A Game-Changer for Diabetes: Polymer Delivers Insulin Painlessly Through Skin
November 25, 2025
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Brand Name :
NexAVAR
(United States) [Available]Synonyms :
sorafenib
Class :
Antineoplastic agents and Tyrosinase Kinase Inhibitor; VEGF Inhibitor
Brand Name :
NexAVAR
(United States) [Available]Synonyms :
sorafenib
Class :
Antineoplastic agents and Tyrosinase Kinase Inhibitor; VEGF Inhibitor
Dosage forms & StrengthsÂ
TabletÂ
200mgÂ
400
mg
Tablet
Oral
every 12 hrs
In case of toxicity of the skin, reduce or discontinue the dose
400
mg
Tablet
Oral
every 12 hrs
In case of toxicity of the skin, reduce or discontinue the dose
sorafenib is indicated to treat metastatic or locally recurrent, differentiated, progressive thyroid cancer that shows refraction to radioactive iodine treatment
A dose of 400 mg orally is administered every 12 hours
In case of toxicity of the skin, reduce or discontinue the dose
Dose Adjustments
For differentiated thyroid cancer:
Dose reduction for dermatologic toxicities
1st dose reduction- reduce the dose to 600 mg/day
2nd dose reduction- 200 mg every 12 hours
3rd dose reduction- 200 mg per day
In the case of mild to moderate renal impairment, no dose adjustment is required
Dosing for severe renal impairment is not studied
In the case of mild to moderate hepatic impairment, no dose adjustment is required
Dosing for severe hepatic impairment is not studied
(Orphan)
Treatment of stage II B is through stage IV melanoma
(Orphan)
sorafenib is designated as orphan for the treatment of the above condition
The safety and efficacy of sorafenib are not seen in pediatric patientsÂ
Refer to the adult dosingÂ
the drug is contraindicated in patients who have severe hypersensitivity to sorafenib or any other excipient of the formulation sorafenib should be used in combination with paclitaxel and carboplatin in the patients suffering from squamous lung cancer
may have an increased hepatotoxic effect when combined with sorafenib
the drug is contraindicated in patients who have severe hypersensitivity to sorafenib or any other excipient of the formulation sorafenib should be used in combination with paclitaxel and carboplatin in the patients suffering from squamous lung cancer
dasatinib may enhance the QTc-prolonging effect of QT-prolonging
may enhance the Qtc prolonging effect
may increase the hepatotoxic effect
may have an increased QTc-prolonging effect when combined with QT-prolonging agents
may have an increased QTc-prolonging effect when combined with doxepin-containing products
may increase the QTc-prolonging effect of QT-prolonging Agents
may increase the hepatotoxic effect of acetaminophen
may increase the hepatotoxic effect when combined
dronedarone: they may increase the QTc-prolonging effect of QTc-prolonging miscellaneous agents
gilteritinib: they may increase the QTc-prolonging effect of QTc-prolonging agents
halofantrine: they may increase the QTc-prolonging effect of QTc-prolonging Agents
osimertinib: they may increase the QTc-prolonging effect of QTc-prolonging Agents
pentamidine: they may increase the QTc-prolonging effect of QTc-prolonging Agents
may enhance the QTc-prolonging effect of each other when combined
may enhance the QTc-prolonging effect of each other when combined
chloroquine: they may increase the QTc-prolonging effect of QTc-prolonging Agents
dasatinib: they may increase the QTc-prolonging effect of QTc-prolonging Agents
methadone: they may increase the QTc-prolonging effect of QTc-prolonging Agents
QTc prolonging effect of azithromycin is increased with QT-prolonging class III Antiarrhythmics
carbinoxamine: it may increase the risk of QTc prolongation agents
capsaicin: it may increase the risk of QTc prolongation agents
benzydamine: it may increase the risk of QTc prolongation agents
rosoxacin: it may increase the risk of QTc prolongation agents
it increases the effect of myelosuppression in myelosuppressive agents
they decrease the concentration of sorafenib in serum
it increases the toxic/adverse effects of myelosuppressive agents
it decreases the concentration of sorafenib in serum
sorafenib increases the toxic/adverse effects of paclitaxel
UGT1A1 inhibitors increase the concentration of active metabolites of sacituzumab govitecan in serum
QTc interval is increased both by lenvatinib and sorafenib
CYP3A strong enhancers of the small intestine may reduce the bioavailability of sorafenib
when used together, entrectinib and sorafenib both increase the QTc interval
when used together, encorafenib and sorafenib both increase the QTc interval
may have an increased QTc-prolonging effect when combined with levoketoconazole
may have an increased QTc-prolonging effect when combined with nilotinib
May increase the QTc-prolonging effect of QT-prolonging Agents
may increase the QTc-prolonging effect of QT-prolonging Agents
may have an increased QTc-prolonging effect when combined with QT-prolonging agents
pazopanib: they may increase the QTc-prolonging effect of QTc-prolonging Agents
quetiapine: they may increase the QTc-prolonging effect of QTc-prolonging Agents
ribociclib: they may increase the QTc-prolonging effect of QTc-prolonging Agents
may increase the QTc-prolonging effect of each other when combined
may increase the QTc-prolonging effect of each other when combined
may increase the QTc-prolonging effect of each other when combined
may increase the QTc-prolonging effect of each other when combined
may increase the QTc-prolonging effect of each other when combined
the QTc-prolonging effect of clarithromycin can be increased with QT-prolonging agents
amoxicillin: it may increase the risk of QTc prolongation agents
anagrelide: it may increase the risk of QTc prolongation agents
antipyrine: it may increase the risk of QTc prolongation agents
bendamustine: it may increase the risk of QTc prolongation agents
hypertensive agents may increase the hypertensive effect of androgens
it increases the toxic/adverse effect of myelosuppressive drugs
myelosuppressive agents increase the toxic/adverse effect of clozapine
it decreases the concentration of CYP3A4 substrates in serum
myelosuppressive agents increase the effect of myelosuppression of olaparib
it increases the effect of myelosuppression in myelosuppressive agents
it increases the effect of hypertension in hypertension-associated agents
sorafenib increases the effect of anticoagulation in warfarin
QT-prolonging Miscellaneous Agents may enhance the QTc-prolonging effect of anti-arrhythmics
QT-prolonging Miscellaneous Agents may enhance the QTc-prolonging effect of anti-arrhythmics
QT-prolonging Miscellaneous Agents may enhance the QTc-prolonging effect of anti-arrhythmics
QT-prolonging Miscellaneous Agents may enhance the QTc-prolonging effect of anti-arrhythmics
QT-prolonging Miscellaneous Agents may enhance the QTc-prolonging effect of anti-arrhythmics
they increase the toxicity of bisphosphonate derivatives
they increase the toxicity of bisphosphonate derivatives
they increase the toxicity of bisphosphonate derivatives
they increase the toxicity of bisphosphonate derivatives
they increase the risk of other QT prolongers
they increase the risk of other QT prolongers
they increase the risk of other QT prolongers
they increase the risk of other QT prolongers
they increase the risk of other QT prolongers
sorafenib: they may diminish the serum concentration of CYP3A4 Inducers
sorafenib: they may diminish the serum concentration of CYP3A4 Inducers
sorafenib: they may diminish the serum concentration of CYP3A4 Inducers
sorafenib: they may diminish the serum concentration of CYP3A4 Inducers
sorafenib: they may diminish the serum concentration of CYP3A4 Inducers
interaction increases the serum concentration of docetaxel
angiogenesis Inhibitors may enhance the adverse/toxic effect of bisphosphonate derivatives
angiogenesis Inhibitors may enhance the adverse/toxic effect of bisphosphonate derivatives
angiogenesis Inhibitors may enhance the adverse/toxic effect of bisphosphonate derivatives
angiogenesis Inhibitors may enhance the adverse/toxic effect of bisphosphonate derivatives
QT-prolongers increase the effect of QTc prolongation of haloperidol
they increase the risk of other QT prolongers
they increase the risk of other QT prolongers
they increase the risk of other QT prolongers
they increase the risk of other QT prolongers
they increase the risk of other QT prolongers
may increase the QTc prolonging effect of QT-prolonging agents
may increase the QTc-prolonging effect
may increase the QTc-prolonging effect
may increase the QTc-prolonging effect
may increase the QTc-prolonging effect
may increase the QTc-prolonging effect
may increase the QTc-prolonging effect
may increase the QTc-prolonging effect
may increase the QTc-prolonging effect
may increase the QTc-prolonging effect
may increase the QTc-prolonging effect
may increase the QTc-prolonging effect
may increase the QTc-prolonging effect
may increase the QTc-prolonging effect
may increase the QTc-prolonging effect
may increase the QTc-prolonging effect
may have an increased QTc-prolonging effect when combined with QT-prolonging agents
certoparin: it may increase the risk or severity of QTc prolongation
benoxaprofen: it may increase the risk or severity of QTc prolongation agents
cabozantinib: it may increase the risk or severity of QTc prolongation agents
it may enhance the QTc-prolonging effect
it may enhance the QTc-prolonging effect
it may enhance the QTc-prolonging effect
it may enhance the QTc-prolonging effect
it may enhance the QTc-prolonging effect
it alters the QTc interval and increases the toxicity of sorafenib
sorafenib increases the efficacy of cocaine by altering the hepatic CYP2B6 enzyme metabolism
it increases the efficacy of sorafenib by altering the hepatic CYP3A4 enzyme metabolism
it increases the efficacy of sorafenib by altering the hepatic CYP3A4 enzyme metabolism
Actions and Spectrum:Â
Actions:Â
Spectrum:Â
sorafenib is approved for the treatment of several types of cancer, including:Â
Frequency defined:Â
>10%Â
Thrombocytopenia Â
AnemiaÂ
Diarrhea Â
Rash/desquamation Â
Fatigue Â
Abdominal pain Â
Hand-foot skin reaction Â
Weight loss Â
Anorexia Â
Alopecia Â
Nausea Â
Lymphopenia Â
Neutropenia Â
Hemorrhage Â
Hypertension Â
Vomiting Â
Constipation Â
NeuropathyÂ
Dry skin Â
1-10%Â
Headache Â
Joint pain Â
Congestive heart failureÂ
QT prolongation Â
<1%Â
Acute renal failureÂ
AngioedemaÂ
Bone painÂ
Contraindication/Caution:Â
Contraindications:Â
Cautions:Â
Pregnancy consideration: The drug is toxic and unsafe for pregnant women and the developing fetus. Â
Breastfeeding warnings: No data on the excretion of sorafenib in breast milk is available. Because of possible serious effects, women are advised to breastfeed two weeks after the last dose of sorafenib.Â
Pregnancy category:Â
Pharmacology:Â
sorafenib is a small molecule kinase inhibitor that is used in the treatment of cancer. It was first approved by the US Food and Drug Administration (FDA) in 2005 for the treatment of advanced renal cell carcinoma and later for other types of cancer, such as hepatocellular carcinoma and thyroid cancer.Â
sorafenib inhibits multiple tyrosine kinase receptors, including vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, VEGFR-3), platelet-derived growth factor receptor (PDGFR-β), c-KIT, and the RAF kinases (RAF-1, B-RAF). By inhibiting these kinases, sorafenib can inhibit tumor angiogenesis, cell proliferation, and survival, and induce apoptosis in cancer cells.Â
sorafenib is primarily metabolized in the liver, with the primary metabolite being sorafenib N-oxide. The drug has a half-life of approximately 25-48 hours and is excreted primarily through the feces.Â
Pharmacodynamics:Â
sorafenib is a multi-targeted tyrosine kinase inhibitor that can bind to the ATP-binding site of multiple receptors, including vascular endothelial growth factor receptors (VEGFRs), platelet-derived growth factor receptor beta (PDGFR-β), fibroblast growth factor receptor (FGFR), rearranged during transfection (RET), c-KIT, and the RAF kinases (RAF-1, B-RAF). Â
By inhibiting the activity of these kinases, sorafenib can block the downstream signaling pathways involved in tumor angiogenesis, cell proliferation, and survival. Specifically, sorafenib inhibits the activation of RAF-MEK-ERK and VEGFR signaling pathways. Inhibition of RAF-MEK-ERK pathway leads to inhibition of tumor cell proliferation and induction of apoptosis, while inhibition of VEGFR signaling pathway leads to inhibition of tumor angiogenesis and reduction of blood supply to the tumor. Â
sorafenib can also modulate the immune system by increasing the activation of natural killer (NK) cells and T-cells, which in turn can enhance anti-tumor immune response. The pharmacodynamics of sorafenib is characterized by a dose-dependent effect on the inhibition of the target kinases. Studies have shown that sorafenib at clinically relevant doses can inhibit the phosphorylation of VEGFRs, PDGFR-β, and RAF kinases in tumor tissues. Â
In conclusion, sorafenib exerts its pharmacodynamic effect through multi-targeted inhibition of key kinases involved in tumor angiogenesis, cell proliferation, and survival, as well as modulation of the immune system. This makes it an effective drug in the treatment of various types of cancer.Â
Pharmacokinetics:Â
AbsorptionÂ
The bioavailability is 38-49% which is reduced by high fat dietÂ
The peak plasma concentration is achieved in 3 hoursÂ
DistributionÂ
The protein bound is 99.5%Â
MetabolismÂ
The drug is metabolised in liver by UGT1A9 & CYP3A4Â Â
Elimination and ExcretionÂ
The half-life of the drug is 25-48 hoursÂ
The drug is excreted 77%; in feces and 19% in urineÂ
Administration:Â
sorafenib is an orally administered medication and is typically taken twice daily on an empty stomach, at least one hour before or two hours after a meal. The tablets should be swallowed whole with water and should not be crushed, chewed, or broken. The recommended starting dose of sorafenib may vary depending on the type of cancer being treated, the patient’s body weight, and overall health status.
Typically, the starting dose for advanced renal cell carcinoma is 400 mg twice daily, and for hepatocellular carcinoma, it is 400 mg twice daily. The dosage may be adjusted based on the patient’s individual response to the medication and any adverse effects that may occur. However, the maximum recommended daily dose of sorafenib is 800 mg.Â
sorafenib is usually taken continuously until disease progression or intolerable adverse effects occur. Treatment interruptions or dose adjustments may be necessary based on the patient’s overall health status, laboratory values, or adverse effects experienced during treatment.Â
Patient information leafletÂ
Generic Name: sorafenib (Rx)Â
Pronounced: Soe-RAF-e-nibÂ
Why do we use sorafenib?Â
sorafenib is a medication that is used to treat certain types of cancers, such as liver cancer, renal cell carcinoma, and thyroid cancer. It works by inhibiting the growth of cancer cells and the blood vessels that supply them with nutrients.Â
sorafenib is a type of targeted therapy that specifically targets the signaling pathways within cancer cells that contribute to their growth and survival. By blocking these pathways, sorafenib can slow down or even stop the growth of cancer cells.Â
sorafenib is typically used in patients with advanced or metastatic cancers, where the cancer has spread beyond its original site. It may be used alone or in combination with other treatments, such as chemotherapy or radiation therapy, depending on the type and stage of the cancer.Â
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