Drug information of Sorafenib
Mechanism of effect
Sorafenib interacts with multiple intracellular (CRAF, BRAF and mutant BRAF) (and cell surface kinases (KIT, FLT-3, VEGFR-2, VEGFR-3, and PDGFR-ß)
Decreases tumor cell proliferation in vitro
Bioavailability is 38% to 49%. T max is 3 h. Steady state plasma levels occur within 7 days. Administration with high-fat meals reduced sorafenib bioavailability 29%. In vitro protein binding is 99.5%. Metabolism occurs primarily in the liver by CYP3A4 and UGT1A9-mediated glucuronidation. Eight metabolites have been identified, of which pyridine N-oxide has shown in vitro potency similar to the parent drug. Mean elimination t ½ is about 25 to 48 h. After oral administration of a sorafenib 100 mg oral solution, 96% was recovered within 14 days (77% in the feces and 19% in the urine)
Adults PO 400 mg (two 200 mg tablets) twice daily. Continue treatment until patient is no longer clinically benefiting from therapy or until unacceptable toxicity occurs
Drug contraindicationshypersensitivity to drug or its components.
Side effectsnausea , Headache , Dermatit , constipation , abdominal pain , decreased appetite , vomiting , fatigue , Hepatic dysfunction , rash , flushing , Depression , Diarrhea , Dyspnea , asthenia , pruritus , Hypertension , thrombocytopenia , neutropenia , lymphopenia , leukopenia , anemia , Erythema , neuropathy , acne , dyspepsia , fever , impotence , weight decrease , myalgia , Flu-like symptoms , Alopecia , anorexia , Arthralgia , Pain , Hand-and-Foot Syndrome , stomatitis , dysphagia , dry skin , elevated INR
InteractionsBevacizumab , Trastuzumab , Deferasirox , Bupropion , Docetaxel , Doxorubicin , Phenobarbital , Phenytoin , Warfarin , Clozapine , Carbamazepine , Carboplatin , Rifabutin , Toremifene , Dolasetron , vandetanib , sparfloxacin , Dofetilide , Inotuzumab , Butalbital and Acetaminophen , Dabrafenib , Halofantrine , Grepafloxacin , Entrectinib , Bepridil , bedaquiline , Gemtuzumab , Remdesivir , Artesunate , Fidaxomicin
1-Monitor BP weekly during first 6 wk of therapy and monitor and treat thereafter if necessary
2-Caution women of childbearing potential to avoid becoming pregnant while using sorafenib and for 2 wk after stopping therapy
Points of recommendation
• Administer each dose with a full glass of water on an empty stomach, at least 1 h before or 2 h after eating.
• Caution patient not to chew, crush, or break tablets.
• If a dose is missed, skip that dose and administer the next dose at the regularly scheduled time. Never administer 2 doses at the same time to catch up.
• Advise patient to notify health care provider if rash; persistent diarrhea; persistent nausea and/or vomiting; weakness; mouth sores; or numbness, tingling, or pain in hands or feet develops
• Instruct patient to immediately notify health care provider if any of the following occur:
chest pain, chest pressure, or unexplained shortness of breath on exertion or with activity; redness, pain, swelling, or blistering of palms of hands or soles of feet; unexplained bleeding