Pipeline

RG7440 is a small molecule pan-Akt inhibitor. The PI3K/Akt/mTOR pathway regulates cell growth and survival.§§Oncology§NME§solid tumors§solid tumors§Phase 2§Array BioPharma§gRED

Cancer immunotherapy is the use of the immune system to fight cancer. Atezolizumab (anti-PDL1, RG7446, MPDL3280A) is an engineered monoclonal antibody that targets the ligand PD-L1 (programmed death ligand 1) aiming to prevent cancer immune evasion. A phase II trial evaluating anti-PDL1 for locally advanced or metastatic urothelial bladder cancer is ongoing§§Oncology§AI§bladder cancer§metastatic urothelial bladder cancer§Phase 2§§Roche Group

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.§§Oncology§NME§hematological malignancies§hematological malignancies§Phase 2§Seattle Genetics§gRED

RG7599 (Anti-NaPi2b, DNIB0600A) is an antibody drug conjugate (ADC) comprised of a monoclonal antibody directed against NaPi2b, sodium-dependent phosphate transport protein 2b, linked to the small molecule, cytotoxic, microtubule-disrupting agent, monomethyl auristatin E (MMAE). NaPi2b can be overexpressed in certain types of cancer.§§Oncology§NME§Pt-resistant ovarian cancer§platinum-resistant ovarian cancer§Phase 2§Seattle Genetics§gRED

Venetoclax (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.§§Oncology§AI§diffuse large B cell lymphoma§front-line diffuse large B cell lymphoma§Phase 2§AbbVie/WEHI§Roche Group

PI3 Kinase is an oncogene that is commonly mutated in cancer. The PI3K/Akt/mTOR pathway regulates cell growth and survival. Taselisib is being investigated as a potential treatment for PIK3CA mutation-positive, hormone receptor-positive metastatic breast cancer, PIK3CA mutation-positive squamous non-small cell lung cancer, and other solid tumours.§§Oncology§AI§squamous NSCLC§squamous non-small cell lung cancer§Phase 2§§Roche Group

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).§§Oncology§NME§liver cancer§metastatic liver cancer§Phase 2§Chugai§pRED

Alectinib is a small molecule designed to selectively target ALK (anaplastic lymphoma kinase) and to penetrate and stay in the central nervous system. Alectinib binds ALK, inhibiting downstream malignant pathways that contribute to tumorigenesis and disease progression. Alectinib was approved in Japan in July 2014 and is available under the brand name Alecensa.§§Oncology§NME§Non-small cell lung cancer, 2nd-line§ALK-positive non-small cell lung cancer, second-line treatment§Phase 2§Chugai§Roche Group

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 §Perjeta§Oncology§AI§early HER2-pos BC§early HER2-positive breast cancer§Phase 3§§Roche Group

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. 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 T-DM1 is to determine if the combination may provide a more comprehensive blockade of HER signalling pathways.§Kadcyla + Perjeta§Oncology§AI§HER2-positive breast cancer, neoadjuvant treatment§early HER2-positive breast cancer, neoadjuvant treatment§Phase 3§Immunogen§Roche Group

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.§Kadcyla§Oncology§AI§HER2-pos BC adj§early HER2-positive breast cancer adj§Phase 3§ImmunoGen§Roche Group

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.§Gazyva§Oncology§AI§refractory iNHL§rituximab-refractory indolent Non Hodgkin's lymphoma§Phase 3§Biogen Idec§Roche Group

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.§Zelboraf§Oncology§AI§adj melanoma, BRAF mut pos§adjuvant melanoma, BRAF mutation positive§Phase 3§Plexxikon Inc., member of Daiichi Sankyo Group§Roche Group

Cancer immunotherapy is the use of the immune system to fight cancer. Atezolizumab (anti-PDL1, RG7446, MPDL3280A) is an engineered monoclonal antibody that targets the ligand PD-L1 (programmed death ligand 1) aiming to prevent cancer immune evasion. Atezolizumab is being evaluated in a phase III clinical trial as a potential adjuvant treatment, following surgery and adjuvant cisplatin-based chemotherapy, for patients with non-small cell lung cancer whose tumours express PDL1.§§Oncology§AI§NSCLC, adjuvant treatment, PDL1-selected patients§non-small cell lung cancer, adjuvant treatment, PDL1-selected patients§Phase 3§§Roche Group

Venetoclax (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. with AbbVie§§§§§§§§

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.§§Ophthalmology§NME§geographic atrophy§geographic atrophy associated with AMD§Phase 3§§gRED

RG6013/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.§§Other§NME§hemophilia A§hemophilia A§Phase 2§Chugai§Roche Group

Danoprevir is a macrocyclic peptidomimetic small molecule compound that competitively inhibits the HCV NS3/4A protease.§§Infectious Diseases§NME§HCV§hepatitis C§Phase 2§§pRED

RG7745 (Anti-Influenza A, MHAA4549A) 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. A Phase IIa clinical trial evaluating RG7745 in an influenza challenge model in ongoing.§§Infectious Diseases§NME§influenza A§influenza A§Phase 2§§gRED

RG7795 is an investigational oral small-molecule compound that acts via the Toll-like receptor 7 (TLR7) pathway in hepatitis. TLR7 agonists cause the production of antiviral cytokines and the activation/maturation of immune cells with the potential to enhance immune response.§§Infectious Diseases§NME§hepatitis B§hepatitis B§Phase 2§§pRED

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.§§Immunology§AI§idiopathic pulmonary fibrosis§idiopathic pulmonary fibrosis§Phase 2§§Roche Group

Actemra (tocilizumab) is a humanised monoclonal antibody to the interleukin-6 receptor, inhibiting the activity of interleukin-6. Elevated tissue and serum levels of IL-6 have been implicated in large-vessel vasculitis. Inhibition of IL-6 therefore represents a new and novel approach for the treatment of large-vessel vasculitis.§Actemra§Immunology§AI§large-vessel vasculitis§large-vessel vasculitis§Phase 3§Roche participation§Chugai

MabThera/Rituxan is a monoclonal antibody that binds specifically to a protein called CD20 located on the surface of B cells. MabThera works with the body's 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 MabThera treatment. MabThera has been approved for the treatment of specific autoimmune diseases where B cells are thought to be involved: rheumatoid arthritis and two rare forms of vasculitis. MabThera is also being studied in a global phase III trial in a serious skin condition called pemphigus vulgaris (an autoimmune blistering disease), where preliminary data suggest the medicine may be effective.§MabThera/Rituxan§Immunology§AI§pemphigus vulgaris§pemphigus vulgaris§Phase 3§§Roche Group

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.§§Immunology§NME§severe asthma§severe asthma§Phase 3§§Roche Group

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.§§Immunology§AI§Crohn's disease§Crohn's disease§Phase 3§§Roche Group

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.§§Immunology§NME§ulcerative colitis§ulcerative colitis§Phase 3§§Roche Group

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.§§Neuroscience§NME§Alzheimer's disease§Alzheimer's disease§Phase 2§Evotec§pRED

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.§§Neuroscience§NME§Down syndrome§Down syndrome§Phase 2§§pRED

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.§§Neuroscience§NME§obsessive compulsive disorder§obsessive compulsive disorder§Phase 2§§Roche Group

Olesoxime (RG6083) is an investigational medicine being tested for its potential ability to preserve healthy motor nerve cells. Olesoxime is a cholesterol-like compound that binds to proteins in cells and designed to reduce the release of cell death factors and promote the survival of motor cells. Olesoxime is believed to work by preserving the function of mitochondria, the powerhouse of cells.§§Neuroscience§NME§spinal muscular atrophy§spinal muscular atrophy§Phase 2§Trophos acquisition§Roche Group

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.§§Neuroscience§NME§TRD§treatment-resistant depression§Phase 2§§pRED

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.§§Neuroscience§NME§autism§autism§Phase 2§§pRED

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.§§Neuroscience§NME§Alzheimer's disease§Alzheimer's disease§Phase 2§AC Immune§gRED

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.§§Neuroscience§NME§Alzheimer's disease§Alzheimer's disease§Phase 3§Morphosys§Roche Group

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.§§Neuroscience§AI§PPMS§primary progressive multiple sclerosis§Phase 3§§Roche Group

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.§§Neuroscience§NME§RMS§relapsing multiple sclerosis§Phase 3§§Roche Group

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.§Kadcyla§Oncology§AI§HER2-pos adv NSCLC§HER2-positive advanced non-small cell lung cancer§Phase 2§§Roche Group

RG6046 (GDC-0810, ARN-810) 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.§§Oncology§NME§metastatic ER-pos., HER2-neg. BC§metastatic estrogen receptor-positive, HER2-negative breast cancer§Phase 2§Seragon acquisition§gRED

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§§Oncology§NME§solid tumors & PVNS§solid tumors & pigmented villonodular synovitis§Phase 2§§pRED