“May all be happy, may all be healed, may all be at peace and may no one ever suffer."
Ponatinib is a kinase inhibitor. Ponatinib inhibited the in vitro tyrosine kinase activity of ABL and T315I mutant ABL with IC 50 concentrations of 0.4 nM and 2.0 nM, respectively. Ponatinib inhibited the in vitro activity of additional kinases with IC 50 concentrations between 0.1 nM and 20 nM, including members of the VEGFR, PDGFR, FGFR, EPH receptors and SRC families of kinases, and KIT, RET, TIE2, and FLT3. Ponatinib inhibited the in vitro viability of cells expressing native or mutant BCR-ABL, including T315I. In mice, treatment with ponatinib reduced the size of tumors expressing native or T315I mutant BCR-ABL when compared to controls.
Ponatinib is a kinase inhibitor indicated for the:
Recommended dose: 45 mg taken orally once daily with or without food
Hepatic Impairment: 30 mg orally once daily. Modify or interrupt dosing for hematologic and non-hematologic toxicity
None
The most common non-hematologic adverse reactions (≥20%) were, abdominal pain, rash, constipation, headache, dry skin, arterial occlusion, fatigue, hypertension, pyrexia, arthralgia, nausea, diarrhea, lipase increased, vomiting, myalgia and pain in extremity.
Use in Special Populations
Pediatric Use: Safety and effectiveness have not been established in pediatric patients.
Pregnancy & Lactation
Based on its mechanism of action and findings in animals, Ponatinib can cause fetal harm when administered to a pregnant woman. There are no available data on Ponatinib use in pregnant women. In animal reproduction studies, oral administration of ponatinib to pregnant rats during organogenesis caused adverse developmental effects at doses lower than human exposures at the recommended human dose. Advise pregnant women of the potential risk to a fetus.
There is no data on the presence of ponatinib in human milk, the effects on the breastfed infant or on milk production.