Binimetinib
Deterministic view of the source YAML entity. Clinical authority remains with the cited source IDs and reviewer sign-off state.
| ID | DRUG-BINIMETINIB |
|---|---|
| Type | Drug |
| Aliases | ARRY-162MEK162MektoviБінiметиніб |
| Status | reviewed 2026-04-27 | pending_clinical_signoff |
| Diseases | DIS-MELANOMA |
| Sources | SRC-ESMO-MELANOMA-2024 SRC-NCCN-MELANOMA-2025 |
Drug Facts
| Class | MEK1/2 inhibitor |
|---|---|
| Mechanism | Selective allosteric (non-ATP-competitive) inhibitor of MEK1/MEK2 kinases that bind a pocket adjacent to the ATP site, locking MEK in an inactive conformation. Blocks downstream phosphorylation of ERK1/2 in the constitutively activated RAS/RAF/MEK/ERK pathway, suppressing proliferation and survival signaling in BRAF V600-mutant tumor cells. Combined with a BRAF inhibitor (encorafenib) the doublet mitigates paradoxical MAPK reactivation seen with BRAFi monotherapy and prolongs response duration. Clinical evidence: COLUMBUS (encorafenib + binimetinib vs vemurafenib in BRAF V600 unresectable / metastatic melanoma, mPFS 14.9 vs 7.3 mo, mOS 33.6 vs 16.9 mo). Historically evaluated as the third agent in BEACON-CRC triplet (no OS gain over encorafenib + cetuximab doublet — doublet is the standard for BRAF V600E mCRC). |
| Typical dosing | 45 mg PO BID continuous (every ~12 hours), with or without food, in combination with encorafenib 450 mg PO once daily (COLUMBUS schedule for BRAF V600 melanoma). Dose-modify for hepatic impairment (avoid in moderate-severe per label) and for adverse events: dose level -1 is 30 mg BID; -2 is permanent discontinuation if recurrent G3-4 toxicity. Hold for serous retinopathy / RVO until resolution. |
| Ukraine registered | False |
| NSZU reimbursed | False |
| Ukraine last verified | 2026-04-27 |
Notes
Used exclusively in combination with encorafenib for BRAF V600 melanoma (COLUMBUS) — encorafenib monotherapy is not standard. Mandatory baseline workup: LFTs, CK, LVEF echo, ophthalmologic exam, ECG (for QTc), pregnancy test. Monitor: LFTs + CK every 2 weeks for first 8 weeks then monthly; LVEF echo at 1 month then every 3 months; ophtho for any new visual symptom. Compared with dabrafenib+trametinib the toxicity profile is broadly similar but with less pyrexia and somewhat more retinal events. In UA, access is via cross-border EU centers, EAP, or self-pay; dabrafenib+trametinib remains the НСЗУ-funded BRAFi+MEKi.
Used By
Regimens
REG-ENCORAFENIB-BINIMETINIB-MELANOMA- Encorafenib + binimetinib (BRAF V600E/K melanoma)