Sorafenib
Generic Name: sorafenib
Brand Names:
Sorafenib
11 DESCRIPTION Sorafenib, a kinase inhibitor, is the tosylate salt of sorafenib. Sorafenib tosylate has the chemical name 4-(4-{3-[4-Chloro-3-(trifluoromethyl)phenyl]ureido}phenoxy)- N 2 -methylpyridine-2 carboxamide mono(4-methylbenzenesulfonate). The molecular formula of sorafenib tosylate is C 21 H 16 ClF 3 N 4 O 3 x C 7 H 8 O 3 S and the molecular weight of sorafenib tosylate is 637.03 g/mole.
Overview
11 DESCRIPTION Sorafenib, a kinase inhibitor, is the tosylate salt of sorafenib. Sorafenib tosylate has the chemical name 4-(4-{3-[4-Chloro-3-(trifluoromethyl)phenyl]ureido}phenoxy)- N 2 -methylpyridine-2 carboxamide mono(4-methylbenzenesulfonate). The molecular formula of sorafenib tosylate is C 21 H 16 ClF 3 N 4 O 3 x C 7 H 8 O 3 S and the molecular weight of sorafenib tosylate is 637.03 g/mole.
Uses
1 INDICATIONS AND USAGE Sorafenib tablets are a kinase inhibitor indicated for the treatment of • Unresectable hepatocellular carcinoma ( 1.1 ) • Advanced renal cell carcinoma ( 1.2 ) • Locally recurrent or metastatic, progressive, differentiated thyroid carcinoma (DTC) refractory to radioactive iodine treatment ( 1.3 ) 1.1 Hepatocellular Carcinoma Sorafenib tablets are indicated for the treatment of patients with unresectable hepatocellular carcinoma (HCC). 1.2 Renal Cell Carcinoma Sorafenib tablets are indicated for the treatment of patients with advanced renal cell carcinoma (RCC).
Dosage
2 DOSAGE AND ADMINISTRATION The recommended dosage is 400 mg orally twice daily without food. ( 2.1 ) 2.1 Recommended Dosage The recommended dosage of sorafenib tablets are 400 mg orally twice daily without food (at least 1 hour before or 2 hours after a meal) until the patient is no longer clinically benefiting from therapy or until unacceptable toxicity. 2.2 Dosage Modifications for Adverse Reactions Recommended Dosage Modifications The recommended dosage modifications for adverse reactions are provided in Tables 1, 2, and 3.
Side Effects
6 ADVERSE REACTIONS The following clinically significant adverse reactions are discussed elsewhere in the labeling: • Cardiovascular events [see Warnings and Precautions ( 5.1 )] • Hemorrhage [see Warnings and Precautions ( 5.2 )] • Hypertension [see Warnings and Precautions ( 5.3 )] • Dermatologic toxicities [see Warnings and Precautions ( 5.4 )] • Gastrointestinal perforation [see Warnings and Precautions ( 5.5 )] • QT interval prolongation [see Warnings and Precautions ( 5.9 ) and Clinical Pharmacology ( 12.2 )] • Drug-induced liver injury [see Warnings and Precautions ( 5.10 )] • Impairment of TSH suppression in DTC [see Warnings and Precautions ( 5.12 )] The most common adverse reactions (≥20%) are diarrhea, fatigue, infection, alopecia, hand-foot skin reaction, rash, weight loss, dec...
Interactions
7 DRUG INTERACTIONS Strong CYP3A Inducers: Avoid strong CYP3A4 inducers. ( 7.1 ) 7.1 Effect of Other Drugs on Sorafenib Strong CYP3A4 Inducers The concomitant use of sorafenib with rifampin, a strong CYP3A4 inducer decreased the mean AUC of sorafenib, which may decrease the antitumor activity [see Clinical Pharmacology ( 12.3 )] . Avoid concomitant use of sorafenib with strong CYP3A4 inducers, when possible, because these drugs can decrease the systemic exposure to sorafenib. Neomycin The concomitant use of sorafenib with neomycin decreased the mean AUC of sorafenib, which may decrease the antitumor activity. Avoid concomitant use of sorafenib with neomycin. The effects of other antibiotics on the pharmacokinetics of sorafenib have not been studied [see Clinical Pharmacology ( 12.3 )].
Warnings
5 WARNINGS AND PRECAUTIONS • Cardiovascular Events : Consider temporary or permanent discontinuation of sorafenib tablets. ( 2.2 , 5.1 ) • Hemorrhage: Discontinue sorafenib tablets if needed. ( 5.2 ) • Hypertension: Monitor blood pressure weekly during the first 6 weeks and periodically thereafter. Consider temporary or permanent discontinuation for severe or persistent hypertension despite antihypertensive therapy. ( 5.3 ) • Dermatologic Toxicities : Interrupt and/or decrease dose. Discontinue for severe or persistent reactions, or if Stevens-Johnson syndrome and toxic epidermal necrolysis is suspected. ( 5.4 ) • Gastrointestinal Perforation : Discontinue sorafenib tablets. 4 CONTRAINDICATIONS •Sorafenib tablets are contraindicated in patients with known severe hypersensitivity to sorafenib or any other component of sorafenib tablets. •Sorafenib tablets in combination with carboplatin and paclitaxel is contraindicated in patients with squamous cell lung cancer [see Warnings and Precautions ( 5.8 )] .
Pregnancy
8.1 Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action [see Clinical Pharmacology ( 12.1 )] , sorafenib may cause fetal harm when administered to a pregnant woman. There are no available data in pregnant women to inform a drug-associated risk. In animal reproduction studies, oral administration of sorafenib to pregnant rats and rabbits during the period of organogenesis resulted in embryo-fetal toxicities at maternal exposures that were significantly lower than human exposures at the recommended dose of 400 mg twice daily (see Data).
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING Sorafenib Tablets are supplied as 200 mg, round biconvex, red film-coated tablets, debossed with "F11" on one side and plain on the other side.
Frequently Asked Questions
What is Sorafenib used for?▼
1 INDICATIONS AND USAGE Sorafenib tablets are a kinase inhibitor indicated for the treatment of • Unresectable hepatocellular carcinoma ( 1.1 ) • Advanced renal cell carcinoma ( 1.2 ) • Locally recurrent or metastatic, progressive, differentiated thyroid carcinoma (DTC) refractory to radioactive iodine treatment ( 1.3 ) 1.1 Hepatocellular Carcinoma Sorafenib tablets are indicated for the treatment of patients with unresectable hepatocellular carcinoma (HCC). 1.2 Renal Cell Carcinoma Sorafenib tablets are indicated for the treatment of patients with advanced renal cell carcinoma (RCC).
What are the side effects of Sorafenib?▼
6 ADVERSE REACTIONS The following clinically significant adverse reactions are discussed elsewhere in the labeling: • Cardiovascular events [see Warnings and Precautions ( 5.1 )] • Hemorrhage [see Warnings and Precautions ( 5.2 )] • Hypertension [see Warnings and Precautions ( 5.3 )] • Dermatologic toxicities [see Warnings and Precautions ( 5.4 )] • Gastrointestinal perforation [see Warnings and Precautions ( 5.5 )] • QT interval prolongation [see Warnings and Precautions ( 5.9 ) and Clinical Pharmacology ( 12.2 )] • Drug-induced liver injury [see Warnings and Precautions ( 5.10 )] • Impairment of TSH suppression in DTC [see Warnings and Precautions ( 5.12 )] The most common adverse reactions (≥20%) are diarrhea, fatigue, infection, alopecia, hand-foot skin reaction, rash, weight loss, dec...
Can I take Sorafenib during pregnancy?▼
8.1 Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action [see Clinical Pharmacology ( 12.1 )] , sorafenib may cause fetal harm when administered to a pregnant woman. There are no available data in pregnant women to inform a drug-associated risk. In animal reproduction studies, oral administration of sorafenib to pregnant rats and rabbits during the period of organogenesis resulted in embryo-fetal toxicities at maternal exposures that were significantly lower than human exposures at the recommended dose of 400 mg twice daily (see Data).
What are the important warnings for Sorafenib?▼
5 WARNINGS AND PRECAUTIONS • Cardiovascular Events : Consider temporary or permanent discontinuation of sorafenib tablets. ( 2.2 , 5.1 ) • Hemorrhage: Discontinue sorafenib tablets if needed. ( 5.2 ) • Hypertension: Monitor blood pressure weekly during the first 6 weeks and periodically thereafter. Consider temporary or permanent discontinuation for severe or persistent hypertension despite antihypertensive therapy. ( 5.3 ) • Dermatologic Toxicities : Interrupt and/or decrease dose. Discontinue for severe or persistent reactions, or if Stevens-Johnson syndrome and toxic epidermal necrolysis is suspected. ( 5.4 ) • Gastrointestinal Perforation : Discontinue sorafenib tablets. 4 CONTRAINDICATIONS •Sorafenib tablets are contraindicated in patients with known severe hypersensitivity to sorafenib or any other component of sorafenib tablets. •Sorafenib tablets in combination with carboplatin and paclitaxel is contraindicated in patients with squamous cell lung cancer [see Warnings and Precautions ( 5.8 )] .
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.