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Binimetinib is the MEK inhibitor partnered with encorafenib; blocking the next step in the same relay stops the tumour rerouting around the BRAF block.
Binimetinib is an allosteric, ATP-non-competitive inhibitor of MEK1 and MEK2, the kinases immediately downstream of BRAF; blocking the next step in the relay stops the tumour rerouting around a BRAF inhibitor. It is given at 45 mg twice daily with encorafenib 450 mg once daily for BRAF V600E/K melanoma (approved June 2018 on COLUMBUS) and BRAF V600E metastatic NSCLC (2023). COLUMBUS showed median PFS of 14.9 versus 7.3 months for vemurafenib (HR 0.54) and median OS of 33.6 months, with less pyrexia than dabrafenib-trametinib. Class effects are retinopathy (serous retinal detachment), CK elevation, left-ventricular dysfunction, rash and diarrhoea, so eye examinations, echocardiograms and CK monitoring are recommended. Whether BRAF/MEK doublets or immunotherapy should come first in BRAF-mutant melanoma remains debated. For a newcomer, binimetinib is the MEK half of the encorafenib pair.
Allosteric, ATP-non-competitive MEK1/2 inhibitor. Connects to BRAF.
1.Binds MEK1/2 outside the ATP site and locks them in an inactive conformation
Source: www.accessdata.fda.gov/drugsatfda_docs/label/2023/210498s009lbl.pdf. Doses are for orientation; the current label governs.
Oral, self-administered, so it is a Part D drug: covered through a stand-alone Part D plan or Medicare Advantage drug benefit, usually on the specialty tier with 25 to 33% coinsurance until the annual cap ($2,000 in 2025, $2,100 in 2026).
Covered for FDA-labelled and NCCN-listed uses, but almost always behind prior authorisation confirming diagnosis, biomarker and line of therapy; dispensed through a specialty pharmacy.
Part D out-of-pocket capped at $2,000 (2025) / $2,100 (2026). Medicare patients cannot use manufacturer co-pay cards; charity funds (PAN, HealthWell, CancerCare) and the Extra Help subsidy are the routes.
Sources: Medicare.gov: Drug coverage (Part D) · Medicare.gov: Costs for Medicare drug coverage (annual out-of-pocket cap). Not medical or financial advice; verify with your plan.
Sources: NICE TA562 · SMC advice: binimetinib. Funding decisions are indication-specific and change monthly; verify with NICE and your treating team.
| Date | Deal | Type | Upfront | Total | Source |
|---|---|---|---|---|---|
| 2019-06-17 | Array BioPharma to Pfizer (incl. Seagen) Encorafenib (Braftovi) and binimetinib (Mektovi) | Acquisition | not disclosed | $11.4bn | source |
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Encorafenib + binimetinib approved for BRAF V600 melanoma
| Region | Year | Indication |
|---|---|---|
| US | 2018 | BRAF V600E/K melanoma with encorafenib |
| US | 2023 | BRAF V600E metastatic NSCLC with encorafenib |
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Encorafenib-binimetinib is approved for BRAF V600E lung cancer and offers a second targeted option, particularly for patients troubled by fever on dabrafenib-trametinib.
Encorafenib with cetuximab became the standard second-line treatment for BRAF V600E disease, and the platform BREAKWATER later moved into first line with chemotherapy added, doubling survival again.
Encorafenib-binimetinib is one of three standard BRAF-MEK doublets for advanced melanoma and is often chosen for its tolerability.
Query for this drug: (TITLE:"Binimetinib" OR ABSTRACT:"Binimetinib" OR TITLE:"Mektovi" OR ABSTRACT:"Mektovi") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Binimetinib, not a curated reading list.
Shares COLUMBUS: encorafenib plus binimetinib versus vemurafenib or encorafenib in BRAF-mutant melanoma, COLUMBUS, Melanoma (KEGG map), BRAF V600E (and V600K).
Shares BEACON CRC, Encorafenib, binimetinib, and cetuximab in BRAF V600E-mutated colorectal cancer (BEACON CRC), Encorafenib, BRAF V600E-mutant colorectal cancer.
Shares COLUMBUS, Encorafenib, BRAF V600-mutant melanoma, BRAF.
Shares PHAROS, BRAF V600E (and V600K), BRAF V600E-mutant non-small-cell lung cancer, BRAF V600-mutant melanoma.
Shares Encorafenib, binimetinib, and cetuximab in BRAF V600E-mutated colorectal cancer (BEACON CRC), Encorafenib, BRAF V600E-mutant colorectal cancer, BRAF.
Shares PHAROS, BRAF V600E-mutant non-small-cell lung cancer, BRAF, RAS / RAF / MEK / ERK (MAPK).
Shares BEACON CRC, BRAF V600E (and V600K), Encorafenib, BRAF.
Shares BEACON CRC, Encorafenib, BRAF V600E-mutant colorectal cancer, BRAF.