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TEVA-SUNITINIB is a brand name for Sunitinib, supplied as a capsule. The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: AND CLINICAL USE ..............................................................................3 CONTRAINDICATIONS ...................................................................................................4 WARNINGS AND PRECAUTIONS…
Verbatim from this product's HC label. Tap a section to expand.
Recommended Dose for GIST and MRCC The recommended dose of Teva-Sunitinib (sunitinib malate) is one 50 mg oral dose taken once daily, on a schedule of 4 weeks on treatment followed by 2 weeks off. 5 mg taken orally once daily without a scheduled off-treatment period.
Teva-Sunitinib may be taken with or without food. Dose Modification Daily doses should not exceed 50 mg nor be decreased below 25 mg. 5 mg is recommended based on individual safety and tolerability.
CYP3A4 Inhibitors:
Concurrent administration of sunitinib malate with the CYP3A4 inhibitor, ketoconazole, resulted in 49% and 51% increases in combined (sunitinib + active metabolite) Cmax and AUC0-∞ values, respectively, after a single dose of sunitinib malate in healthy volunteers.
Doses of Teva-Sunitinib may need to be reduced to a minimum of 25 mg daily, and clinical response and tolerability should be carefully monitored, in patients receiving a potent CYP3A4 inhibitor such as ketoconazole (see DRUG INTERACTIONS and ACTION AND CLINICAL PHARMACOLOGY).
Selection of an alternate concomitant medication with no or minimal enzyme inhibition potential should be considered.
NOTE:
This recommendation is based on pharmacokinetic data from healthy volunteers. In clinical trials conducted to date, the safety and efficacy of sunitinib with concomitant use of CYP3A4 inhibitors has not been established. In the 2 cytokine-refractory MRCC studies, 14 of the 169 patients used a potent CYP 3A4 inhibitor concomitantly with sunitinib with no modification of the starting dose of sunitinib.
CYP3A4 Inducers:
Concurrent administration of sunitinib malate with the potent CYP3A4 inducer, rifampin, resulted in a more than 23% and 46% reduction in combined (sunitinib + active metabolite) Cmax and AUC0-∞ values, respectively, after a single dose of sunitinib in healthy volunteers.
The dose of Teva-Sunitinib may need to be increased (maximum 50 mg), and clinical response and tolerability should be carefully monitored, in patients receiving Teva- Sunitinib with a potent CYP3A4 inducer, such as rifampin (see DRUG INTERACTIONS and ACTION AND CLINICAL PHARMACOLOGY).
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
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Selection of an alternate concomitant medication with no or minimal enzyme induction potential should be considered.
NOTE:
This recommendation is based on pharmacokinetic data from healthy volunteers. In clinical trials conducted to date, the safety and efficacy of sunitinib with concomitant use of CYP3A4 inducers has not been established. In the two cytokine-refractory MRCC studies, 33 of the 169 patients received a potent CYP3A4 inducer concomitantly with sunitinib with no modification of the starting dose of sunitinib.
Teva-Sunitinib Capsules Page 35 of 73 Special Populations:
No dose adjustment is required on the basis of patient age, body weight, creatinine clearance, race, gender or ECOG score (see ACTION AND CLINICAL PHARMACOLOGY, Special Populations). OVERDOSAGE Treatment of overdose with Teva-Sunitinib should consist of general supportive measures.
There is no specific antidote for overdose with Teva-Sunitinib. If indicated, elimination of unabsorbed drug should be achieved by emesis or gastric lavage. Cases of accidental overdose have been reported; some cases were associated with adverse reactions consistent with the known safety profile of sunitinib.
A case of intentional overdose involving the ingestion of 1,500 mg of sunitinib in an attempted suicide was reported without adverse reaction. For management of a suspected drug overdose, contact your regional Poison Control Centre.
ACTION AND CLINICAL PHARMACOLOGY Sunitinib malate is a small molecule that inhibits multiple receptor tyrosine kinases (RTKs), some of which are implicated in tumour growth, pathologic angiogenesis, and metastatic progression of cancer.
Sunitinib was evaluated for its inhibitory activity against a variety of kinases (> 80 kinases) and was identified as a potent inhibitor of platelet-derived growth factor receptors (PDGFRα and PDGFRβ), vascular endothelial growth factor receptors (VEGFR1, VEGFR2 and VEGFR3), stem cell factor receptor (KIT), Fms-like tyrosine kinase-3 (FLT3), colony stimulating factor receptor (CSF-1R), and the glial cell-line derived neurotrophic factor receptor (RET).
Inhibition of the activity of these RTKs by sunitinib has been demonstrated in biochemical and/or cellular assays, and inhibition of function has been demonstrated in cell proliferation or viability assays. The primary metabolite exhibits similar potency compared to sunitinib in biochemical and cellular assays (see DETAILED PHARMACOLOGY).
Sunitinib inhibited the phosphorylation of multiple RTKs (PDGFRβ, VEGFR2, KIT) in tumour xenografts expressing RTK targets in vivo and demonstrated inhibition of tumour growth or tumour regression and/or inhibited metastases in some experimental models of cancer.
Sunitinib demonstrated the ability to inhibit growth of tumour cells expressing dysregulated target RTKs (PDGFR, RET, or KIT) in vitro and to inhibit PDGFRβ- and VEGFR2-dependent tumour angiogenesis in vivo. Pharmacokinetics The pharmacokinetics of sunitinib and its primary active metabolite have been evaluated in 135 healthy volunteers and in 266 patients with solid tumours.
Absorption and Distribution Teva-Sunitinib Capsules Page 36 of 73 Maximum plasma concentrations (Cmax) of sunitinib are generally observed from 6 to 12 hours (Tmax) post-dose. Food has no effect on the bioavailability of sunitinib. Following administration of a single oral dose in healthy volunteers, the terminal half-lives of sunitinib and its primary active metabolite are approximately 40 to 60 hours and 80 to 110 hours, respectively.
After repeated daily administration, in the dosing ranges of 25 to 100 mg, the area under the plasma concentration-time curve (AUC) and Cmax for sunitinib and total drug […]