Generic Name |
Axitinib | |
---|---|---|
IND |
AG-013736 | |
Brand Name (US) |
Inlyta | |
Manufacturer |
Pfizer | |
Drug Type |
Tyrosine Kinase Inhibitor | |
Delivery |
Oral | |
Approval Status |
Approved for a non-GIST cancer | |
Indications |
Renal cell carcinoma (RCC) | |
Overall Strategy |
KIT Protein Based | |
Strategy |
Block KIT | |
Drug Category |
KIT/PDGFRA inhibitor+ VEGF inhibitor (TKI) |
Axitinib is an oral multi-tyrosine kinase inhibitor. It is approved in the United States and the EU as a treatment for Renal Cell Carcinoma (kidney cancer). It is not approved for GIST.
In addition to inhibiting VEGF 1,2 & 3, axitinib also inhibits KIT and PDGFRA.
In a randomized phase III trial for kidney cancer, axitinib provided longer progression-free survival with less patients discontinuing therapy compared to sorafenib (an approved kidney cancer drug). See link below.
The most common (≥20%) side effects occurring in patients receiving INLYTA (all grades) were diarrhea, hypertension, fatigue, decreased appetite, nausea, dysphonia, hand-foot syndrome, weight decreased, vomiting, asthenia and constipation. Hypothyrodism has also been reported (see thyrotropin link below)
The most common (≥10%) grade 3/4 AEs occurring in patients receiving INLYTA were hypertension, diarrhea and fatigue.
The most common (≥20%) lab abnormalities occurring in patients receiving INLYTA (all grades) included increased creatinine, decreased bicarbonate, hypocalcemia, decreased hemoglobin, decreased lymphocytes (absolute), increased ALP, hyperglycemia, increased lipase, increased amylase, increased ALT and increased AST.
As of September, 2012, there have been no clinical trials for GIST. It is unknown whether axitinib has any activity in GIST.