drug · small molecule

BRAFTOVI

updated 5mo ago

by $AVBP ArriVent BioPharma, Inc.🔗 ChEMBL

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Small molecule drug with a maximum clinical stage of Approval (across all indications), with 4 approved and 5 investigational indications.

targets

Serine/threonine-protein kinase B-raf

all catalysts(0)

nothing on the calendar yet

Trials studying BRAFTOVI

phase1Open-label Phase 1b Study of Ulixertinib and Cetuximab or Ulixertinib in Combination With Cetuximab and Encorafenib in Patients With Unresectable or Metastatic Colorectal Cancer Who Have Previously Received EGFR or BRAF-directed Therapyrecruitingn=27
phase3A Clinical Trial of Three Study Medicines (Encorafenib, Binimetinib, and Pembrolizumab) in Patients With Advanced or Metastatic Melanomaactive not recruitingn=257
phase2A Study of Encorafenib Plus Cetuximab Taken Together With Pembrolizumab Compared to Pembrolizumab Alone in People With Previously Untreated Metastatic Colorectal Canceractive not recruitingn=108
phase2Encorafenib, Binimetinib and Cetuximab in Subjects With Previously Untreated BRAF-mutant ColoRectal Cancercompletedn=95
phase1PF-07284892 in Participants With Advanced Solid Tumorsterminatedn=53
phase4Surgical or Radiotherapeutic Intervention Concerning Large Singular Stable to Progressive Metastases in Patients With BRAFV600-mutated Melanoma Receiving Treatment With Encorafenib + Binimetinibwithdrawn
—UK ENcorafenib and BInimetinib Real-world Study in Melanomaactive not recruitingn=50
phase4The FLOTILLA Study: Providing Continued Access to The Study Medicines Encorafenib and Binimetinib for Participants in Prior Clinical Trialsrecruitingn=46

News(2)

STAT+: Does Revolution Medicines’ pancreatic cancer drug have even greater potential?
Revolution Medicines' pancreatic cancer drug has not yet been approved — and already talk has shifted to how (and when) its use might be expanded.
stat · 4mo ago
Biomarker-Directed Therapies Move the GI Oncology Paradigm Beyond a One-Size-Fits-All Approach: With Michael J. Pishvaian, MD, PhD
Michael J. Pishvaian, MD, PhD discusses how biomarker-directed strategies, including HER2, CLDN18.2, and KRAS inhibition, are transforming GI cancer care.
onclive · 4mo ago

brand

BRAFTOVI

trade names

Braftovi

generic

ENCORAFENIB

MOA

12.1 Mechanism of Action Encorafenib is a kinase inhibitor that targets BRAF V600E, as well as wild-type BRAF and CRAF in in vitro cell-free assays with IC 50 values of 0.35, 0.47, and 0.3 nM, respectively. Mutations in the BRAF gene, such as BRAF V600E, can result in constitutively activated BRAF kinases that may stimulate tumor cell growth. Encorafenib was also able to bind to other kinases in vitro including JNK1, JNK2, JNK3, LIMK1, LIMK2, MEK4, and STK36 and reduce ligand binding to these kinases at clinically achievable concentrations (≤0.9 µM). Encorafenib inhibited in vitro growth of tumor cell lines expressing BRAF V600 E, D, and K mutations. In mice implanted with tumor cells expressing BRAF V600E , encorafenib induced tumor regressions associated with RAF/MEK/ERK pathway suppression. Encorafenib and binimetinib target two different kinases in the RAS/RAF/MEK/ERK pathway. Compared with either drug alone, coadministration of encorafenib and binimetinib resulted in greater anti-proliferative activity in vitro in BRAF mutation-positive cell lines and greater anti-tumor activity with respect to tumor growth inhibition in BRAF V600E mutant human melanoma xenograft studies in mice. Additionally, the combination of encorafenib and binimetinib delayed the emergence of resistance in BRAF V600E mutant human melanoma xenografts in mice compared to either drug alone. In a BRAF V600E mutant NSCLC patient-derived xenograft model in mice, coadministration of encorafenib and binimetinib resulted in greater anti-tumor activity compared to binimetinib alone, with respect to tumor growth inhibition. Increased tumor growth delay after dosing cessation was also observed with the coadministration compared to either drug alone. In the setting of BRAF-mutant CRC, induction of EGFR-mediated MAPK pathway activation has been identified as a mechanism of resistance to BRAF inhibitors. Combinations of a BRAF inhibitor and agents targeting EGFR have been shown to overcome this resistanc

indication

1 INDICATIONS AND USAGE BRAFTOVI is a kinase inhibitor indicated: Melanoma • in combination with binimetinib, for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-authorized test. ( 1.1 , 2.1 ) Colorectal Cancer (CRC) • in combination with cetuximab and fluorouracil-based chemotherapy, for the treatment of adult patients with metastatic colorectal cancer (mCRC) with a BRAF V600E mutation, as detected by an FDA‑authorized test. ( 1.2 , 2.1 ) • in combination with cetuximab, for the treatment of adult patients with mCRC with a BRAF V600E mutation, as detected by an FDA-authorized test, after prior therapy. ( 1.2 , 2.1 ) Non-Small Cell Lung Cancer (NSCLC) • in combination with binimetinib, for the treatment of adult patients with metastatic non–small cell lung cancer (NSCLC) with a BRAF V600E mutation, as detected by an FDA-authorized test. ( 1.3 , 2.1 ) Limitations of Use BRAFTOVI is not indicated for treatment of patients with wild-type BRAF melanoma, wild-type BRAF CRC, or wild-type BRAF NSCLC. ( 1.4 , 5.2 ) 1.1 BRAF V600E or V600K Mutation–Positive Unresectable or Metastatic Melanoma BRAFTOVI is indicated, in combination with binimetinib, for the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-authorized test [see Dosage and Administration (2.1) ] . 1.2 BRAF V600E Mutation-Positive Metastatic Colorectal Cancer (mCRC) • BRAFTOVI is indicated, in combination with cetuximab and fluorouracil-based chemotherapy , for the treatment of adult patients with metastatic colorectal cancer (mCRC) with a BRAF V600E mutation, as detected by an FDA- authorized test [see Dosage and Administration (2.1) ]. • BRAFTOVI is indicated, in combination with cetuximab, for the treatment of adult patients with mCRC with a BRAF V600E mutation, as detected by an FDA- authorized test, after prior therapy [see Dosage and Administration (2.1) ]. 1.

Data sources

ClinicalTrials.gov · OpenTargets

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News(2)

STAT+: Does Revolution Medicines’ pancreatic cancer drug have even greater potential?

Revolution Medicines' pancreatic cancer drug has not yet been approved — and already talk has shifted to how (and when) its use might be expanded.

stat · 4mo ago

Biomarker-Directed Therapies Move the GI Oncology Paradigm Beyond a One-Size-Fits-All Approach: With Michael J. Pishvaian, MD, PhD

Michael J. Pishvaian, MD, PhD discusses how biomarker-directed strategies, including HER2, CLDN18.2, and KRAS inhibition, are transforming GI cancer care.

onclive · 4mo ago

BRAFTOVI

🐶 often sniffed alongside

targets

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Trials studying BRAFTOVI

News(2)

Report a data issue

comments(0)

BRAFTOVI

🐶 often sniffed alongside

targets

all catalysts(0)

Trials studying BRAFTOVI

News(2)

Report a data issue

comments(0)