:

Pictilisib is a PI3 kinase inhibitor currently investigated in a phase II clinical trial. PI3 kinase is an oncogene that is commonly mutated in cancer. The PI3K/Akt/mTOR pathway regulates cell growth and survival.

Managed by:
3. Genentech Research and Early Development
Roche Only
1. Oncology
RG7414 parsatuzumab
solid tumors
3. Phase 2
post 2016

Description/Summary:

Parsatuzumab (anti-EGFL7) is a humanized antibody against EGFL7 (Epidermal Growth Factor Domain-Like 7). EGFL7 is a vascular-restricted secreted protein present in the tracks that surround tumor blood vessels, supporting their survival. Anti-EGFL7 antibody reduces tumor vascular function and is designed to inhibit tumor growth.

Managed by:
3. Genentech Research and Early Development
Roche Only
1. Oncology
RG7422
solid tumors, non-Hodgkin's lymphoma
3. Phase 2
post 2016

Description/Summary:

RG7422 is designed to be a selective, dual inhibitor of PI3 Kinase and mTOR Kinase. PI3 Kinase is an oncogene that is commonly mutated in cancer. The PI3K/Akt/mTOR pathway regulates cell growth and survival.

Managed by:
3. Genentech Research and Early Development
Roche Only
1. Oncology
RG7593
hematological malignancies
3. Phase 2

Description/Summary:

Anti-CD22 is an antibody drug conjugate (ADC) that consists of a humanized IgG1 anti-CD22 monoclonal antibody, conjugated to a anti-mitotic agent, monomethyl auristatin E (MMAE).

Managed by:
3. Genentech Research and Early Development
Partner:
Seattle Genetics
1. Oncology
RG7596
hematological malignancies
3. Phase 2

Description/Summary:

Anti-CD79b is an antibody drug conjugate (ADC) that consists of a monoclonal antibody, conjugated to a potent anti-cancer agent that is selectively delivered to tumor cells.

Managed by:
3. Genentech Research and Early Development
Partner:
Seattle Genetics
1. Oncology
RG7597
metastatic epithelial tumors
3. Phase 2

Description/Summary:

Anti-HER3/EGFR, a dual action antibody, is a phage-derived, human IgG1 monoclonal antibody that is designed to target human epidermal growth factor receptor 3 (HER3) and epidermal growth factor receptor (EGFR).

Managed by:
3. Genentech Research and Early Development
Roche Only
1. Oncology
RG7686
metastatic liver cancer
3. Phase 2

Description/Summary:

RG7686 is a first in class monoclonal humanized anti-glypican 3 antibody being developed as single agent and in combination against metastatic hepatocellular carcinoma. Its therapeutic activity in pre-clinical models was shown to take place via antibody-dependent cell-mediated cytotoxicity (ADCC) and antibody-dependent cellular phagocytosis (ADCP).

Managed by:
2. Pharma Research and Early Development
Partner:
Chugai
1. Oncology
RG1273 pertuzumab
Perjeta
early HER2-positive breast cancer
2. Phase 3
2016

Description/Summary:

Pertuzumab is a humanized monoclonal antibody designed to prevent HER2 dimerisation, a process that is believed to play an important role in the growth and formation of several different cancer types. The mechanism of action of pertuzumab is thought to be complementary to Herceptin, as both bind to the HER2 receptor but on different regions. The goal of combining pertuzumab with Herceptin and chemotherapy is to determine if the combination may provide a more comprehensive blockade of HER signalling pathways.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG1415 erlotinib
Tarceva
adjuvant non-small cell lung cancer
2. Phase 3
2013 EU

Description/Summary:

Tarceva is a small molecule, oral, non-chemotherapy treatment for the treatment of advanced or metastatic NSCLC. It has been shown to potently inhibit EGFR, a protein involved in the growth and development of cancers.

Managed by:
1. Roche Group
Partner:
Astellas Group
1. Oncology
RG3502 trastuzumab-DM1
Kadcyla
1st line HER2-positive metastatic breast cancer
2. Phase 3
2014

Description/Summary:

Trastuzumab emtansine (T–DM1) is a novel antibody–drug conjugate that combines the therapeutic effect of trastuzumab (the active substance of Herceptin) with intracellular delivery of DM1, a highly potent chemotherapy agent, to specifically target HER2-positive tumors.

Managed by:
1. Roche Group
Partner:
ImmunoGen
1. Oncology
RG3502 trastuzumab-DM1
Kadcyla
3rd line HER2-positive metastatic breast cancer
2. Phase 3

Description/Summary:

Trastuzumab emtansine (T–DM1) is a novel antibody–drug conjugate that combines the therapeutic effect of trastuzumab (the active substance of Herceptin) with intracellular delivery of DM1, a highly potent chemotherapy agent, to specifically target HER2-positive tumors.

Managed by:
1. Roche Group
Partner:
ImmunoGen
1. Oncology
RG3638 onartuzumab
metastatic HER2-negative gastric cancer
2. Phase 3
2016

Description/Summary:

Onartuzumab, MetMAb, is a first-in-class monoclonal monovalent (one-armed) antibody designed to inhibit Met signalling in cancer cells by binding to the extracellular domain of Met, thereby blocking HGF-mediated activation. HGF/Met signalling is activated through over expression of either HGF and/or Met in tumours as well as through activating mutations in Met. Activation of Met signalling drives tumour growth and has also been linked to tumour angiogenesis and metastatic potential.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG3638 onartuzumab
metastatic non-small cell lung cancer
2. Phase 3
2014

Description/Summary:

Onartuzumab, MetMAb, is a first-in-class monoclonal monovalent (one-armed) antibody designed to inhibit Met signalling in cancer cells by binding to the extracellular domain of Met, thereby blocking HGF-mediated activation. HGF/Met signalling is activated through over expression of either HGF and/or Met in tumours as well as through activating mutations in Met. Activation of Met signalling drives tumour growth and has also been linked to tumour angiogenesis and metastatic potential.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG435 bevacizumab
Avastin
relapsed ovarian cancer, platinum-resistant
2. Phase 3
2013

Description/Summary:

Avastin is a monoclonal antibody that specifically binds and blocks the biological effects of VEGF (vascular endothelial growth factor). VEGF is the key driver of tumor angiogenesis – a fundamental process required for a tumor to grow and to spread (metastasise) to other parts of the body

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG435 bevacizumab
Avastin
1st line metastatic ovarian cancer
2. Phase 3
2013 US

Description/Summary:

Avastin is a monoclonal antibody that specifically binds and blocks the biological effects of VEGF (vascular endothelial growth factor). VEGF is the key driver of tumor angiogenesis – a fundamental process required for a tumor to grow and to spread (metastasise) to other parts of the body.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG435 bevacizumab
Avastin
adjuvant breast cancer, HER2-negative
2. Phase 3
post 2014

Description/Summary:

Avastin is a monoclonal antibody that specifically binds and blocks the biological effects of VEGF (vascular endothelial growth factor). VEGF is the key driver of tumor angiogenesis – a fundamental process required for a tumor to grow and to spread (metastasise) to other parts of the body.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG435 bevacizumab
Avastin
adjuvant breast cancer, HER2-positive
2. Phase 3
2013

Description/Summary:

Avastin is a monoclonal antibody that specifically binds and blocks the biological effects of VEGF (vascular endothelial growth factor). VEGF is the key driver of tumor angiogenesis – a fundamental process required for a tumor to grow and to spread (metastasise) to other parts of the body.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG435 bevacizumab
Avastin
adjuvant non-small cell lung cancer
2. Phase 3
post 2014

Description/Summary:

Avastin is a monoclonal antibody that specifically binds and blocks the biological effects of VEGF (vascular endothelial growth factor). VEGF is the key driver of tumor angiogenesis – a fundamental process required for a tumor to grow and to spread (metastasise) to other parts of the body.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG435 bevacizumab
Avastin
high-risk carcinoid
2. Phase 3

Description/Summary:

Avastin is a monoclonal antibody that specifically binds and blocks the biological effects of VEGF (vascular endothelial growth factor). VEGF is the key driver of tumor angiogenesis – a fundamental process required for a tumor to grow and to spread (metastasise) to other parts of the body.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG7159 obinutuzumab
diffuse large B-cell lymphoma
2. Phase 3
2016

Description/Summary:

Obinutuzumab, GA101, is the first glycoengineered, type II, humanized anti-CD20 monoclonal antibody. It has a distinct mode of action compared with other anti-CD20s, including MabThera/Rituxan, and was specifically designed to selectively target the CD20 protein on malignant B-cells and to bind with high affinity to the cell surface in a type II configuration.

Managed by:
1. Roche Group
Partner:
Biogen Idec
1. Oncology
RG7159 obinutuzumab
front-line indolent non-Hodgkin's lymphoma
2. Phase 3
post 2016

Description/Summary:

Obinutuzumab, GA101, is the first glycoengineered, type II, humanized anti-CD20 monoclonal antibody. It has a distinct mode of action compared with other anti-CD20s, including MabThera/Rituxan, and was specifically designed to selectively target the CD20 protein on malignant B-cells and to bind with high affinity to the cell surface in a type II configuration.

Managed by:
1. Roche Group
Partner:
Biogen Idec
1. Oncology
RG7159 obinutuzumab
refractory indolent Non Hodgkin's lymphoma
2. Phase 3
2015

Description/Summary:

Obinutuzumab, GA101, is the first glycoengineered, type II, humanized anti-CD20 monoclonal antibody. It has a distinct mode of action compared with other anti-CD20s, including MabThera/Rituxan, and was specifically designed to selectively target the CD20 protein on malignant B-cells and to bind with high affinity to the cell surface in a type II configuration.

Managed by:
1. Roche Group
Partner:
Biogen Idec
1. Oncology
RG7159 obinutuzumab
front-line chronic lymphocytic leukemia
2. Phase 3
2013

Description/Summary:

Obinutuzumab, GA101, is the first glycoengineered, type II, humanized anti-CD20 monoclonal antibody. It has a distinct mode of action compared with other anti-CD20s, including MabThera/Rituxan, and was specifically designed to selectively target the CD20 protein on malignant B-cells and to bind with high affinity to the cell surface in a type II configuration.

Managed by:
1. Roche Group
Partner:
Biogen Idec
1. Oncology
RG7204 vemurafenib
Zelboraf
adjuvant metastatic melanoma, BRAF mutation positive
2. Phase 3
post 2014

Description/Summary:

Zelboraf is an oral, small molecule, BRAF kinase inhibitor. The BRAF protein is a key component of the RAS-RAF pathway involved in normal cell growth and survival. Mutations that keep the BRAF protein in an active state may cause excessive pathway signalling, leading to uncontrolled cell growth and survival.

Managed by:
1. Roche Group
Partner:
Plexxikon Inc., member of Daiichi Sankyo Group
1. Oncology
RG7421+RG7204 cobimetinib+vemurafenib
metastatic melanoma BRAF mutation positive
2. Phase 3
2014

Description/Summary:

RG7421, a selective inhibitor of MEK, also known as mitogen activated protein kinase kinase (MAPKK), is a key component of the RAS/RAF/MEK/ERK pathway, which is frequently activated in human tumors. Inappropriate activation of the MEK/ERK pathway promotes cell growth in the absence of exogenous growth factors. Combination study with the oral, small molecule, BRAF kinase inhibitor Zelboraf.

Managed by:
1. Roche Group
Partner:
Exelixis
1. Oncology
RG105 rituximab
MabThera / Rituxan
non-Hodgkin's lymphoma subcutaneous formulation
1. Filed
2012 EU

Description/Summary:

Rituxan is a monoclonal antibody that binds to a specific protein called CD20 found on the surface of cancerous and normal B-cells. Rituxan works with the body's own immune system to eliminate CD20-positive B-cells. Stem cells (B-cell progenitors that give rise to B-cells) in bone marrow do not have the CD20 protein allowing B-cells to repopulate after Rituxan treatment.

Managed by:
1. Roche Group
Partner:
Biogen Idec, Halozyme
1. Oncology
RG1415 erlotinib
Tarceva
1st line metastatic non-small cell lung cancer, EGFR mutation positive
1. Filed
2012 US

Description/Summary:

Tarceva is a small molecule, oral, non-chemotherapy treatment for the treatment of advanced or metastatic NSCLC. It has been shown to potently inhibit EGFR, a protein involved in the growth and development of cancers.

Managed by:
1. Roche Group
Partner:
Astellas Group
1. Oncology
RG3502 trastuzumab-DM1
Kadcyla
pretreated HER2-positive metastatic breast cancer
1. Filed
2012

Description/Summary:

Trastuzumab emtansine (T–DM1) is a novel antibody–drug conjugate that combines the therapeutic effect of trastuzumab (the active substance of Herceptin) with intracellular delivery of DM1, a highly potent chemotherapy agent, to specifically target HER2-positive tumors.

Managed by:
1. Roche Group
Partner:
ImmunoGen
1. Oncology
RG435 bevacizumab
Avastin
1st line glioblastoma multiforme
1. Filed
2013

Description/Summary:

Avastin is a monoclonal antibody that specifically binds and blocks the biological effects of VEGF (vascular endothelial growth factor). VEGF is the key driver of tumor angiogenesis – a fundamental process required for a tumor to grow and to spread (metastasise) to other parts of the body.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG435 bevacizumab
Avastin
relapsed ovarian cancer, platinum-sensitive
1. Filed
2013 US

Description/Summary:

Avastin is a monoclonal antibody that specifically binds and blocks the biological effects of VEGF (vascular endothelial growth factor). VEGF is the key driver of tumor angiogenesis – a fundamental process required for a tumor to grow and to spread (metastasise) to other parts of the body.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG597 trastuzumab
Herceptin
early HER2-positive breast cancer, subcutaneous formulation
1. Filed
2012 EU

Description/Summary:

Herceptin is a humanised monoclonal antibody, designed to target and block the function of HER2, a protein produced by a specific gene with cancer-causing potential. The mode of action of Herceptin is unique in that it activates the body’s immune system and suppresses HER2 to target and destroy the tumour.

Managed by:
1. Roche Group
Partner:
Halozyme
1. Oncology
RG105 rituximab
MabThera / Rituxan
non-Hodgkin's lymphoma fast infusion
2011

Description/Summary:

Rituxan is a monoclonal antibody that binds to a specific protein called CD20 found on the surface of cancerous and normal B-cells. Rituxan works with the body's own immune system to eliminate CD20-positive B-cells. Stem cells (B-cell progenitors that give rise to B-cells) in bone marrow do not have the CD20 protein allowing B-cells to repopulate after Rituxan treatment.

Managed by:
1. Roche Group
Partner:
Biogen Idec
1. Oncology
RG1273 pertuzumab
Perjeta
1st line HER2-positive metastatic breast cancer
2011

Description/Summary:

Pertuzumab is a humanized monoclonal antibody designed to prevent HER2 dimerisation, a process that is believed to play an important role in the growth and formation of several different cancer types. The mechanism of action of pertuzumab is thought to be complementary to Herceptin, as both bind to the HER2 receptor but on different regions. The goal of combining pertuzumab with Herceptin and chemotherapy is to determine if the combination may provide a more comprehensive blockade of HER signalling pathways.

Managed by:
1. Roche Group
Roche Only
1. Oncology
RG3616 vismodegib
Erivedge
advanced basal cell carcinoma
2011

Description/Summary:

Vismodegib is an oral, small molecule targeted medicine designed to selectively inhibit abnormal signaling in the Hedgehog pathway, which is an underlying molecular driver of BCC.

Managed by:
1. Roche Group
Partner:
Curis
1. Oncology
RG7204 vemurafenib
Zelboraf
metastatic melanoma, BRAF mutation positive
2011

Description/Summary:

Zelboraf is an oral, small molecule, BRAF kinase inhibitor. The BRAF protein is a key component of the RAS-RAF pathway involved in normal cell growth and survival. Mutations that keep the BRAF protein in an active state may cause excessive pathway signalling, leading to uncontrolled cell growth and survival.

Managed by:
1. Roche Group
Partner:
Plexxikon Inc., member of Daiichi Sankyo Group

2. Immunology

2. Immunology
CHU
atopic dermatitis
4. Phase 1

Description/Summary:

CIM331 is a humanized monoclonal antibody. It is currently investigated as a therapy for atopic dermatitis.

Managed by:
4. Chugai
Partner:
Roche participation
2. Immunology
CHU
rheumatoid arthritis
4. Phase 1

Description/Summary:

A humanized monoclonal antibody to the interleukin-6 receptor.

Managed by:
4. Chugai
Partner:
Roche participation
2. Immunology
RG7624
autoimmune disease
4. Phase 1

Description/Summary:

RG7624 is a fully human monoclonal antibody designed to specifically and selectively bind to the human interleukin-17 family of cytokines. A Phase I clinical trial evaluating RG6724 for autoimmune disease is ongoing.

Managed by:
3. Genentech Research and Early Development
Partner:
NovImmune
2. Immunology
RG1569 tocilizumab
Actemra / RoActemra
systemic sclerosis
3. Phase 2
post 2014

Description/Summary:

Actemra/RoACTEMRA (tocilizumab) is a humanised monoclonal antibody to the interleukin-6 receptor, inhibiting the activity of interleukin-6 , a protein that plays a major role in the rheumatoid arthritis inflammation process.

Managed by:
1. Roche Group
Partner:
Chugai
2. Immunology
RG7413 etrolizumab
ulcerative colitis
3. Phase 2
post 2016

Description/Summary:

Etrolizumab is a humanized IgG1 MAb targeting the beta 7 integrin subunit. It binds to two integrin receptors, alpha4beta7 and alphaEbeta7. These receptors are required for trafficking and retention in lymphocytes in the gastrointestinal tract and appear to play a role in inflammatory bowel diseases.

Managed by:
3. Genentech Research and Early Development
Roche Only
2. Immunology
RG7415 rontalizumab
systemic lupus erythematosus
3. Phase 2
post 2016

Description/Summary:

Rontalizumab is a recombinant humanized monoclonal antibody to interferon alpha, which recognizes and neutralizes IFN alpha subtypes.

Managed by:
3. Genentech Research and Early Development
Roche Only
2. Immunology
RG7449 quilizumab
asthma
3. Phase 2
post 2016

Description/Summary:

Quilizumab is a humanized monoclonal antibody, targeting the IgE pathway, that binds to the M1 prime segment of membrane IgE. Anti-M1 prime is designed to eliminate the B cells that would develop into plasma cells and produce IgE, rather than binding to and neutralizing existing IgE.

Managed by:
3. Genentech Research and Early Development
Roche Only
2. Immunology
CHU sodium hyaluronate
Suvenyl
enthesopathy
2. Phase 3

Description/Summary:

A phase III study in enthesopathy (lateral epicondylitis, patellar tendinitis, achilles tendinopathy, and plantar fasciitis) is ongoing to evaluate the reduction of pain by Suvenyl due to the alleviation of stress occurring where tendon and ligament meet the bone.

Managed by:
4. Chugai
Partner:
Roche participation
2. Immunology
RG1569 tocilizumab
Actemra / RoActemra
early rheumatoid arthritis
2. Phase 3
2013

Description/Summary:

Actemra/RoACTEMRA (tocilizumab) is a humanised monoclonal antibody to the interleukin-6 receptor, inhibiting the activity of interleukin-6 , a protein that plays a major role in the rheumatoid arthritis inflammation process.

Managed by:
1. Roche Group
Partner:
Chugai
2. Immunology
RG3637 lebrikizumab
severe asthma
2. Phase 3

Description/Summary:

Lebrikizumab is a novel humanized monoclonal antibody designed to specifically block the action of the interleukin-13 cytokine (a signalling protein that serves as a messenger between cells that is increased in some patients with asthma) and so reduce airway inflammation, a key feature of asthma.

Managed by:
1. Roche Group
Roche Only
2. Immunology
RG3648 omalizumab
Xolair
chronic idiopathic urticaria
2. Phase 3
2013

Description/Summary:

Xolair is a monoclonal antibody that specifically targets the antibody IgE (immunoglobulin E), an underlying component of allergic asthma. Xolair is designed to bind to the circulating IgE antibodies in the blood, decreasing the amount of IgE antibodies available to bind to mast cells. With Xolair, fewer IgE antibodies can bind to mast cells, making IgE cross-linking less likely and inhibiting the mast cell's release of those chemicals that can lead to the symptoms of asthma.

Managed by:
1. Roche Group
Partner:
Novartis
2. Immunology
RG3806 octreolin
acromegaly
2. Phase 3
2014

Description/Summary:

Octreolin is an investigational oral form of the peptide octreotide, a somatostatin analog that is commercially available only by injection. It is currently in phase III trials for the treatment of acromegaly, a disorder that results when the body creates excess growth hormone.

Managed by:
1. Roche Group
Roche Only
2. Immunology
RG105 rituximab
MabThera / Rituxan
ANCA-associated vasculitis
1. Filed
2012

Description/Summary:

Rituxan is a monoclonal antibody that binds to a specific protein called CD20 found on the surface of cancerous and normal B-cells. Rituxan works with the body's own immune system to eliminate CD20-positive B-cells. Stem cells (B-cell progenitors that give rise to B-cells) in bone marrow do not have the CD20 protein allowing B-cells to repopulate after Rituxan treatment.

Managed by:
1. Roche Group
Partner:
Biogen Idec
2. Immunology
RG1569 tocilizumab
Actemra / RoActemra
polyarticular-course juvenile idiopathic arthritis
1. Filed
2012

Description/Summary:

Actemra/RoACTEMRA (tocilizumab) is a humanised monoclonal antibody to the interleukin-6 receptor, inhibiting the activity of interleukin-6 , a protein that plays a major role in the rheumatoid arthritis inflammation process.

Managed by:
1. Roche Group
Partner:
Chugai
2. Immunology
RG1569 tocilizumab
Actemra / RoActemra
rheumatoid arthritis, subcutaneous formulation
1. Filed
2012 EU

Description/Summary:

Actemra/RoACTEMRA (tocilizumab) is a humanised monoclonal antibody to the interleukin-6 receptor, inhibiting the activity of interleukin-6 , a protein that plays a major role in the rheumatoid arthritis inflammation process.

Managed by:
1. Roche Group
Partner:
Chugai
2. Immunology
RG1569 tocilizumab
Actemra / RoActemra
rheumatoid arthritis 1st line biologic
2011 US

Description/Summary:

Actemra/RoACTEMRA (tocilizumab) is a humanised monoclonal antibody to the interleukin-6 receptor, inhibiting the activity of interleukin-6 , a protein that plays a major role in the rheumatoid arthritis inflammation process.

Managed by:
1. Roche Group
Partner:
Chugai
2. Immunology
RG1569 tocilizumab
Actemra / RoActemra
rheumatoid arthritis, head-to-head versus adalimumab
2012 EU

Description/Summary:

Actemra/RoACTEMRA (tocilizumab) is a humanised monoclonal antibody to the interleukin-6 receptor, inhibiting the activity of interleukin-6 , a protein that plays a major role in the rheumatoid arthritis inflammation process.

Managed by:
1. Roche Group
Partner:
Chugai

3. Ophthalmology

3. Ophthalmology
RG3645 ranibizumab
Lucentis
sustained delivery age-related macular degeneration/retinal vein occlusion/diabetic macular edema
4. Phase 1

Description/Summary:

Lucentis is a monoclonal antibody fragment. It is designed to bind to and inhibit VEGF (vascular endothelial growth factor), a protein that is believed to play a critical role in the formation of new blood vessels (angiogenesis) and the hyperpermeability (leakiness) of the vessels. In DME, damaged blood vessels leak fluid into the central portion of the retina, called the macula, causing it to swell. The macula is the part of the eye responsible for sharp central vision.

Managed by:
1. Roche Group
Partner:
Novartis, ForSight VISION4
3. Ophthalmology
RG7417 lampalizumab
geographic atrophy associated with AMD
3. Phase 2
post 2016

Description/Summary:

Lampalizumab (anti-Factor D Fab) is a humanized monoclonal antibody fragment targeting complement factor D. It is designed to inhibit complement activation and chronic inflammation in tissues. Complement Factor D is a member of the trypsin family of peptidases and is a component of the alternative complement pathway.

Managed by:
3. Genentech Research and Early Development
Roche Only
3. Ophthalmology
RG3645 ranibizumab
Lucentis
age-related macular degeneration (neovascular) 0.5 mg PRN study
2012 US

Description/Summary:

Lucentis is a monoclonal antibody fragment. It is designed to bind to and inhibit VEGF (vascular endothelial growth factor), a protein that is believed to play a critical role in the formation of new blood vessels (angiogenesis) and the hyperpermeability (leakiness) of the vessels. In wet AMD, these blood vessels grow under the retina and leak blood and fluid, causing rapid damage to the macula. The macula is the part of the eye responsible for sharp central vision.

Managed by:
1. Roche Group
Partner:
Novartis
3. Ophthalmology
RG3645 ranibizumab
Lucentis
diabetic macular edema
2011 US

Description/Summary:

Lucentis is a monoclonal antibody fragment. It is designed to bind to and inhibit VEGF (vascular endothelial growth factor), a protein that is believed to play a critical role in the formation of new blood vessels (angiogenesis) and the hyperpermeability (leakiness) of the vessels. In DME, damaged blood vessels leak fluid into the central portion of the retina, called the macula, causing it to swell. The macula is the part of the eye responsible for sharp central vision.

Managed by:
1. Roche Group
Partner:
Novartis

4. Virology

4. Virology
RG7128 mericitabine
hepatitis C
3. Phase 2
2016

Description/Summary:

Mericitabine is an oral, small molecule nucleoside analog NS5B RNA-dependent RNA polymerase inhibitor of hepatitis C viral replication. Intracellular mericitabine is phosphorylaed to two distinct active triphosphates. These triphosphates disable an enzyme required to copy hepatitis C virus RNA, hence viral replication is halted.

Managed by:
1. Roche Group
Partner:
Pharmasset
4. Virology
RG7227 danoprevir
hepatitis C
3. Phase 2
2016

Description/Summary:

Danoprevir is a macrocyclic peptidomimetic small molecule compound that competitively inhibits the HCV NS3/4A protease.

Managed by:
2. Pharma Research and Early Development
Roche Only
4. Virology
RG7667
CMV disease
3. Phase 2

Description/Summary:

A Phase II clinical trial in CMV disease is ongoing.

Managed by:
3. Genentech Research and Early Development
Roche Only
4. Virology
RG7790 setrobuvir
hepatitis C
3. Phase 2
2016

Description/Summary:

Setrobuvir is a potent small molecule non-nucleoside inhibitor of the hepatitis C virus genotype 1 NS5b RNA polymerase.

Managed by:
2. Pharma Research and Early Development
Roche Only

5. CardioMetabolism

5. CardioMetabolism
RG7697
type 2 diabetes
4. Phase 1

Description/Summary:

RG7697 is a dual agonist peptide analogue with biologic homology to both GLP-1 and GIP for the treatment of type 2 diabetes. GLP-1 and GIP are incretin hormones involved in glucose homeostasis as well as regulation of other metabolic processes.

Managed by:
2. Pharma Research and Early Development
Roche Only
5. CardioMetabolism
RG1512 inclacumab
acute coronary syndrome/cardiovascular disease
3. Phase 2
post 2016

Description/Summary:

Inclacumab is a fully human monoclonal Ab designed to neutralize P-selectin, a multifunctional molecule at the interface of inflammation and thrombosis. By inhibiting both inflammatory and thrombotic reactions, anti-P-selectin could be an effective therapy for cardiovascular diseases.

Managed by:
2. Pharma Research and Early Development
Partner:
Genmab
5. CardioMetabolism
RG7652
metabolic disease
3. Phase 2

Description/Summary:

RG7652 (Anti-PCSK9, MPSK3169A) is a monoclonal antibody directed against PCSK9 (proprotein convertase subtilisin/kexin type 9), a secreted protein that regulates blood LDL-c (low-density lipoprotein cholesterol) levels. PCSK9 protein promotes the degradation of low-density lipoprotein receptors in the liver, resulting in increased LDL-c levels in the blood. Anti-PCSK9 is intended to decrease circulating LDL-c levels by inhibiting this protein.

Managed by:
3. Genentech Research and Early Development
Roche Only
5. CardioMetabolism
CHU tofogliflozin
type 2 diabetes
2. Phase 3

Description/Summary:

Tofogliflozin, an oral, small molecule sodium-glucose cotransporter 2 (SGLT2) inhibitor, blocks the activity of SGLT2. SGLT2 is a protein in the kidneys responsible for the reabsorption of filtered glucose to prevent glucose excretion into the urine. Tofogliflozin’s efficacy in increasing renal glucose excretion is currently studied in patients with type 2 diabetes.

Managed by:
4. Chugai
Partner:
Roche participation
5. CardioMetabolism
RG1439 aleglitazar
cardiovascular risk reduction stable cardiovascular disease and type 2 diabetes or pre-diabetes
2. Phase 3
post 2016

Description/Summary:

Aleglitazar is an oral, rationally designed small molecule providing balanced dual peroxisome proliferator-activated receptor (PPAR) α/γ activation. Specifically it combines the improvements in peripheral insulin sensitivity (and therefore glycemic control) associated with PPAR γ activation, with improved management of dyslipidemia, which is commonly associated with PPAR α activation.

Managed by:
1. Roche Group
Roche Only
5. CardioMetabolism
RG1439 aleglitazar
type 2 diabetes
2. Phase 3
2015

Description/Summary:

Aleglitazar is an oral, rationally designed small molecule providing balanced dual peroxisome proliferator-activated receptor (PPAR) α/γ activation. Specifically it combines the improvements in peripheral insulin sensitivity (and therefore glycemic control) associated with PPAR γ activation, with improved management of dyslipidemia, which is commonly associated with PPAR α activation.

Managed by:
1. Roche Group
Roche Only
5. CardioMetabolism
RG1439 aleglitazar
cardiovascular risk reduction post acute coronary syndrome in type 2 diabetes
2. Phase 3
2015

Description/Summary:

Aleglitazar is an oral, rationally designed small molecule providing balanced dual peroxisome proliferator-activated receptor (PPAR) α/γ activation. Specifically it combines the improvements in peripheral insulin sensitivity (and therefore glycemic control) associated with PPAR γ activation, with improved management of dyslipidemia, which is commonly associated with PPAR α activation.

Managed by:
1. Roche Group
Roche Only

6. Neuroscience

6. Neuroscience
RG1662
cognitive disorders
4. Phase 1

Description/Summary:

RG1662 is a small molecule negative allosteric modulator that acts on a specific subset of receptors called gamma-aminobutyric acid (GABA) A receptors alpha 5, GABRA5. They are present in discrete brain regions associated with cognitive processing. A relative increase in GABAergic tone is believed to be present in people with Down syndrome and responsible for cognitive disability.

Managed by:
2. Pharma Research and Early Development
Roche Only
6. Neuroscience
RG7129
Alzheimer's disease
4. Phase 1

Description/Summary:

A small molecule inhibitor of beta-secretase (BACE), a key enzyme in the production of amyloid-beta peptides. These peptides are neurotoxic and form the amyloid plaques which constitute the primary pathology leading to Alzheimer's disease.

Managed by:
2. Pharma Research and Early Development
Roche Only
6. Neuroscience
RG7203
schizophrenia
4. Phase 1

Description/Summary:

RG7203 is a highly potent and selective small molecule inhibitor of phosphodiesterase 10A (PDE10A). Pharmacological inhibition of PDE10A has demonstrated efficacy in preclinical animal models for positive and negative symptoms in schizophrenia as well as pro-cognitive effects.

Managed by:
2. Pharma Research and Early Development
Roche Only
6. Neuroscience
RG7314
autism
4. Phase 1

Description/Summary:

RG7314 is a potent and specific small molecule antagonist of the V1A vasopressin receptor, which is implicated in modulating emotional processing and key social deficits exhibited in patients with Autism spectrum disorders.

Managed by:
2. Pharma Research and Early Development
Roche Only
6. Neuroscience
RG1450 gantenerumab
Alzheimer's disease
3. Phase 2
post 2016

Description/Summary:

Gantenerumab is a fully human monoclonal antibody that binds and neutralises disease-relevant aggregated forms of amyloid-beta: those that accumulate as plaques in the brain and those which interfere with brain-cell functioning.

Managed by:
1. Roche Group
Partner:
Morphosys
6. Neuroscience
RG1577
Alzheimer's disease
3. Phase 2
post 2016

Description/Summary:

RG1577 is a potent small molecule inhibitor of monoamine oxidase-B (MAO-B) which reduces the formation of toxic reactive oxygen species in the brain of Alzheimer’s disease patients where overexpression of MAO-B is postulated to contribute to neuronal damage.

Managed by:
2. Pharma Research and Early Development
Partner:
Evotec
6. Neuroscience
RG1578
depression
3. Phase 2
post 2016

Description/Summary:

RG1578 is a small molecule negative modulator of metabotropic glutamate 2/3 receptor that plays an important role in affective and cognitive functions in the central nervous system. RG1578 has exhibited robust antidepressant and cognitive enhancing effects in a broad range of preclinical models and is currently studied for the treatment of depressive disorders.

Managed by:
2. Pharma Research and Early Development
Roche Only
6. Neuroscience
RG1678 bitopertin
obsessive compulsive disorder
3. Phase 2
post 2016

Description/Summary:

Bitopertin is an oral, small molecule first-in-class glycine reuptake inhibitor (GRI). Bitopertin enhances N-methyl-D-aspartate (NMDA) receptor activity, thereby targeting an important pathway in the treatment of psychiatric disorders, especially schizophrenia.

Managed by:
1. Roche Group
Roche Only
6. Neuroscience
RG7090
treatment-resistant depression
3. Phase 2
2016

Description/Summary:

RG7090 is a small molecule negative modulator of metabotropic glutamate receptor 5 (mGluR5), a receptor in the central nervous system regulating neurotransmitter release, signal transduction, mood and memory formation. Preclinical data has suggested that modulation of mGluR5 functioning is expected to play an important therapeutic role in depression and Fragile X syndrome.

Managed by:
2. Pharma Research and Early Development
Roche Only
6. Neuroscience
RG7412 crenezumab
Alzheimer's disease
3. Phase 2
post 2016

Description/Summary:

Crenezumab is a humanized monoclonal antibody, which binds to amyloid beta (Abeta). Abeta is the main constituent of amyloid plaque in the brains of patients with Alzheimer's disease and is proposed to be causative in the development of the disease.

Managed by:
3. Genentech Research and Early Development
Partner:
AC Immune
6. Neuroscience
SST arbaclofen
autism spectrum disorders
3. Phase 2

Description/Summary:

Arbaclofen is a small molecule that acts as a selective gamma-amino butyric acid type B (GABA-B) receptor agonist. Research suggests that individuals with autism and fragile X syndrome have abnormalities in synaptic transmission. Through the GABA-B receptor, arbaclofen may serve to restore the normal balance at the synapse and correct abnormalities associated with these disorders.

Managed by:
5. Seaside Therapeutics
Partner:
Roche participation
6. Neuroscience
RG1594 ocrelizumab
primary progressive multiple sclerosis
2. Phase 3
2015

Description/Summary:

Ocrelizumab is a humanized monoclonal antibody that selectively targets the CD20-positive B-cells implicated in the inflammatory and neurodegenerative processes of multiple sclerosis (MS), to effectively impact disease progression while maintaining immunosurveillance.

Managed by:
1. Roche Group
Roche Only
6. Neuroscience
RG1594 ocrelizumab
relapsing multiple sclerosis
2. Phase 3
2015

Description/Summary:

Ocrelizumab is a humanized monoclonal antibody that selectively targets the CD20-positive B-cells implicated in the inflammatory and neurodegenerative processes of multiple sclerosis (MS), to effectively impact disease progression while maintaining immunosurveillance.

Managed by:
1. Roche Group
Roche Only
6. Neuroscience
RG1678 bitopertin
schizophrenia; suboptimally controlled symptoms
2. Phase 3
2014

Description/Summary:

Bitopertin is an oral, small molecule first-in-class glycine reuptake inhibitor (GRI). Bitopertin enhances N-methyl-D-aspartate (NMDA) receptor activity, thereby targeting an important pathway in the treatment of psychiatric disorders, especially schizophrenia.

Managed by:
1. Roche Group
Roche Only
6. Neuroscience
RG1678 bitopertin
schizophrenia; persistent, predominant negative symptoms
2. Phase 3
2014

Description/Summary:

Bitopertin is an oral, small molecule first-in-class glycine reuptake inhibitor (GRI). Bitopertin enhances N-methyl-D-aspartate (NMDA) receptor activity, thereby targeting an important pathway in the treatment of psychiatric disorders, especially schizophrenia.

Managed by:
1. Roche Group
Roche Only
6. Neuroscience
SST arbaclofen
fragile X syndrome
2. Phase 3

Description/Summary:

Arbaclofen is a small molecule that acts as a selective gamma-amino butyric acid type B (GABA-B) receptor agonist. Research suggests that individuals with autism and fragile X syndrome have abnormalities in synaptic transmission. Through the GABA-B receptor, arbaclofen may serve to restore the normal balance at the synapse and correct abnormalities associated with these disorders.

Managed by:
5. Seaside Therapeutics
Partner:
Roche participation

7. Other

7. Other
CHU
hemophilia A
4. Phase 1

Description/Summary:

ACE910 is a bispecific antibody that mimics coagulation factor VIII, an essential blood clotting protein. It is currently investigated as a therapy for people with hemophilia A, a congenital bleeding disorder that is caused by deficiency or dysfunction of coagulation factor VIII.

Managed by:
4. Chugai
Partner:
Roche participation

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RG1273

Perjeta

HER2-positive BC neoadj

HER2-positive breast cancer neoadjuvant

 
 

RG435

Avastin

1st line GBM

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RG1273

Perjeta

1st line HER2-pos mBC

1st line HER2-positive metastatic breast cancer

 
 

RG3645

Lucentis

AMD 0.5 mg PRN

age-related macular degeneration (neovascular) 0.5 mg PRN study

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RG3806

acromegaly

acromegaly

 
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