Vemurafenib
Deterministic view of the source YAML entity. Clinical authority remains with the cited source IDs and reviewer sign-off state.
| ID | DRUG-VEMURAFENIB |
|---|---|
| Type | Drug |
| Aliases | PLX4032RG7204ZelborafВемурафеніб |
| Status | reviewed 2026-04-27 | pending_clinical_signoff |
| Diseases | None declared |
| Sources | SRC-ESMO-MELANOMA-2024 SRC-NCCN-MELANOMA-2025 |
Drug Facts
| Class | BRAF V600 kinase inhibitor |
|---|---|
| Mechanism | First-in-class selective ATP-competitive small-molecule inhibitor of the mutant BRAF V600E (and to a lesser extent V600K, V600D) serine/threonine kinase. By preferentially binding the activated conformation of mutant BRAF, vemurafenib suppresses the constitutive RAS-RAF-MEK-ERK signaling that drives BRAF V600 melanoma; tumor responses are typically rapid (weeks). Monotherapy provided the historical proof-of-concept (BRIM-3, vs dacarbazine: ORR 48% vs 5%, mOS 13.6 vs 9.7 mo) but is now superseded by combination with the MEKi cobimetinib (coBRIM) which mitigates paradoxical RAF activation in BRAF-WT cells and reduces cutaneous SCC / keratoacanthoma incidence. Active in BRAF V600E Erdheim-Chester disease, hairy-cell leukemia (off-label / accelerated), and rare BRAF V600 pediatric tumors. |
| Typical dosing | 960 mg PO BID continuous (~12 h apart), with or without food but consistently. In combination with cobimetinib 60 mg PO daily x 21 days then 7-day break (28-day cycle, coBRIM). Dose level -1 = 720 mg BID; -2 = 480 mg BID; permanent discontinuation if G3-4 toxicity recurs at -2. No formal renal adjustment for CrCl ≥30; caution in severe hepatic impairment. Hold for QTc >500 ms or any clinically significant arrhythmia. |
| Ukraine registered | False |
| NSZU reimbursed | False |
| Ukraine last verified | 2026-04-27 |
Notes
Skin surveillance (full-body dermatologic exam at baseline, every 2 months on therapy, and 6 months post-discontinuation) is mandatory due to high SCC / keratoacanthoma incidence — these are excised but do not require BRAFi discontinuation. Rigorous photoprotection (SPF 50+ broad-spectrum, hat, long sleeves, avoid midday sun) given UVA photosensitivity. Baseline + serial ECG (QTc), LFTs, dermatologic + ophthalmologic exam. Combination with cobimetinib reduces SCC and improves PFS/OS vs monotherapy and is the standard. In contemporary UA practice the BRAFi+MEKi reimbursed under НСЗУ is dabrafenib+trametinib; vemurafenib accessed via EAP / cross-border. Active in non-melanoma BRAF V600E neoplasms (Erdheim-Chester, histiocytosis, occasional hairy-cell leukemia) — niche use.
Used By
No reverse references found in the YAML corpus.