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Trametinib (Mekinist) blocks MEK, the protein one step below BRAF in the growth-signal chain. Paired with dabrafenib it treats BRAF-mutant melanoma, lung, thyroid and other cancers, including brain tumours in children.
Trametinib was approved by the FDA in May 2013 as a single agent for BRAF V600E or V600K metastatic melanoma (METRIC: progression-free survival superior to chemotherapy) and in January 2014 in combination with dabrafenib, the pairing that became standard after COMBI-d and COMBI-v. All later indications are with dabrafenib: adjuvant stage III melanoma (COMBI-AD), BRAF V600E metastatic NSCLC, anaplastic thyroid cancer, tumour-agnostic BRAF V600E solid tumours and paediatric low-grade glioma with an oral solution (2023). The EU authorised Mekinist in 2014. Rash, diarrhoea, reduced ejection fraction, retinal vein occlusion and central serous retinopathy are the MEK-class toxicities; pyrexia dominates the combination.
Reversible, non-ATP-competitive inhibitor of MEK1 and MEK2 kinase activity and activation, blocking ERK phosphorylation downstream of BRAF. Connects to MEK1/2.
1.Trametinib slips into a pocket on MEK1/2.
Background: ADC sequencing, Antigen escape (antigen loss, lineage switch), BCG-unresponsive, Castration-resistant prostate cancer (CRPC), Circulating tumour DNA (ctDNA). Also on OnCo: Resistance: how tumours escape each drug class · Lines of therapy.
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In combination with dabrafenib for unresectable or metastatic melanoma with BRAF V600E or V600K mutations, as detected by an FDA-approved test
Accelerated approval on a surrogate endpoint, with a confirmatory trial required.
In combination with dabrafenib for unresectable or metastatic melanoma with BRAF V600E or V600K mutations, as detected by an FDA-approved test
Confirmed: the accelerated approval of 2014 converted to traditional approval 1.9 years after it was granted.
In combination with dabrafenib for adult and pediatric patients 6 years of age and older with unresectable or metastatic solid tumors with BRAF V600E mutation who have progressed following prior treatment and have no satisfactory alternative treatment options *
Accelerated approval on a surrogate endpoint; the confirmatory requirement was still open 4.2 years later, when the FDA's table was read. source
| Region | Year | Indication |
|---|---|---|
| US | 2013 | BRAF V600E/K unresectable or metastatic melanoma (single agent) |
| US | 2014 | With dabrafenib: metastatic melanoma; later adjuvant melanoma, NSCLC, anaplastic thyroid cancer, tumour-agnostic BRAF V600E solid tumours, paediatric low-grade glioma |
| EU | 2014 | BRAF V600 melanoma alone or with dabrafenib; later NSCLC and adjuvant melanoma |
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BRAF V600E testing is mandatory in childhood high-grade glioma and the combination is a standard at relapse and, increasingly, alongside or before radiotherapy in newly diagnosed disease; it supported the tumour-agnostic approval in children.
Immunotherapy first is the standard for BRAF-mutant advanced melanoma in patients who can wait for a response; targeted therapy is reserved for rapid control or after immunotherapy.
MEK inhibition is a standard option for recurrent low-grade serous ovarian cancer, and the trial validated the MAPK pathway as the disease's therapeutic target, now extended by avutometinib-defactinib.
Rapid BRAF testing is mandatory at diagnosis of anaplastic thyroid cancer, and BRAF-MEK inhibition, increasingly with pembrolizumab and as neoadjuvant therapy, is the standard for BRAF-mutant disease.
Adjuvant dabrafenib-trametinib is a standard for resected stage III BRAF-mutant melanoma alongside adjuvant PD-1 blockade; the choice weighs a finite year of oral therapy against immune side effects.
BRAF plus MEK inhibition is a standard first-line option for BRAF V600E lung cancer, with chemo-immunotherapy as the alternative or subsequent line.
BRAF V600E is a routinely tested lung cancer driver, and BRAF plus MEK inhibition is the standard targeted therapy for it.
BRAF plus MEK inhibitor doublets replaced BRAF monotherapy, and dabrafenib-trametinib became the reference regimen for BRAF-mutant melanoma, later extended to adjuvant use in COMBI-AD.
Query for this drug: (TITLE:"Trametinib" OR ABSTRACT:"Trametinib" OR TITLE:"Mekinist" OR ABSTRACT:"Mekinist") 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 Trametinib, not a curated reading list.
Shares Conjunctival melanoma, BRAF class II and class III mutations (non-V600), BRF113928 cohort C (dabrafenib with trametinib, untreated BRAF V600E), ROAR (Rare Oncology Agnostic Research) basket: BRAF V600E biliary tract cancer cohort.
Shares BRAF class II and class III mutations (non-V600), BRF113928 cohort C (dabrafenib with trametinib, untreated BRAF V600E), BRAF V600E (and V600K), BRAF V600E-mutant non-small-cell lung cancer.
Shares BRAF class II and class III mutations (non-V600), Optic pathway glioma, Glioma (KEGG map), Paediatric low-grade glioma.
Shares Melanoma (KEGG map), BRAF V600E (and V600K), BRAF V600E-mutant non-small-cell lung cancer, NCI-MATCH (EAY131).
Shares COMBI-d, NCI-MATCH (EAY131), Dabrafenib + trametinib, BRAF V600-mutant melanoma.
Shares BRF113928 cohort C (dabrafenib with trametinib, untreated BRAF V600E), BRAF V600E-mutant non-small-cell lung cancer, Dabrafenib + trametinib, RAS / RAF / MEK / ERK (MAPK).
Shares COMBI-AD, COMBI-d, BRAF V600-mutant melanoma, Stage III melanoma (after surgery).
Shares Optic pathway glioma, Selumetinib, MEK1/2, RAS / RAF / MEK / ERK (MAPK).