Dabrafenib

Dabrafenib is a selective oral inhibitor of the BRAF kinase, with particular activity against the BRAF V600-mutant forms. By blocking aberrant BRAF signaling in the MAPK pathway, it can slow or halt the proliferation of tumor cells that rely on this mutation.

Indications and use: Dabrafenib is approved for unresectable or metastatic melanoma harboring BRAF V600E or V600K mutations. It is commonly given in combination with trametinib, a MEK inhibitor, because together they improve efficacy and reduce certain skin cancers associated with BRAF inhibitors. The dabrafenib–trametinib combination is also approved for other BRAF V600 mutation–positive cancers in select settings, notably non-small cell lung cancer, among others.

Dosing: For melanoma, dabrafenib is typically prescribed at 150 mg taken orally twice daily. When used in combination therapy, the regimen is dabrafenib 150 mg twice daily plus trametinib 2 mg once daily, with dose adjustments for adverse effects as needed.

Adverse effects and safety: Common side effects include fever (pyrexia), fatigue, nausea, and rash. The risk of new skin cancers such as cutaneous squamous cell carcinoma is present with BRAF inhibitors, but is reduced with combination therapy. Other potential effects include edema, elevated liver enzymes, photosensitivity, and ocular events. Regular monitoring for skin lesions, liver function, and cardiovascular status is often recommended.

Special considerations: Dabrafenib is metabolized in the liver and can interact with strong CYP3A4 inhibitors or inducers. It should be used in pregnancy only if clearly needed, with appropriate contraception. As with all anticancer therapies, treatment should be individualized and managed by a healthcare professional, with careful assessment of risks and benefits.