|Trade names||Alunbrig, others|
|Drug class||Tyrosine kinase inhibitor|
|Main uses||Non-small cell lung cancer (NSCLC)|
|Side effects||Diarrhea, tiredness, nausea, rash, muscle pain, headache, high blood pressure, shortness of breath|
|Chemical and physical data|
|Molar mass||584.10 g·mol−1|
|3D model (JSmol)|
Brigatinib, sold under the brand name Alunbrig among others, is a medication used to treat non-small cell lung cancer (NSCLC). Specifically it is used for metastatic cases that are ALK-positive. It is taken by mouth.
Common side effects include diarrhea, tiredness, nausea, rash, muscle pain, headache, high blood pressure, and shortness of breath. Other side effects may include pneumonitis, vision problems, muscle breakdown, pancreatitis, high blood sugar, and sunburns. Use in pregnancy may harm the baby. It is a tyrosine kinase inhibitor that blocks ALK.
Brigatinib was approved for medical use in the United States in 2017 and Europe in 2018. In the United Kingdom 4 weeks of medication costs the NHS about £4,900 as of 2021. This amount in the United States is about 17,400 USD.
It is taken at a dose of 90 mg once per day for 7 days and than increased to 180 mg once per day.
Mechanism of action
ALK was first identified as a chromosomal rearrangement in anaplastic large cell lymphoma (ALCL). Genetic studies indicate that abnormal expression of ALK is a key driver of certain types of non-small cell lung cancer (NSCLC) and neuroblastomas, as well as ALCL. Since ALK is generally not expressed in normal adult tissues, it represents a highly promising molecular target for cancer therapy.
Epidermal growth factor receptor (EGFR) is another validated target in NSCLC. Additionally, the T790M “gatekeeper” mutation is linked in approximately 50 percent of patients who grow resistant to first-generation EGFR inhibitors. While second-generation EGFR inhibitors are in development, clinical efficacy has been limited due to toxicity thought to be associated with inhibiting the native (endogenous or unmutated) EGFR. A therapy designed to target EGFR, the T790M mutation but avoiding inhibition of native EGFR is another promising molecular target for cancer therapy.
Ariad Pharmaceuticals, Inc. filed an investigational new drug (IND) application to the US FDA on August 29, 2016.
Society and culture
On 22 April 2015 ARIAD Pharmaceuticals, Inc. announced the issuance of its first U.S. patent on brigatinib, the protection is through December 30, 2030. The United States Patent and Trademark Office granted U.S. Patent No. 9,012,462 under the title, “Phosphorous Derivatives as Kinase Inhibitors.” 
Brigatinib is manufactured by ARIAD Pharmaceuticals, Inc. (NASDAQ: ARIA) which is focused on rare cancers. ARIAD then was acquired by Takeda Pharmaceutical Company Limited (TSE: 4502) in February 2017 through a tender offer (for $24.00 per share in cash) and subsequent merger of ARIAD with Kiku Merger Co., Inc., a wholly owned subsidiary of Takeda Pharmaceuticals U.S.A. ARIAD is now an indirect wholly owned subsidiary of Takeda.
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- Takeda Announces FDA Accelerated Approval of Alunbrig (brigatinib)
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