Alectinib
ALK + non-small cell lung cancer
*
Alectinib is a small molecule designed to selectively target ALK (anaplastic lymphoma kinase).
Mechanism of Action / Target
Alectinib is designed to bind to ALK and block downstream signaling pathways, such as STAT3, PIK3/AKT and MAPK
Status
Phase 1/2 clinical trials evaluating alectinib in patients with ALK-positive NSCLC (non-small cell lung cancer) are ongoing. Phase III trials comparing alectinib with crizotinib in ALK-positive NSCLC patients are ongoing.
Anti-CD20/CD3 MAb
Hematologic malignancies
Anti-CD20/CD3 (BTCT4465A, RG7828) is a humanized full-length T cell–dependent bispecific (TDB) antibody designed to target both CD20 on B cells and CD3 on T cells. This dual targeting antibody is designed to redirect T cells to attack cancer cells.
Mechanism of Action / Target
T cell–dependent bispecific (TDB), CD20 expressing B-Cell malignancies
Anti-MUC16 TDC
Pancreatic and ovarian cancers
Anti-MUC16 (DMUC4064A, RG7882) is a cysteine-engineered THIOMAB™ drug conjugate (TDC) that consists of a humanized monoclonal antibody directed against MUC16-expressing tumor cells, conjugated to an anti-mitotic agent, monomethyl auristatin E (MMAE). Anti-MUC16 TDC is designed to bind to mucin repeats present in both membrane-bound MUC16 and circulating CA125.
Mechanism of Action / Target
THIOMAB drug conjugate, mucin family glycoproteins
This molecule is being developed utilizing Seattle Genetics' ADC technology.
Anti-OX40 MAb
Solid tumors and urothelial carcinoma
Anti-OX40 (MOXR0916, RG7888), a humanized monoclonal antibody, is designed to target OX40, a costimulatory receptor that is selectively expressed on the surface of antigen-experienced T cells. Anti-OX40 functions as an agonist antibody, which results in activation rather than blockade, of the OX40 signaling pathway upon receptor binding.
Mechanism of Action / Target
OX40, a tumor necrosis factor (TNF) receptor family member
Anti-TIGIT MAb
Solid tumors
Anti-TIGIT (MTIG7192A, RG6058) is a fully human monoclonal antibody designed to bind to TIGIT and prevent its interaction with poliovirus receptor (PVR).
Mechanism of Action / Target
T cell immunoglobulin and ITIM domain protein (TIGIT), a member of the immunoglobulin super family, is a novel immune inhibitory receptor
Antibody drug conjugate
Non-Hodgkin's lymphoma
Atezolizumab
Solid tumors
*
Metastatic melanoma
*
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.
Bevacizumab
Newly diagnosed glioblastoma
*
Relapsed platinum-sensitive ovarian cancer
*
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.
ChK1 Inhibitor (GDC-0575)
Solid tumors
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.
Mechanism of Action / Target
Cell cycle signaling, checkpoint kinase 1 (ChK1) inhibitor
This molecule is being developed by Genentech as part of an oncology agreement with Array BioPharma.
Cobimetinib
Solid tumors
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Metastatic melanoma
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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.
Ipatasertib
Gastric cancer
*
Triple negative breast cancer
*
Prostate cancer
*
Ipatasertib (GDC-0068, RG7440) is a small molecule pan-Akt inhibitor. The PI3K/Akt/mTOR pathway regulates cell growth and survival.
Mechanism of Action / Target
Receptor tyrosine kinase signaling, Akt pan-inhibitor
This molecule was discovered in collaboration with Array BioPharma Inc.
Navoximod (IDO Inhibitor)
Solid tumors
Navoximod (NLG919, GDC-0919, RG6078) is a small molecule investigational immunotherapy designed to inhibit IDO (Indoleamine 2,3-dioxygenase), a protein often overproduced by many cancer cells.
Mechanism of Action / Target
Indoleamine 2,3-dioxygenase (IDO) inhibitor
This molecule is being developed in collaboration with NewLink Genetics Corporation.
Obinutuzumab
Diffuse large B-cell lymphoma
*
Front-line indolent non-Hodgkin's lymphoma
*
Refractory indolent Non Hodgkin's lymphoma
*
Front-line chronic lymphocytic leukemia
*
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.
Personalized Cancer Vaccine
Cancer
RG6180 is a messenger RNA (mRNA) based individually tailored, personalized cancer vaccine. Each vaccine will be made using unique neoantigen signatures from an individual patient’s tumor, which is expected to elicit an effective immune response against that patient's tumor.
Mechanism of Action / Target
Vaccines; messenger RNA (mRNA) based
This program is being developed in collaboration with BioNTech.
Pertuzumab
Early HER2-positive breast cancer
*
HER2-positive gastric cancer
*
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.
PI3K Inhibitor (GDC-0077)
Solid tumors and ER+ HER2-negative breast cancer
GDC-0077 (RG6114) is a small molecule PI3 kinase (PI3K) inhibitor. Dysregulation of PI3K signaling is implicated in a broad range of human cancers and activating mutations in the PI3K alpha-isoform gene (PIK3CA) are common oncogenic drivers. The PI3K/Akt/mTOR pathway regulates cell growth and survival.
Mechanism of Action / Target
Receptor tyrosine kinase signaling, phosphoinositide 3-kinase (PI3K) inhibitor
Polatuzumab vedotin
Non-Hodgkin's lymphoma and diffuse large B-cell lymphoma
*
Polatuzumab vedotin (Anti-CD79b, DCDS4501A, RG7596) is an antibody drug conjugate (ADC) composed of a monoclonal antibody directed against CD79b, link to the small molecule, cytotoxic, microtubule-disrupting agent, monomethyl auristatin E (MMAE). Polatuzumab vedotin 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 pinatuzumab vedotin or polatuzumab vedotin in combination with Rituxan® (Rituximab) for relapsed or refractory follicular non-Hodgkin's lymphoma and relapsed or refractory diffuse large B-cell lymphoma 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.
RAF Inhibitor (GDC-5573)
Solid tumors
GDC-5573 (HM95573, RG6185) is a selective small molecule inhibitor of the RAF family kinases designed to inhibit the MAPK pathway, which is frequently activated in human tumors and drives tumor growth.
Mechanism of Action / Target
Rapidly accelerated fibrosarcoma (RAF) kinase; mitogen activated protein kinases (MAPK)
This molecule is being developed in collaboration with Hanmi Pharmaceutical.
SERD (GDC-0927)
ER+ HER2-negative breast cancer
GDC-0927 (SRN-927, RG6047) is a selective estrogen receptor degrader (SERD) that is designed to bind to the estrogen receptor to limit its function. In addition, when SERDs bind to the estrogen receptor, they may be able to change the shape of the receptor in such a way that the cell eliminates it by degradation.
Mechanism of Action / Target
Selective estrogen receptor degrader
Taselisib
HER2-negative metastatic breast cancer
*
Solid tumors and HR+ breast cancer
*
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.
Mechanism of Action / Target
Receptor tyrosine kinase signaling, phosphoinositide 3-kinase (PI3K) inhibitor
Status
Clinical trials are ongoing evaluating GDC-0032 for solid tumor and metastatic hormone receptor-positive breast cancer, and metastatic HER2-negative breast cancer.
Trastuzumab emtansine
1st line HER2-positive metastatic breast cancer
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3rd line HER2-positive metastatic breast cancer
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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
Adjuvant metastatic melanoma, BRAF mutation positive
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Papillary thyroid cancer, BRAF mutation positive
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Metastatic melanoma, BRAF mutation positive
*
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.
Please see accompanying full Prescribing Information and Medication Guide for additional important safety information.
Venetoclax
Chronic lymphocytic leukemia and non-Hodgkin's lymphoma
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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 AbbVie.
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.
Vismodegib
Operable basal cell carcinoma
*
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-ST2 MAb
Asthma
Anti-ST2 (AMG 282, RG6149) is a fully human monoclonal antibody designed to inhibit binding of interleukin-33 (IL-33) to the ST2 receptor.
Mechanism of Action / Target
ST2 receptor; Interleukin-33 (IL-33)
This molecule was in-licensed from Amgen.
BTK Inhibitor (GDC-0853)
Rheumatoid arthritis and lupus
GDC-0853 (RG7845) is an orally administered Bruton’s tyrosine kinase (BTK) inhibitor designed to block B cell proliferation and the resulting excessive immune response seen in autoimmune disorders.
Mechanism of Action / Target
Bruton’s tyrosine kinase inhibitor
Etrolizumab
Ulcerative colitis and Crohn's disease
*
Etrolizumab (rhuMAb Beta7, RG7413) is a humanized IgG1 MAb targeting the beta 7 integrin subunit. It binds to two integrins, alpha4beta7 and alphaEbeta7. These integrins are required for lymphocyte trafficking and retention, respectively, in the gastrointestinal tract and appear to play a role in inflammatory bowel diseases.
Mechanism of Action / Target
Anti-Beta7 integrin subunit
Status
Phase III clinical trials evaluating etrolizumab in ulcerative colitis are ongoing; Phase III clinical trials in Crohn's disease are planned.
GDC-3280
Interstitial lung disease
IL22-Fc
Inflammatory diseases and diabetic foot ulcers
IL22-Fc (UTTR1147A, RG7880) is a recombinant human protein with potential application across multiple inflammatory and metabolic diseases.
Mechanism of Action / Target
Interleukin-22 (IL-22), a member of the IL-10 family of cytokines that activates IL-22R signaling; fusion protein
Lebrikizumab
Idiopathic pulmonary fibrosis and severe atopic dematitis
*
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.
New Molecular Entity
Asthma
RG7990 (BITS7201A) is an investigational medicine designed to target inflammation associated with asthma.
This molecule is being developed in collaboration with NovImmune.
Obinutuzumab
Lupus nephritis and end-stage renal disease
Obinutuzumab, GA101, is a glycoengineered, type II, humanized anti-CD20 monoclonal antibody.
Rituximab
Pemphigus vulgaris
Rituxumab (Rituxan) is a therapeutic antibody that targets and selectively depletes CD20-positive B-cells without targeting stem cells or existing plasma cells. It is being studied in autoimmune diseases with significant unmet medical needs. For full prescribing information, please visit http://www.rituxan.com.
Tocilizumab
Systemic sclerosis
*
Giant Cell Arteritis
*
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.
Anti-Tau
Alzheimer’s Disease
RG6100 is an investigational medicine being evaluated for the potential treatment of Alzheimer’s disease.
Mechanism of Action / Target
Tau
This molecule is being developed in collaboration with AC Immune SA.
Crenezumab
Alzheimer's Disease
*
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)
This molecule is being developed in collaboration with AC Immune SA.
DLK Inhibitor (GDC-0134)
Amyotrophic lateral sclerosis
GDC-0134 (RG6000) is a small molecule dual leucine zipper kinase (DLK) inhibitor being evaluated for the potential treatment of amyotrophic lateral sclerosis. DLK is a neuronally-enriched kinase that is designed to mediate stress-induced cell death. DLK inhibition may exhibit neuroprotective potential.
Mechanism of Action / Target
Dual leucine zipper kinase (DLK)
Gantenerumab
Alzheimer's Disease
*
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.
Nav1.7 Inhibitor (GDC-0310)
Pain
GDC-0310 (RG6029) is an orally administered selective Nav1.7 inhibitor. Nav1.7 is a voltage gated sodium channel that is expressed in peripheral pain sensing neurons and may drive pain signaling.
Mechanism of Action / Target
Nav1.7 sodium channel
This molecule is being developed in collaboration with Xenon.
Ocrelizumab
Primary progressive multiple sclerosis
*
Relapsing multiple sclerosis
*
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).
Anti-Influenza A MAb
Severe and acute influenza
Anti-Influenza A (MHAA4549A, RG7745) is a human monoclonal antibody that binds to a highly conserved epitope on the influenza A hemagglutinin stalk region, which is designed to neutralize the influenza A virus across a broad range of different strains.
Mechanism of Action / Target
Influenza A hemagglutinin protein
Anti-S. aureus TAC
Staphylococcus aureus infections
Anti-S. aureus TAC (DSTA4637S, RG7861) is a THIOMAB™ antibiotic conjugate (TAC) that consists of a human monoclonal antibody directed against Staphylococcus aureus, conjugated to an antiobiotic agent. Anti-S. aureus TAC is designed to bind to the surface of Staphylococcus aureus bacteria.
Mechanism of Action / Target
THIOMAB antibiotic conjugate (TAC); Staphylococcus aureus
This molecule was developed utilizing Seattle Genetics' antibody drug conjugate (ADC) technology and the antibody was discovered in collaboration with Symphogen.
Lampalizumab
Geographic atrophy associated with advanced 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 critical for alternative complement pathway activation which is hypothesized to generate inflammatory responses that contribute to GA development and progression.
Mechanism of Action / Target
Complement Factor D; antibody fragment
Status
A Phase I/II clinical trial evaluating lampalizumab for geographic atrophy associated with advanced age-related macular degeneration is ongoing.
Ranibizumab
Sustained delivery age-related macular degeneration
*
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 wet AMD.
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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