| Drug Name |
Pemigatinib |
| Drug ID |
BADD_D02582 |
| Description |
Pemigatinib is a small molecule kinase inhibitor with antitumour activity. It works by inhibiting fibroblast growth factor receptors (FGFRs), which are receptor tyrosine kinases that activate signalling pathways in tumour cells.[A193719] FGFRs gained attention as potential therapeutic targets in selected cancers, as FGFR gene alterations were observed in a wide variety of cancers including those of the urinary bladder, breast, ovary, prostate, endometrium, lung, and stomach.[A198984] Deregulated FGFR signalling pathway can lead the development of oncogenes and tumour-promoting physiological processes, such as cancer cell proliferation, enhanced angiogenesis, and evasion of cell death.[A193716]
In April 2020, pemigatinib was approved by the FDA for the treatment of unresectable locally advanced or metastatic cholangiocarcinoma in previously treated adult patients with a fibroblast growth factor receptor 2 (FGFR2) gene fusion or other rearrangements as detected by an FDA-approved test.[L13068] Cholangiocarcinoma is the most common primary malignancy affecting the biliary tract and the second most common primary hepatic malignancy. This malignancy accounts for 15% to 20% of primary hepatobiliary malignancies, which account for 13% of overall cancer-related global mortality. With increasing research on the pathogenesis of cholangiocarcinoma and potential therapeutic targets for anticancer drug treatment, recent studies show that up to 45% of patients with intrahepatic cholangiocarcinoma exhibited gene rearrangements resulting in oncogenic fibroblast growth factor 2 (FGFR2) fusion proteins.[A198963] The FDA-approved indication for pemigatinib was granted under accelerated approval based on the overall response rate and duration of response in pre-marketing clinical trials. Pemigatinib is marketed under the brand name Pemazyre, and it is available as oral tablets.[L13050] |
| Indications and Usage |
Pemigatinib is indicated for the treatment of unresectable locally advanced or metastatic cholangiocarcinoma in previously-treated adult patients with a fibroblast growth factor receptor 2 (FGFR2) fusion or other rearrangement as detected by an FDA-approved test.[L13050] |
| Marketing Status |
approved; investigational |
| ATC Code |
L01EN02 |
| DrugBank ID |
DB15102
|
| KEGG ID |
D11417
|
| MeSH ID |
C000705477
|
| PubChem ID |
86705695
|
| TTD Drug ID |
D0O6UY
|
| NDC Product Code |
70277-503; 50881-026; 70277-501; 50881-028; 58567-108; 50881-027; 70277-502 |
| UNII |
Y6BX7BL23K
|
| Synonyms |
pemigatinib | 2H-Pyrrolo(3',2':5,6)pyrido(4,3-d)pyrimidin-2-one, 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-1,3,4,7-tetrahydro-8-(4-morpholinylmethyl)- | Pemazyre | INCB054828 | INCB-054828 |
