Dabrafenib mesylate CAS 1195768-06-9

Dabrafenib mesylate More Info

Dabrafenib mesylate is a highly selective BRAF kinase inhibitor that primarily inhibits the kinase activity of mutant BRAF V600 by competitively binding to the ATP-binding site of the BRAF protein, thereby blocking the abnormal activation of the downstream MAPK signaling pathway.

Mechanism of Action

Dabrafenib mesylate is a potent and selective ATP-competitive RAF kinase inhibitor. It targets mutant B-Raf (BRAF V600E) with an IC50 of 0.8 nM, while also inhibiting wild-type B-Raf (IC50 3.2 nM) and c-Raf (IC50 5.0 nM) . By blocking the mutant BRAF protein, it inhibits the MAPK signaling pathway (RAS/RAF/MEK/ERK), which mediates uncontrolled cancer cell growth and survival . The drug is only effective in patients with BRAF V600 mutations and is not indicated for wild-type BRAF tumors due to the risk of tumor promotion .

Applications

Treatment of unresectable or metastatic melanoma with BRAF V600E mutation

Adjuvant treatment of BRAF V600 mutation-positive melanoma following lymph node resection

BRAF V600 mutation-positive metastatic non-small cell lung cancer (NSCLC)

Anaplastic thyroid cancer with BRAF V600 mutation

Always used in combination with trametinib (MEK inhibitor) for enhanced efficacy

Routes of Administration

Oral: capsules or tablets for suspension, 150 mg twice daily (total 300 mg/day)

Administered with trametinib until disease progression or unacceptable toxicity

Take at least 1 hour before or 2 hours after meals, approximately 12 hours apart

If a dose is missed and next dose is <6 hours away, skip the missed dose

Safety & Side Effects

Common adverse reactions ( ≥ 20%): hyperkeratosis, headache, pyrexia (fever), arthralgia (joint pain), papilloma, alopecia (hair loss), and palmar-plantar erythrodysesthesia syndrome (hand-foot syndrome) . When combined with trametinib, additional adverse events may occur, requiring ongoing safety monitoring . Contraindicated in wild-type BRAF melanoma due to potential tumor promotion .

Pharmacokinetics

Absorption: Median Tmax 2 hours; mean absolute oral bioavailability 95%

Distribution: 99.7% bound to human plasma proteins

Metabolism: Hepatic, primarily via CYP2C8 and CYP3A4 to form hydroxy-dabrafenib, then further oxidized to carboxy-dabrafenib

   Elimination: 71% excreted in feces; 23% excreted in urine (as metabolites only)

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