Genentech Research and Early Development operates as an independent center within the Roche Group. Our R&D activities are focused on applying excellent science to discover and develop potential new medicines with the goal of becoming first-in-class or best-in-class therapeutics.
Displaying 47
MOLECULES
Oncology
Immunology
Neuroscience
Metabolism
Infectious Disease
Ophthalmology
Managed by Roche
Molecule
Indication
Phase
Akt Inhibitor (GDC-0068)
Solid tumors
Prostate cancer
GDC-0068 (RG7440) is a small molecule pan-Akt inhibitor. The PI3K/Akt/mTOR pathway regulates cell growth and survival.
A Phase I/II clinical trial evaluating both GDC-0068 and GDC-0980 for castration-resistant prostate cancer, a Phase Ib clinical trial in combination with GDC-0973, a MEK Inhibitor, for solid tumors, and Phase I clinical trials for solid tumors are ongoing.
This molecule was discovered in collaboration with Array BioPharma Inc.
Non-Hodgkin's lymphoma and diffuse large B-cell lymphoma
Anti-CD22 (DCDT2980S, RG7593) is designed to selectively bind to CD22 on hematologic cells.
Mechanism of Action / Target
Antibody drug conjugate; anti-CD22
Status
A Phase II clinical trial evaluating either anti-CD22 ADC or anti-CD79b ADC in combination with Rituxan® (Rituximab) for relapsed or refractory follicular non-Hodgkin's lymphoma and relapsed or refractory diffuse large B-cell lymphoma and a Phase I clinical trial evaluating anti-CD22 ADC in combination with Rituxan® (Rituximab) for hematologic malignancies is ongoing.
This molecule is being developed utilizing Seattle Genetics' ADC technology.
For Rituxan full prescribing information, including Boxed WARNINGS, Medication Guide and additional important safety information, please visit http://www.rituxan.com or call 1-800-821-8590.
Non-Hodgkin's lymphoma and diffuse large B-cell lymphoma
Anti-CD79b (DCDS4501A, RG7596) is designed to selectively bind to CD79b on hematologic cells.
Mechanism of Action / Target
Antibody drug conjugate; anti-CD79b
Status
A Phase II clinical trial evaluating either anti-CD22 ADC or anti-CD79b ADC in combination with Rituxan® (Rituximab) for relapsed or refractory follicular non-Hodgkin's lymphoma and relapsed or refractory diffuse large B-cell lymphoma and a Phase I clinical trial evaluating anti-CD79b ADC in combination with Rituxan® (Rituximab) for hematologic malignancies is ongoing.
This molecule is being developed utilizing Seattle Genetics' ADC technology.
For Rituxan full prescribing information, including Boxed WARNINGS, Medication Guide and additional important safety information, please visit http://www.rituxan.com or call 1-800-821-8590.
Anti-HER3/EGFR (MEHD7945A, RG7597), 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).
Clinical trials are ongoing evaluating anti-HER3/EGFR for metastatic epithelial tumors, metastatic squamous cell carcinoma of the head and neck cancer, and metastatic colorectal cancer.
Anti-MUC16 (DMUC5754A, RG7458) is an antibody drug conjugate (ADC) composed of a monoclonal antibody directed against MUC16, also known as mucin 16, linked to the small molecule, cytotoxic, microtubule-disrupting agent, monomethyl auristatin E (MMAE). MUC16 is a transmembrane protein that can be overexpressed in certain types of cancers.
Mechanism of Action / Target
Antibody drug conjugate, mucin 16 (MUC16)
Status
A Phase I clinical trial evaluating anti-MUC16 ADC for platinum-resistant ovarian cancer is ongoing.
This molecule is being developed utilizing Seattle Genetics' ADC technology.
Anti-NaPi2b (DNIB0600A, RG7599) is an antibody drug conjugate (ADC) comprised of a monoclonal antibody directed against NaPi2b, sodium-dependent phosphate transport protein 2b, link to the small molecule, cytotoxic, microtubule-disrupting agent, monomethyl auristatin E (MMAE). NaPi2b can be overexpressed in certain types of cancer.
Mechanism of Action / Target
Antibody drug conjugate, sodium-dependent phosphate transport protein 2b (NaPi2b)
Status
A Phase I clinical trial evaluating anti-NaPi2b ADC in metastatic non-squamous non−small cell lung cancer and platinum-resistant ovarian cancer is ongoing.
This molecule is being developed utilizing Seattle Genetics' ADC technology.
Anti-PDL1 (MPDL3280A, RG7446) is an engineered monoclonal antibody that targets the ligand PD-L1 (programmed death ligand 1).
Mechanism of Action / Target
Tumor immunotherapy, programmed death ligand 1 (PD-L1)
Status
A Phase I clinical trial evaluating anti-PDL1 for solid tumors, a Phase Ib clinical trial evaluating anti-PDL1 in combination with Avastin® (bevacizumab) for solid tumor, and a Phase I trial evaluating anti-PDL1 in combination with Zelboraf® (vemurafenib) for metastatic melanoma are ongoing. A Phase II trial evaluating anti-PDL1 in patients with metastatic non-small cell lung cancer is planned.
For Avastin full prescribing information, including Boxed WARNINGS and additional important safety information, please visit http://www.avastin.com.
For Zelboraf full prescribing information, including Medication Guide and important safety information, please visit http://www.zelboraf.com.
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.
Mechanism of Action / Target
Antibody drug conjugate, anti-six transmembrane epithelial antigen of the prostate 1 (STEAP1)
Status
A Phase I clinical trial evaluating anti-STEAP1 ADC for metastatic castration-resistant prostate cancer is ongoing.
This molecule is being developed utilizing Seattle Genetics' ADC technology. STEAP1 antibody was in-licensed from Agensys.
Chronic lymphocytic leukemia and non-Hodgkin's lymphoma
*
GDC-0199 (RG7601) is a 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.
Mechanism of Action / Target
Apoptosis, Bcl-2 selective inhibitor
Status
A Phase I trial evaluating GDC-0199 for chronic lymphocytic leukemia and non-Hodgkin's lymphoma is ongoing, and a Phase I trial evaluating GDC-0199 in combination with Rituxan® (Rituximab) for non-Hodgkin's lymphoma is planned.
This molecule is being developed in collaboration with Abbott.
For Rituxan full prescribing information, including Boxed WARNINGS, Medication Guide and additional important safety information, please visit http://www.rituxan.com or call 1-800-821-8590.
Bevacizumab (Avastin) is a monoclonal antibody that is designed to specifically bind and block the biological effects of VEGF (vascular endothelial growth factor) protein on blood vessel cells. The tumor blood supply is thought to be critical to a tumor’s ability to grow and spread in the body (metastasize) to other parts of the body. It is being investigated in a variety of solid cancers.
For Avastin full prescribing information, including Boxed WARNINGS, Medication Guide and additional important safety information, please visit http://www.avastin.com or call 1-877-428-2784.
GDC-0425 (RG7602) is a small molecule ChK1 selective inhibitor designed to prevent tumor cells from recovering from DNA damage.
Checkpoint kinase 1 (ChK1) is a protein kinase that regulates tumor cells' response to DNA damage. In response to DNA damage, ChK1 blocks cell cycle progression in order to allow for repair of damaged DNA. This is being tested for its effect on tumor cell death.
GDC-0575 (RG7741) is a small molecule ChK1 selective inhibitor designed to prevent tumor cells from recovering from DNA damage.
Checkpoint kinase 1 (ChK1) is a protein kinase that regulates tumor cells' response to DNA damage. In response to DNA damage, ChK1 blocks cell cycle progression in order to allow for repair of damaged DNA. This is being tested for its effect on tumor cell death.
GDC-0973 (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.
Mechanism of Action / Target
Receptor tyrosine kinase signaling, mitogen-activated protein kinase (MEK) selective inhibitor
Status
A Phase III and a Phase Ib clinical trial in combination with Zelboraf® (vemurafenib) for metastatic melanoma; a Phase Ib clinical trial in combination with GDC-0068, an Akt Inhibitor, for solid tumors; and a Phase Ib clinical trial in combination with GDC-0941, a PI3 Kinase Inhibitor, for solid tumors are ongoing. A Phase I clinical trial evaluating GDC-0973 as a single agent in solid tumor is ongoing.
GDC-0973 is being developed in collaboration with Exelixis, Inc. and Zelboraf is being developed in collaboration with Plexxikon, Inc. co-developed under a 2006 license and collaboration agreement between Roche/Genentech and Plexxikon, a member of the Daiichi Sankyo Group.
For Zelboraf full prescribing information, including Medication Guide and important safety information, please visit http://www.zelboraf.com.
GDC-0623 (RG7420), 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.
Mechanism of Action / Target
Receptor tyrosine kinase signaling, mitogen-activated protein kinase (MEK) selective inhibitor
Status
A Phase I clinical trial evaluating GDC-0623 for solid tumors is ongoing.
Obinutuzumab, GA101, is a glycoengineered, type II, humanized anti-CD20 monoclonal antibody. It was specifically designed to selectively target the CD20 protein on malignant B-cells.
Onartuzumab, MetMAb, is a 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.
Parsatuzumab (Anti-EGFL7, MEGF0444A, RG7414) antibody is designed to target EGFL7, which has a role in blood vessel formation. Parsatuzumab is being tested on its effect on tumor growth.
Clinical trials are ongoing evaluating parsatuzumab in combination with Avastin®(bevacizumab) for first-line metastatic colorectal cancer and first-line metastatic non-squamous non-small cell lung cancer.For Avastin full prescribing information, including Boxed WARNINGS and additional important safety information, please visit http://www.avastin.com.
Pertuzumab (Perjeta) 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.
For Perjeta full prescribing information, including Boxed WARNINGS, Medication Guide and additional important safety information, please visit http://www.perjeta.com or call:1-888-249-4918.
GDC-0032 (RG7604) is a 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.
GDC-0084 (RG7666) is a 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.
GDC-0980 (RG7422) is small molecule dual inhibitor of both mTOR complexes (TORC1 and TORC2) as well as a Class I PI3 Kinase inhibitor. PI3 Kinase is an oncogene that is commonly mutated in cancer. The PI3K/Akt/mTOR pathway regulates cell growth and survival.
Pictilisib (GDC-0941, RG7321) is a small molecule specific Class I PI3 kinase inhibitor. PI3 Kinase is an oncogene that is commonly mutated in cancer. The PI3K/Akt/mTOR pathway regulates cell growth and survival.
Clinical trails are ongoing evaluating pictilisib for second-line hormone receptor-positive metastatic breast cancer, HER2-negative hormone receptor-positive metastatic breast cancer and first-line metastatic non-small cell lung cancer.
This molecule was discovered by Piramed Ltd., which was acquired by F. Hoffmann-La Roche.
Trastuzumab emtansine (T–DM1) is a novel antibody–drug conjugate that is designed to specifically target cells over expressing HER2. It is being tested in a variety of HER2 positive cancers.
Vemurafenib (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.
For Zelboraf full prescribing information, including Boxed WARNINGS, Medication Guide and additional important safety information, please visit http://www.zelboraf.com/ or call 1-800-FDA-1088.
Vismodegib(Erivedge) is an oral, small molecule designed to selectively inhibit abnormal signaling in the Hedgehog pathway. It is being tested in a variety of cancers.
For Erivedge full prescribing information, including Boxed WARNINGS, Medication Guide and additional important safety information, please visit http://www.erivedge.com or call 1-855-737-4833.
Anti-IL17 (MCAF5352A, RG7624) is a fully human monoclonal antibody designed to specifically and selectively bind to the human interleukin-17 family of cytokines.
Mechanism of Action / Target
Anti-interleukin-17 (IL-17)
Status
Phase I clinical trials evaluating anti-IL17 for autoimmune disease are ongoing.
This molecule is being developed in collaboration with NovImmune.
Etrolizumab (rhuMAb Beta7, RG7413) 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.
Mechanism of Action / Target
Anti-Beta7 integrin subunit
Status
A Phase II clinical trial evaluating etrolizumab for ulcerative colitis is ongoing.
Geographic atrophy associated with age-related macular degeneration
Lampalizumab (Anti-Factor D Fab, FCFD4514S, RG7417) is a humanized monoclonal antibody fragment targeting complement factor D. It is designed to inhibit complement activation in tissues. Complement Factor D is a member of the trypsin family of peptidases and is a component of the alternative complement pathway.
Mechanism of Action / Target
Complement Factor D; antibody fragment
Status
A Phase I/II clinical trial evaluating lampalizumab for geographic atrophy associated with dry age-related macular degeneration is ongoing.
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.
Omalizumab (Xolair) is a monoclonal antibody that specifically targets the antibody IgE (immunoglobulin E). 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.Xolair is being tested in Chronic Idiopathic Urticara (hives)
For Xolair full prescribing information, including Boxed WARNINGS, Medication Guide and additional important safety information, please visit http://www.xolair.com/xolair/index.html or call 1-866-4XOLAIR.
Quilizumab (Anti-M1 prime, MEMP1972A, RG7449) is a humanized monoclonal antibody, targeting the IgE pathway, that binds to the M1 prime segment of membrane IgE. Quilizumab 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.
Mechanism of Action / Target
M1 prime segment of IgE
Status
Phase II clinical trials evaluating Anti-M1 prime Quilizumab for moderate-to-severe allergic asthma are ongoing.
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. It is being tested to see its effect on pain and stress occurring where tendon and ligament meet the bone.
Tocilizumab (Actemra/RoACTEMRA) 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.
For Actemra full prescribing information, including Boxed WARNINGS, Medication Guide and additional important safety information, please visit http://www.actemra.com or call 1-800-FDA-1088.
Bitopertin is an oral, small molecule glycine reuptake inhibitor (GRI). Bitopertin is designed to enhance N-methyl-D-aspartate (NMDA) receptor activity. It is thought that this is an important pathway in psychiatric disorders, especially schizophrenia.
Crenezumab (Anti-Abeta, MABT5102A, RG7412) 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.
Mechanism of Action / Target
Anti-amyloid beta (Abeta)
Status
Phase II clinical trials evaluating crenezumab for Alzheimer's Disease are ongoing.
Genentech, the Banner Alzheimer's Institute, and the National Institutes of Health are collaborating on a trial in cognitively healthy individuals who are likely to develop Alzheimer's disease due to their genetic history. We expect to initiate the trial in early 2013. For more information, please click here.
This molecule is being developed in collaboration with AC Immune SA.
Ocrelizumab is a humanized monoclonal antibody that is designed to target CD20-positive B-cells, which are implicated in the inflammatory and neurodegenerative processes of multiple sclerosis (MS).
Aleglitazar is an oral, small molecule designed to provide balanced dual peroxisome proliferator-activated receptor (PPAR) activation. Its effect on peripheral insulin sensitivity associated with PPAR activation and dyslipidemia is being tested.
Anti-PCSK9 (MPSK3169A, RG7652) 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 levels in the blood. Anti-PCSK9 is intended to decrease circulating LDL-c levels by inhibiting this protein.
Mechanism of Action / Target
Anti-proprotein convertase subtilisin/kexin type 9 (PCSK9)
Status
A Phase II clinical trial evaluating anti-PCSK9 for coronary heart disease (CHD) or high risk of CHD is ongoing.
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.
Ranibizumab: ranibizumab (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. Ranibizumab is being tested for sustained delivery in DME. 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.
For Lucentis full prescribing information, including Boxed WARNINGS, Medication Guide and additional important safety information, please visit http://www.lucentis.com/lucentis/ or call 1-866-724-9394.
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