Ponatinib
Other name
-
International/Other brands
Iclusig
Groups
Approved
Structure
Prescription products
| Name | Dosage | Strength | Route | Labeller |
|---|---|---|---|---|
| Iclusig | Tablet | 15 mg | Oral | Ariad Pharmaceuticals |
| Iclusig | Tablet, film coated | 30 mg/1 | Oral | Ariad Pharmaceuticals |
| Iclusig | Tablet, film coated | 15 mg/1 | Oral | Ariad Pharmaceuticals |
| Iclusig | Tablet | 45 mg | Oral | Ariad Pharmaceuticals |
| Iclusig | Tablet, film coated | 45 mg/1 | Oral | Ariad Pharmaceuticals |
Target
Description
Ponatinib is a novel Bcr-Abl tyrosine kinase inhibitor that is especially effective against the T315I mutation for the treatment of chronic myeloid leukemia. FDA approved on December 14, 2012.
Indications
Accelerated phase chronic myologenic leukemia; Acute Lymphoblastic Leukaemias (ALL); Chronic Phase Chronic Myeloid Leukemia; Blast phase Chronic myelocytic leukemia
Other indications
-
Mechaism of action
-
Absorption
The most common non-hematologic adverse reactions (≥ 20%) were hypertension, rash, abdominal pain, fatigue, headache, dry skin, constipation, arthralgia, nausea, and pyrexia. Hematologic adverse reactions included thrombocytopenia, anemia, neutropenia, lymphopenia, and leukopenia.
Metabolism
At least 64% of a ponatinib dose undergoes phase I and phase II metabolism. CYP3A4 and to a lesser extent CYP2C8, CYP2D6 and CYP3A5 are involved in the phase I metabolism of ponatinib in vitro. Ponatinib is also metabolized by esterases and/or amidases.
Toxicity
The most common non-hematologic adverse reactions (≥ 20%) were hypertension, rash, abdominal pain, fatigue, headache, dry skin, constipation, arthralgia, nausea, and pyrexia. Hematologic adverse reactions included thrombocytopenia, anemia, neutropenia, lymphopenia, and leukopenia.