Composition
Axinix 1 Tablet
Each film coated tablet contains Axitinib INN 1 mg.
Axinix 5 Tablet
Each film coated tablet contains Axitinib INN 5 mg.
06 — For prescribers
Prescribinginformation
A structured summary of the package insert. Download the PDF for the complete text.
Clinical pharmacology
Mechanism of action
Axitinib has been shown to inhibit receptor tyrosine kinases including vascular endothelial growth factor receptors (VEGFR)-1, VEGFR-2 and VEGFR-3 at therapeutic plasma concentrations. These receptors are implicated in pathologic angiogenesis, tumor growth and cancer progression.
VEGF-mediated endothelial cell proliferation and survival were inhibited by Axitinib in vitro and in mouse models. Axitinib was shown to inhibit tumor growth and phosphorylation of VEGFR-2 in tumor xenograft mouse models.
Indication
Axitinib is indicated for the treatment of advanced Renal Cell Carcinoma (RCC) after failure of one prior systemic therapy.
Dosage & administration
Recommended dosing
The recommended starting oral dose of Axitinib is 5 mg twice daily. Administer Axitinib doses approximately 12 hours apart with or without food. Axitinib should be swallowed whole with a glass of water.
If the patient vomits or misses a dose, an additional dose should not be taken. The next prescribed dose should be taken at the usual time.
Contraindications
NoneAdverse reactions
The most common (≥20%) adverse reactions are:
DiarrheaHypertensionFatigueDecreased appetiteNauseaDysphoniaPalmar-plantar erythrodysesthesia (hand-foot) syndromeWeight decreasedVomitingAstheniaConstipation
Drug interactions
In vitro data indicate that Axitinib is metabolized primarily by CYP3A4/5 and, to a lesser extent, CYP1A2, CYP2C19 and uridine diphosphate-glucuronosyltransferase (UGT) 1A1.
CYP3A4/5 inhibitors
Exposure ↑Co-administration of ketoconazole, a strong inhibitor of CYP3A4/5, increased the plasma exposure of Axitinib in healthy volunteers. Co-administration with strong CYP3A4/5 inhibitors should be avoided. Grapefruit or grapefruit juice may also increase Axitinib plasma concentrations and should be avoided.
Select concomitant medication with no or minimal CYP3A4/5 inhibition potential. If a strong CYP3A4/5 inhibitor must be co-administered, the Axitinib dose should be reduced.
CYP3A4/5 inducers
Exposure ↓Co-administration of rifampin, a strong inducer of CYP3A4/5, reduced the plasma exposure of Axitinib in healthy volunteers. Avoid strong CYP3A4/5 inducers; select concomitant medication with no or minimal induction potential.
Strong inducers — avoid
RifampinDexamethasonePhenytoinCarbamazepineRifabutinRifapentinePhenobarbitalSt. John’s wort
Moderate inducers — avoid if possible
BosentanEfavirenzEtravirineModafinilNafcillin
Curves are schematic, showing direction of change only.
Pharmaceutical information
Storage
Store in a cool and dry place, away from light. Keep out of the reach of children.
Axinix 1 Tablet
Each commercial box contains 180 tablets in a bottle.
Axinix 5 Tablet
Each commercial box contains 60 tablets in a bottle.
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