Drug intelligence / Profile preview

ponatinib + chemotherapy (Takeda)

Development stage
Unknown
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral, Intravenous, Intrathecal
01

Overview

Ponatinib is a potent, third-generation oral tyrosine kinase inhibitor (TKI) that targets BCR-ABL1, an abnormal tyrosine kinase that is the hallmark of Philadelphia chromosome-positive (Ph+) leukemias. It was specifically designed to inhibit BCR-ABL1 with the T315I mutation, which confers resistance to all other first- and second-generation TKIs. In the context of acute lymphoblastic leukemia (ALL), ponatinib is often administered in combination with various chemotherapy agents (such as vincristine, dexamethasone, and anthracyclines) to improve remission rates and overcome resistance. Takeda Pharmaceuticals markets ponatinib under the brand name Iclusig. It has received accelerated approval for newly diagnosed Ph+ ALL in adults when used with chemotherapy and is also indicated for patients with CML or Ph+ ALL who are resistant or intolerant to prior TKI therapy.

Other names
ponatinib hydrochloride
02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)BCR-ABL1 T315I (Bcr-Abl T315I mutant protein)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR4 (Fibroblast growth factor receptor 4)FLT3 D835Y (Fms-like Tyrosine Kinase 3 Receptor D835Y Mutant)KIT (c-KIT proto-oncogene receptor tyrosine kinase)CD274 (Programmed cell death protein 1 ligand 1)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)RET (Rearranged during transfection receptor tyrosine kinase)SRC (Proto-oncogene tyrosine-protein kinase Src)VEGFR2 (Vascular endothelial growth factor receptor 2)

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