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Vemurafenib

Kinase InhibitorProtein Kinase InhibitorsCytochrome P450 1A2 Inhibitors

Route: Oral

8 interactions on record

Vemurafenib has 8 known drug interactions based on U.S. FDA drug labeling data. 6 are classified as major interactions requiring close medical supervision. Notable interactions include combinations with Carbamazepine, Digoxin, Ipilimumab. Patients taking Vemurafenib should inform their healthcare provider of all current medications — including over-the-counter drugs and supplements — to avoid potentially harmful combinations. Data sourced from OpenFDA and the NIH National Library of Medicine.

Total: 8
Major: 6
Moderate: 2

Major (6)

Vemurafenib + Carbamazepine— Strong CYP3A4 inducer that decreases vemurafenib plasma concentrations and may result in decreased efficacy. Avoid coadm…
Vemurafenib + Digoxin— P-glycoprotein substrate with narrow therapeutic index. Vemurafenib increased digoxin systemic exposure by 1.8-fold. Avo…
Vemurafenib + Ipilimumab— Concurrent use increases transaminases and bilirubin in majority of patients. Increased hepatotoxicity risk.
Vemurafenib + Phenytoin— Strong CYP3A4 inducer that decreases vemurafenib plasma concentrations and may result in decreased efficacy. Avoid coadm…
Vemurafenib + Rifampin— Strong CYP3A4 inducer that decreases vemurafenib plasma concentrations and may result in decreased efficacy. Avoid coadm…
Vemurafenib + Tizanidine— CYP1A2 substrate with narrow therapeutic window. Vemurafenib increased tizanidine systemic exposure by 4.7-fold. Avoid c…

Moderate (2)

Vemurafenib + Nimodipine— Moderate and weak CYP3A4 inducers include, for example: amprenavir, aprepitant, armodafinil, bosentan, efavirnenz, etrav…
Vemurafenib + Riluzole— The concomitant use of strong or moderate CYP1A2 inhibitors (e.g., ciprofloxacin, enoxacin, fluvoxamine, methoxsalen, me…

Vemurafenib + Carbamazepine⚠️Major

Strong CYP3A4 inducer that decreases vemurafenib plasma concentrations and may result in decreased efficacy. Avoid coadministration; replace with alternative drugs when possible.

Vemurafenib + Digoxin⚠️Major

P-glycoprotein substrate with narrow therapeutic index. Vemurafenib increased digoxin systemic exposure by 1.8-fold. Avoid concurrent use or consider dose reduction.

Vemurafenib + Ipilimumab⚠️Major

Concurrent use increases transaminases and bilirubin in majority of patients. Increased hepatotoxicity risk.

Vemurafenib + Phenytoin⚠️Major

Strong CYP3A4 inducer that decreases vemurafenib plasma concentrations and may result in decreased efficacy. Avoid coadministration; replace with alternative drugs when possible.

Vemurafenib + Rifampin⚠️Major

Strong CYP3A4 inducer that decreases vemurafenib plasma concentrations and may result in decreased efficacy. Avoid coadministration; replace with alternative drugs when possible.

Vemurafenib + Tizanidine⚠️Major

CYP1A2 substrate with narrow therapeutic window. Vemurafenib increased tizanidine systemic exposure by 4.7-fold. Avoid concomitant use or monitor closely for toxicities and consider dose reduction.

Vemurafenib + Nimodipine🟡Moderate

Moderate and weak CYP3A4 inducers include, for example: amprenavir, aprepitant, armodafinil, bosentan, efavirnenz, etravirine, Echinacea, modafinil, nafcillin, pioglitazone, prednisone, rufinamide, and vemurafenib.

Vemurafenib + Riluzole🟡Moderate

The concomitant use of strong or moderate CYP1A2 inhibitors (e.g., ciprofloxacin, enoxacin, fluvoxamine, methoxsalen, mexiletine, oral contraceptives, thiabendazole, vemurafenib, zileuton) with TIGLUTIK may increase the risk of TIGLUTIK - associated adverse reactions [see Clinical Pharmacology (12.3) ].

Data sourced from U.S. FDA drug labeling via openFDA and the NIH National Library of Medicine. For informational purposes only. Always consult your pharmacist or physician.