MEK1 inhibitors(Dual specificity mitogen-activated protein kinase kinase 1 inhibitors), MEK2 inhibitors(Dual specificity mitogen-activated protein kinase kinase 2 inhibitors)

Therapeutic Areas

NeoplasmsHemic and Lymphatic DiseasesSkin and Musculoskeletal Diseases+ [11]

Active Indication

Histiocytic SarcomaBRAF V600 mutation-positive MelanomaMelanoma+ [49]

Inactive Indication

Acute Myeloid LeukemiaAdvanced breast cancerBRAF V600E Mutation-Positive Melanoma+ [15]

Originator Organization

Exelixis, Inc.

Active Organization

Hoffmann-La Roche, Inc.

Cancer Research UK

Genentech, Inc.

+ [11]

Inactive Organization

F. Hoffmann-La Roche Ltd.

The Vanderbilt-Ingram Cancer Center

Georgetown University

+ [4]

Drug Highest PhaseApproved

First Approval Date

US (10 Nov 2015),

Melanoma

RegulationBreakthrough Therapy (US), Fast Track (US), Orphan Drug (US)

Structure

Molecular FormulaC46H46F6I2N6O8

InChIKeyRESIMIUSNACMNW-BXRWSSRYSA-N

CAS Registry1369665-02-0

122

Clinical Trials associated with Cobimetinib Fumarate

NCT06440850 / RecruitingPhase 2IIT

A Pilot Clinical Trial of Vemurafenib and Cobimetinib as a Redifferentiation Strategy in High-Risk, Radioactive Iodine (RAI) Naïve, BRAFV600E Mutated Differentiated Thyroid Carcinoma Patients Undergoing Initial RAI Therapy

This phase II trial tests how well vemurafenib and cobimetinib work in treating patients with high risk differentiated thyroid carcinoma with BRAFV600E mutation, in preparation for radioactive iodine therapy. Vemurafenib and cobimetinib are used in patients whose cancer has a mutated (changed) form of a gene called BRAF. They are in a class of medications called kinase inhibitors. They work by blocking the action of an abnormal protein that signals cancer cells to multiply. This helps slow or stop the spread of cancer cells. Giving vemurafenib and cobimetinib may work better to treat patients with high risk differentiated thyroid carcinoma with BRAFV600E mutation, in preparation for radioactive iodine therapy.

Start Date30 Nov 2024

Sponsor / Collaborator

City of Hope National Medical Center

[+1]

NCT05756556 / SuspendedPhase 2

A Phase 2a, Open-label Study of T3011 in Combination With Cobimetinib in Patients With Advanced Melanoma

This study will evaluate the efficacy and safety of T3011 in combination with Cobimetinib in patients with advanced melanoma.

Start Date30 Jun 2024

Sponsor / Collaborator

Shenzhen Yinuowei Medical Technology Co., Ltd.Startup

NCT05691504 / RecruitingPhase 1IIT

A Phase 1 Study of APG-1252 (Pelcitoclax) and Cobimetinib in Recurrent Ovarian and Endometrial Cancers

This phase I trial tests the safety, side effects, and best dose of combination therapy with pelcitoclax (APG-1252) and cobimetinib in treating patients with ovarian and endometrial cancers that have come back after a period of improvement (recurrent). APG-1252 is a drug that inhibits activity of proteins that prevent cell death, leading to increased cell death and reduced cell growth. Cobimetinib is used in patients whose cancer has a mutated (changed) form of a gene called BRAF. It is in a class of medications called kinase inhibitors. It works by blocking the action of an abnormal protein that signals cancer cells to multiply. This helps slow or stop the spread of cancer cells. Giving APG-1252 in combination with cobimetinib may shrink or stabilize tumor in patients with recurrent ovarian and endometrial cancers.

Start Date14 Sep 2023

Sponsor / Collaborator

National Cancer Institute

100 Clinical Results associated with Cobimetinib Fumarate

100 Translational Medicine associated with Cobimetinib Fumarate

100 Patents (Medical) associated with Cobimetinib Fumarate

374

Literatures (Medical) associated with Cobimetinib Fumarate

15 Mar 2024·International journal of cancer

BRAF and MEK inhibitor combinations induce potent molecular and immunological effects in NRAS‐mutant melanoma cells: Insights into mode of action and resistance mechanisms

Article

Author: Müller, Anja ; Niessner, Heike ; Sergon, Mildred ; Lesche, Mathias ; Seliger, Barbara ; Tunger, Antje ; Karitzky, Paula C ; Dinter, Lisa ; Meier, Friedegund ; Schmitz, Marc ; Wehner, Rebekka ; Käubler, Theresa ; Wurm, Alexander A ; Mehnert, Marie-Christin ; Dahl, Andreas ; Westphal, Dana ; Beissert, Stefan ; Schulz, Alexander

Abstract:

About 25% of melanoma harbor activating NRAS mutations, which are associated with aggressive disease therefore requiring a rapid antitumor intervention. However, no efficient targeted therapy options are currently available for patients with NRAS‐mutant melanoma. MEK inhibitors (MEKi) appear to display a moderate antitumor activity and also immunological effects in NRAS‐mutant melanoma, providing an ideal backbone for combination treatments. In our study, the MEKi binimetinib, cobimetinib and trametinib combined with the BRAF inhibitors (BRAFi) encorafenib, vemurafenib and dabrafenib were investigated for their ability to inhibit proliferation, induce apoptosis and alter the expression of immune modulatory molecules in sensitive NRAS‐mutant melanoma cells using two‐ and three‐dimensional cell culture models as well as RNA sequencing analyses. Furthermore, NRAS‐mutant melanoma cells resistant to the three BRAFi/MEKi combinations were established to characterize the mechanisms contributing to their resistance. All BRAFi induced a stress response in the sensitive NRAS‐mutant melanoma cells thereby significantly enhancing the antiproliferative and proapoptotic activity of the MEKi analyzed. Furthermore, BRAFi/MEKi combinations upregulated immune relevant molecules, such as ICOS‐L, components of antigen‐presenting machinery and the “don't eat me signal” molecule CD47 in the melanoma cells. The BRAFi/MEKi‐resistant, NRAS‐mutant melanoma cells counteracted the molecular and immunological effects of BRAFi/MEKi by upregulating downstream mitogen‐activated protein kinase pathway molecules, inhibiting apoptosis and promoting immune escape mechanisms. Together, our study reveals potent molecular and immunological effects of BRAFi/MEKi in sensitive NRAS‐mutant melanoma cells that may be exploited in new combinational treatment strategies for patients with NRAS‐mutant melanoma.

01 Feb 2024·Clinical nuclear medicine

The Predictive Value of FDG PET/CT for Determining Progression-Free Survival in Advanced Stage III–IV BRAF-Mutated Melanoma Patients Treated With Targeted Therapy—What Can Be Learned From Progression?

Article

Author: de Wit-van der Veen, Linda J ; Hospers, Geke A P ; Lopez-Yurda, Marta ; Boellaard, Ronald ; van der Veldt, Astrid A M ; Kapiteijn, Ellen W ; Stokkel, Marcel P M ; van den Eertwegh, Alfons J M ; Haanen, John B A G ; Aalbersberg, Else A ; de Vos, Filip Y F L ; van der Hiel, Bernies ; Boers-Sonderen, Marye J ; Aarts, Maureen J B ; de Groot, Jan Willem B

Purpose:

The aims of this study were to investigate whether (early) PERCIST response monitoring with 18F-FDG PET/CT is predictive for progression-free survival (PFS) in unresectable stage III or IV melanoma patients treated with BRAF/MEK inhibitor (MEKi) and to define dissemination patterns at progression with a lesion-based evaluation in direct comparison to baseline to improve our understanding of 18F-FDG PET/CT during BRAF/MEKi.

Patients and Methods:

This prospective multicenter single-arm study included 70 patients with unresectable stage III/IV BRAF-mutated melanoma who underwent contrast-enhanced CT and 18F-FDG PET/CT at baseline and 2 and 7 weeks during treatment with vemurafenib plus cobimetinib and at progression if possible. Tumor response assessment was done with RECIST1.1 and PERCIST. Follow-up PET/CT scans were visually compared with baseline to assess dissemination patterns.

Results:

Using RECIST1.1, PFS was not significantly different between the response groups (P = 0.26). At 2 weeks, PERCIST median PFS was 15.7 months for patients with complete metabolic response (CMR) versus 8.3 months for non-CMR (P = 0.035). The hazards ratio (HR) for progression/death in non-CMR versus CMR was 1.99 (95% confidence interval [CI], 1.03–3.84; P = 0.040) and 1.77 (95% CI, 0.91–3.43; P = 0.0935) when adjusting for lactate dehydrogenase (LDH). At 7 weeks, median PFS for PERCIST CMR was 16.7 months versus 8.5 months for non-CMR (P = 0.0003). The HR for progression/death in the non-CMR group was significantly increased (HR, 2.94; 95% CI, 1.60–5.40; P = 0.0005), even when adjusting for LDH (HR, 2.65; 95% CI, 1.43–4.91; P = 0.0020). At week 7, 18F-FDG PET/CT was false-positive in all 4 (6%) patients with new FDG-avid lesions but CMR of known metastases. When 18F-FDG PET/CT was performed at progressive disease, 18/22 (82%) patients had progression of known metastases with or without new 18F-FDG–avid lesions.

Conclusions:

This study shows that PERCIST response assessment at week 7 is predictive for PFS, regardless of LDH. At 2 weeks, patients with CMR have longer PFS than patients with non-CMR, but different PET parameters should be investigated to further evaluate the added value of early 18F-FDG PET/CT. Disease progression on PET/CT is predominated by progression of known metastases, and new 18F-FDG–avid lesions during BRAF/MEKi are not automatically a sign of recurrent disease.

01 Feb 2024·Melanoma research

Effectiveness, safety and utilization of cobimetinib and vemurafenib in patients with BRAF V600 mutant melanoma with and without cerebral metastasis under real-world conditions in Germany: the non-interventional study coveNIS

Article

Author: Nguyen, Minh Tam ; Zdanowicz-Specht, Agnieszka ; Mohr, Peter ; Schley, Gaston ; Terheyden, Patrick ; Hassel, Jessica C ; Masoudi, Ehsan ; Hoff, Norman-Philipp ; Kaatz, Martin ; Meier, Friedegund ; Tüting, Thomas ; Debus, Dirk ; Kähler, Katharina C ; Stadler, Rudolf ; Göppner, Daniela

Cobimetinib/vemurafenib combination therapy is approved for treatment of adults with unresectable or metastatic BRAF V600 mutated malignant melanoma (mM). The non-interventional post-authorisation safety study coveNIS collected real-world data on cobimetinib/vemurafenib treatment focussing on overall survival (OS), safety and utilization. MM patients with brain metastases are usually excluded from clinical studies. coveNIS observed 2 cohorts: mM patients without (Cohort A) and with cerebral metastases (Cohort B), aiming to close the data gap for the latter population. A direct comparison of the 2 cohorts was not intended. The primary effectiveness objective was OS; the safety objective was the incidence of all and of serious adverse events (AEs). Secondary objectives included progression-free survival (PFS), time to development of cerebral metastasis (Cohort A) and time to central nervous system relapse (Cohort B). All statistical analyses were descriptive. Between 2017 and 2021, 95 patients were included (Cohort A: 54, Cohort B: 41 patients) at 32 sites in Germany. Median OS was 21.6 months in Cohort A, 7.4 months in Cohort B. Median PFS was 6.9 months in Cohort A, 5.2 months in Cohort B. The proportion of patients experiencing any AEs was 83.3% (Cohort A) and 87.8% (Cohort B). The two most common AEs in Cohort A were ‘diarrhoea‘ (37%), ‘vomiting‘ (20.4%) and ‘pyrexia‘ (20.4%); in Cohort B ‘diarrhoea‘ (36.6%) and ‘fatigue‘ (22%). In conclusion, the OS rates in Cohort A and Cohort B of coveNIS are in line with the OS data from other trials with BRAF/MEK inhibitors for mM. No new safety signals were observed.

News (Medical) associated with Cobimetinib Fumarate

03 Jun 2024

·www.globenewswire.com

At ASCO 2024, Treos Bio Reports Key Survival Results for Chemo-Free Regimen of PolyPEPI1018 Peptide Immunotherapy and Roche’s PD-L1 Inhibitor in Late-Stage Colorectal Cancer

PolyPEPI1018 is the first cancer vaccine to demonstrate promising results when combined with a PD-(L)1 inhibitor in late-stage microsatellite stable colorectal cancer (MSS CRC), a form of cancer —representing 96% of all metastatic CRC — historically resistant to checkpoint inhibitor immunotherapy. LONDON and BOSTON, June 03, 2024 (GLOBE NEWSWIRE) -- Treos Bio Limited, a clinical-stage biotechnology company using data science and proprietary biomarkers to develop precision peptide immunotherapies, today announced the presentation of results from its phase 2 OBERTO-301 study of the company’s lead product candidate, PolyPEPI1018, in combination with atezolizumab in patients with late-stage microsatellite stable metastatic colorectal cancer (MSS mCRC) at the 2024 American Society of Clinical Oncology (ASCO) Annual Meeting. PolyPEPI1018 is an off-the-shelf, multi-peptide vaccine that has previously demonstrated the ability to induce immunological responses at both the peripheral and tumor levels, effectively turning immunologically ‘cold’ tumors into ‘hot’ ones. This was observed in first-line maintenance MSS mCRC (OBERTO-101) and late-stage MSS mCRC (OBERTO-201), providing a strong rationale for testing PolyPEPI1018 in combination with PD-(L)1 inhibitors in MSS mCRC. OBERTO-301 is a multicenter, open-label, phase 2 clinical trial, conducted at the Mayo Clinic in Minnesota, Florida and Arizona, evaluating the combination treatment of PolyPEPI1018 and atezolizumab in patients with MSS mCRC who have progressed on two or three prior treatment regimens. The primary endpoint of the study is the incidence and severity of treatment-related adverse events. Secondary endpoints include objective response rate, duration of response, progression-free survival, and overall survival. Key Study Findings: Patient Enrolment and Treatment: The study enrolled 18 patients with refractory non-MSI-H metastatic colorectal cancer who were administered PolyPEPI1018 (1.2 mg) and atezolizumab (1,200 mg) every three weeks. Of these, 67% had undergone three or more prior therapy lines, and 44% had active liver metastasis.Safety and Tolerability: PolyPEPI1018 in combination with atezolizumab was well tolerated, with no unexpected toxicities or serious adverse events related to treatment.Survival Benefits: The median overall survival (mOS) was 12.8 months (95% CI 8.8 - NE) and the 12-months survival was 60%; this compares favorably to the historical data of 7.1 months and 27% respectively for atezolizumab monotherapy in a similar patient population. Differences between the survival of patients with and without liver metastasis were not statistically significant (HR: 0.58 [95% CI 0.18 - 1.90]; P=0.36): Patients without active liver metastases (NLM) had a 12-month overall survival (OS) estimate of 67% and a median OS of 16.5 months.Patients with active liver metastases (LM) had a 12-month OS estimate of 50% and a median OS of 8.6 months. Progression-Free Survival (PFS) and Disease Control Rate (DCR): The median PFS was 2.7 months (95% CI 1.4-4.0), and the DCR was 61%. No tumor responses by RECIST 1.1 were observed.Immune Response and Tumor Microenvironment: PolyPEPI1018-specific CD8+ and/or CD4+ T cell responses were detected in 13 out of 16 subjects (ex vivo FluoroSpot), complemented by humoral responses against multiple PolyPEPI1018-antigens. Patients with available biopsy pairs (n=8) showed significant increases in average PD-L1 expression (IC%, p=0.029) and CD8+ tumor infiltrating lymphocytes (TILs, p=0.019) post-treatment, demonstrating an immune conversion from ‘cold’ to ‘hot’ tumor.Correlation with PFS and Immunological Markers: Patients with increased PFS (>12 weeks) showed significant increases in both post-treatment PD-L1 expression (p=0.007) and TILs (p=0.016) versus patients with PFS ≤ 12 weeks. Pre-treatment levels were not prognostic.T Cell Responses and Survival: Patients with robust CD8+ T cell responses had improved OS compared to patients with poor immunological responses (HR=0.13, p=0.022). Dr. Joleen Hubbard, Deputy Director for Clinical Research at Allina Health Cancer Institute and principal investigator of three clinical studies with PolyPEPI1018 at Mayo Clinic, commented, “MSS mCRC patients represent the largest population of mCRC, most of whom have poor-prognostic metastatic sites, where survival beyond one year with standard care is rare. In this latest study, I was particularly intrigued by the correlative data showing that the combination of PolyPEPI1018 and atezolizumab actually increased TILs and PD-L1 expression, which correlated with improved PFS. I am enthusiastic about the potential of PolyPEPI1018 in the development of new treatment alternatives for this challenging disease.” “We are highly encouraged by the consistency observed across three clinical trials in MSS mCRC in different settings. The survival and biomarker data from this study further highlight the potential benefit of PolyPEPI1018 either as an add-on to standard-of-care or as part of a chemo-free IO-IO combination for treating refractory MSS mCRC. We look forward to progressing PolyPEPI1018 to randomized, controlled trials in combination with chemotherapy, biologics, and PD-(L)1 inhibitor,” added Christopher C. Gallen, M.D., Ph.D., CEO of Treos Bio. The poster can be accessed at http://treosbio.com/index.php/publications-2/ References: Hubbard et al, Safety and Activity of PolyPEPI1018 Combined with Maintenance Therapy in Metastatic Colorectal Cancer: An Open-Label, Multicenter, Phase Ib Study. Clin Cancer Res 2022.Hubbard et al, PolyPEPI1018 Vaccine in Combination with TAS-102 in Participants with Late-Stage Microsatellite-Stable Metastatic Colorectal Cancer (MSS mCRC): A Phase Ib Study to Evaluate Safety, Tolerability, Immunogenicity, and Efficacy (OBERTO-201). ASCO2023.Eng et al, Atezolizumab with or without Cobimetinib versus Regorafenib in Previously Treated Metastatic Colorectal Cancer (IMblaze370): A Multicentre, Open-Label, Phase 3, Randomised, Controlled Trial. Lancet Oncol 2019. About Colorectal Cancer:Colorectal cancer (CRC) is the third most common cancer and cause of cancer-related deaths in the United States and worldwide. There are approximately 1.4 million people living with colorectal cancer in the United States. Current treatments for CRC include surgery and chemotherapy in early stages, and chemotherapy, biologics, and targeted therapies in later stages. Microsatellite stable (MSS) CRC accounts for approximately 85% of all colorectal cancers and approximately 96% of all metastatic CRC. Patients with MSS CRC do not benefit from available immunotherapies. About PolyPEPI1018:PolyPEPI1018, Treos’ lead product candidate, is an immunotherapy in clinical development for the treatment of metastatic colorectal cancer, with plans to incorporate a candidate companion diagnostic in future clinical trials. The therapy is in development as an add-on to first-line maintenance therapy and to third-line treatment. PolyPEPI1018 has been developed using Treos’ proprietary PASCal computational tool to identify Personal EPItopes (PEPIs) likely to induce multiple tumor-specific T cell responses in a patient. Prior to the OBERTO-301 clinical trial, PolyPEPI1018 was evaluated in two Phase Ib clinical trials: OBERTO-101 in the first-line maintenance setting and OBERTO-201 in the advanced, refractory setting of MSS mCRC. These trials explored treatment combinations that had not been previously tested. In the first-line maintenance setting, adding PolyPEPI1018 to fluoropyrimidine and bevacizumab led to unprecedented tumor responses according to RECIST v1.1 and dose-dependent improvements in progression-free survival (PFS). To explore the potential of PolyPEPI1018 in treating advanced, refractory MSS mCRC, Treos adopted a stepwise approach. This involved initially assessing the safety, immunogenicity, and preliminary efficacy of PolyPEPI1018 as an add-on to standard chemotherapy, TAS-102 (OBERTO-201). Following this, the effect of PolyPEPI1018 in combination with an experimental immunotherapy in MSS CRC, atezolizumab, was tested in a similar patient population (OBERTO-301). Treos now plans to advance the testing of PolyPEPI1018 in a randomized, controlled phase 2 study comparing a complex chemo-immunotherapeutic regimen to standard of care. About Treos Bio Limited:Treos Bio develops precision peptide cancer immunotherapies combined with novel biomarkers using proprietary computational data science integrating HLA genetics, tumor profile, and clinical outcome of thousands of real subjects. Treos has conducted three clinical trials in the United States and the European Union of its lead candidate, PolyPEPI1018, an off-the-shelf immunotherapy for the treatment of metastatic colorectal cancer. Treos has completed preclinical development of additional off-the-shelf immunotherapies for ovarian, breast, bladder, gastric, lung cancers, and melanoma. The Company is also developing off-the-shelf immunotherapies personalized to an individual patient’s HLA genotype for several types of solid tumors. Treos has raised $45 million to date. More information can be found at www.treosbio.com. Media Contact: Daniel LevineLevine Media Group+1 (510) 280-5405danny@levinemediagroup.com

Clinical ResultImmunotherapyPhase 2ASCOPhase 3

24 Apr 2024

·www.fiercebiotech.com

Roche's pipeline rethink hits 20% of new molecules as cancer candidates join discard pile

Roche CEO Thomas Schinecker, Ph.D., said the cull has focused on assets that have a “lower likelihood” of success. Roche has performed a little light spring cleaning, sweeping (PDF) a pair of phase 1 solid tumor drugs and an early-stage psychiatric disorder prospect out of the door as part of its update for the first quarter. The culls are part of a broader refocusing that has removed 20% of new molecules from the pipeline in recent quarters. The spring cancer clearout affected belvarafenib and RG6286. Belvarafenib, also known as RG6185 and HM95573, is an oral RAF kinase inhibitor that Roche’s Genentech licensed from Hanmi Pharmaceutical for $80 million upfront in 2016. The candidate was in phase 1 at the time of the deal. Hanmi began a phase 1b study to test belvarafenib in combination with either cobimetinib or cetuximab in 2017. Hanmi, which retained the rights to the asset in South Korea, published data from the phase 1 trial and an expansion study in 2019 and continued to track patients in the phase 1b study to assess the effect of combining belvarafenib with a MEK or EGFR inhibitor. A Roche spokesperson said Genentech was “investigating belvarafenib in two clinical studies in various cancers” but has stopped enrollment in the trials and removed the asset from the portfolio. Genentech will continue to provide study treatment and monitor currently enrolled patients. The cut is part of a wider cull that has seen Roche terminate 20% of its new molecular entities since the third quarter of last year. Roche CEO Thomas Schinecker, Ph.D., said on a media call Wednesday that the cull has focused on assets that have a “lower likelihood” of success. The drugmaker needs to terminate some programs to free up cash to invest in accelerating “a number of projects that have a high likelihood to succeed and have a huge patient impact,” Schinecker said. Roche has split programs into three categories: highly promising prospects it wants to accelerate; assets that don’t warrant further investment because they are unlikely to be first or best in class; and molecules that need to generate more data to show whether they are a priority. Schinecker said the changes will continue in the second quarter, but the pipeline will settle down beyond that. The other newly culled oncology candidate, RG6286, is a bispecific antibody that binds to the colorectal cancer antigen LY6G6D and CD3 on T cells. Genentech began testing the candidate, which is also known as BLYG8824A, in colorectal cancer patients in 2020. The phase 1 clinical trial has an estimated primary completion date of early 2026. Roche also used the update to confirm the removal of camonsertib, also known as RG6526, from phase 1. The Swiss drugmaker told Repare Therapeutics it is returning the rights to the synthetic lethal drug candidate in February, days after the dosing of a phase 2 patient and triggering a $40 million payment. Finally, Roche removed one neuroscience candidate from its phase 1 pipeline and switched horses in an infectious disease. The neuroscience asset, RG6163, was in development psychiatric disorders, but Roche had said little publicly about the program. In complicated urinary tract infections, Roche dropped one LepB inhibitor, RG6319, and switched its focus to another molecule against the same target, RG6436.

Phase 1Phase 2PROTACsLicense out/in

24 Apr 2024

·www.biospace.com

Roche Trims Four Early Assets as Q1 Sales Slip 6% on Currency, COVID Headwinds

Pictured: Roche's building in Shanghai, China/iStock, Robert Way Roche released its first-quarter 2024 earnings results on Wednesday posting a 6% decline in sales compared to the same prior year period, as the company continued to be weighed down by weak demand for COVID-19 products and currency headwinds while narrowly beating analysts’ expectations. In the first quarter of 2024, the pharma group’s sales brought in around $15.79 billion, down from its Q1 2023 earnings of approximately $16.78 billion. The performance of Roche’s pharmaceuticals division likewise slowed by 6% in the quarter, with its sales falling to $11.96 billion from $12.71 billion in the same period last year. CEO Thomas Schinecker in a statement attributed the decline to the ongoing contraction of the COVID-19 market and to the “appreciation of the Swiss franc versus most currencies,” which in turn had a significant adverse impact on the group’s sales reported in Swiss francs. At constant exchange rates, Roche’s earnings grew by 2%. Excluding pandemic-related products, sales increased by 7%. “After this quarter, the COVID-19-related impact on sales is largely behind us,” Schinecker added. The eye treatment Vabysmo (faricimab-svoa) emerged as Roche’s strongest growth driver, bringing in $927.4 million in Q1, a 108% increase compared with the same period in 2023 while beating the analyst consensus. Vabysmo was first approved in February 2022 for wet age-related macular degeneration and diabetic macular edema. The drug picked up another approval in October 2023 for retinal vein occlusion. The blood cancer therapy Polivy (polatuzumab vedotin-piiq) and breast cancer medicine Phesgo (pertuzumab/trastuzumab/hyaluronidase-zzfx) were also strong growth contributors in Q1. These assets brought in $424 million and $273 million, respectively, representing sales increases of 70% and 81%. Roche’s top-performing asset was Ocrevus which secured $1.82 billion in Q1, representing 8% growth from the same time period in 2023. As for its pipeline, the pharma group disclosed in Wednesday’s earnings presentation that it had discontinued the development of four early-stage assets including camonsertinib—which was being trialed in solid tumors—and belvarafenib, which was likewise being assessed for solid tumors in combination with Genentech’s Cotellic (cobimetinib). Roche also terminated two new molecular candidates—one for colorectal cancer and one for psychiatric disorders. Looking forward to the rest of the year, Roche reaffirmed its 2024 outlook and noted in its statement that the company expects a sales increase in the mid-single digit range at constant exchange rates. To meet its forecast, Roche has several milestones lined up including a potential U.S. and European Union approval for crovalimab in paroxysmal nocturnal hemoglobinuria and for subcutaneous Ocrevus in relapsing or primary progressive multiple sclerosis. The pharma group is also preparing for key readouts for the Phase III VERONA study of Venclexta plus azacitidine in first-line myelodysplastic syndrome, as well as the Phase IIb PADOVA trial of prasinezumab in Parkinson’s disease. Tristan Manalac is an independent science writer based in Metro Manila, Philippines. Reach out to him on LinkedIn or email him at tristan@tristanmanalac.com or tristan.manalac@biospace.com.

Drug ApprovalPhase 2Financial StatementPhase 3Phase 1

100 Deals associated with Cobimetinib Fumarate

External Link

KEGG	Wiki	ATC	Drug Bank
D10615	Cobimetinib Fumarate	L01XE38	DB05239

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Histiocytic Sarcoma	US	Genentech, Inc.	28 Oct 2022
BRAF V600 mutation-positive Melanoma	EU	Roche Registration GmbH	20 Nov 2015
BRAF V600 mutation-positive Melanoma	IS	Roche Registration GmbH	20 Nov 2015
BRAF V600 mutation-positive Melanoma	LI	Roche Registration GmbH	20 Nov 2015
BRAF V600 mutation-positive Melanoma	NO	Roche Registration GmbH	20 Nov 2015
Melanoma	US	Genentech, Inc.	10 Nov 2015

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Anaplastic Thyroid Carcinoma	Phase 3	GB	Cancer Research UK	01 Mar 2023
Anaplastic Thyroid Carcinoma	Phase 3	GB	Hoffmann-La Roche Ltd.	01 Mar 2023
BRAF V600 mutation-positive Neoplasms	Phase 3	GB	Cancer Research UK	01 Mar 2023
BRAF V600 mutation-positive Neoplasms	Phase 3	GB	Hoffmann-La Roche Ltd.	01 Mar 2023
Colorectal Cancer	Phase 3	GB	Hoffmann-La Roche Ltd.	01 Mar 2023
Colorectal Cancer	Phase 3	GB	Cancer Research UK	01 Mar 2023
Erdheim-Chester Disease	Phase 3	GB	Cancer Research UK	01 Mar 2023
Erdheim-Chester Disease	Phase 3	GB	Hoffmann-La Roche Ltd.	01 Mar 2023
Glioma	Phase 3	GB	Cancer Research UK	01 Mar 2023
Glioma	Phase 3	GB	Hoffmann-La Roche Ltd.	01 Mar 2023

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03498521 (CUPISCO, CTgov)	Phase 2	Neoplasms	528	platinum (Molecularly-Guided Therapy MGT) Category 1)	mywkzynvgo(rdmgslynam) = qsztcsxhoy cqmoodmqdm (zpiaifeukv, rnathuvuxv - wqebcrtzie) View more	-	14 Jun 2024
				platinum (Chemotherapy Category 1)	mywkzynvgo(rdmgslynam) = drycrnuwlo cqmoodmqdm (zpiaifeukv, ltsgunnvgb - tulghbnxmn) View more
NCT03625141 (TRICOTEL, ASCO2024)	Phase 2	BRAFV600mutation \| NF1 \| NRAS ... View more	65	Atezolizumab (A) + cobimetinib (C) + vemurafenib (V)	lkqaqodwwx(elvepfwbim) = kwkswtorwa iitcwamzux (fjwembizzv, 27 - 51) View more	Positive	24 May 2024
NCT03181100 (NCT03181100, ASCO2024)	Phase 2	thyroid gland poorly differentiated carcinoma RASmutation \| NF1 \| NF2	8	Atezolizumab plus cobimetinib	dnjnmextoq(pmhryvzlvs) = tayflhssgw bajycwvrkj (wqsdhplekq, 12.8 - 33.2) View more	Positive	24 May 2024
				Lenvatinib	dnjnmextoq(pmhryvzlvs) = jnwdbzjsjd bajycwvrkj (wqsdhplekq )
ASCO2024	Not Applicable	Secondary malignant neoplasm of pancreas G12D \| G12V	12	Nab-paclitaxel and Gemcitabine	utjzvhpnpq(wiawnopbvk) = neutropenia and neutrophil support was needed in 6 out of 12 patients urwpfmbnpt (beuftealqu )	Positive	24 May 2024
NCT03201458 (NCT04941287, ASCO2024)	Phase 2	Unresectable Biliary Tract Carcinoma	57	Atezolizumab + Varlilumab	xvrazbwsuw(vxchzxcrqk) = flmnkneabo aqyjherthd (mytttnhzpf ) View more	Negative	24 May 2024
				Cobimetinib + Atezolizumab + Varlilumab	xojyzyzjej(pxmazunyft) = xfrlirgimh lrodyysxnh (waudkobyar ) View more
NCT03625141 (TRICOTEL, CTgov)	Phase 2	Neoplasm Metastasis \| Metastatic melanoma \| BRAF V600 mutation-positive Melanoma	80	Atezolizumab+Cobimetinib+Vemurafenib (Cohort 2 - Cobimetinib, Atezolizumab and Vemurafenib)	lzlhjdtchd(iyjmmmrhdw) = dlchpiykos sjzrnhuadt (mwhkmthivi, bfddnuvfzm - cbnqxgtrcd) View more	-	08 Feb 2024
				Atezolizumab+Cobimetinib (Cohort 1- Cobimetinib and Atezolizumab)	pdwvqpjndh(fncjeuftle) = knliucnyii krgrganecr (gwlmqdxjdv, miagqvmqbx - zirrrblawc) View more
ASH2023	Phase 2	Histiocytic Sarcoma	26	Cobimetinib 60mg	yqedvhebkf(gsvavfqpay) = oofbinppns bhitabccgk (scdhtevivz, 62.62 - 95.26) View more	-	09 Dec 2023
NCT02649972 (CTgov)	Phase 2	Malignant Histiocytic Disorders	35	Cobimetinib	xvvjbevcdd(pcuqxddlty) = ytrjpchjzu cimbzglmap (teeqillgie, tyiekkwdnv - dzcqpxktor) View more	-	18 Nov 2023
NCT03175432 (ESMO2023) Manual	Phase 2	Melanoma BRAF V600E	20	Atezolizumab+ bevacizumab+cobimetinib	upvtjszual(wnzmajadwp) = kdanqdurwy cdqjddimdg (fsjbqsnmqy ) View more	Positive	23 Oct 2023
ESMO2023 Manual	Not Applicable	BRAF mutation positive Melanoma First line BRAF	583	Vemurafenib + Cobimetinib	puzktgqqwj(gwvywpemvk) = alpxizxixu xpvycmdoop (loetufgivq ) View more	Positive	22 Oct 2023
				Dabrafenib + Trametinib	puzktgqqwj(gwvywpemvk) = deospwpjfs xpvycmdoop (loetufgivq ) View more

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