Afatinib dimaleate

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Afatinib dimaleate 화학적 특성, 용도, 생산

• 개요

  Afatinib dimaleate was approved by the U.S. Food and Drug Administration (FDA) in 2013 for the treatment of non-small cell lung cancer (NSCLC). Specifically, it was approved for patients presenting with metastatic NSCLC tumors which contain epidermal growth factor receptor (EGFR) exon deletions or exon 21 mutations. Afatinib dimaleate is a covalent inhibitor of ErbB tyrosine kinases (tyk), which downregulates ErbB signaling by irreversible binding of EGFR tyk binding sites. While no manufacturing route has been disclosed to date, the most scalable published route likely derives from two Boehringer Ingelheim patents.

• 용도

  Afatinib Dimaleate is a salt of Afatinib {BIBW 2992), an aminocrotonylamino-substituted quinazoline derivative used for treating cancer and diseases of the respiratory tract, lungs, gastrointestinal tract, bile duct, and gallbladder. An anilino-quinazoline that irreversibly inhibits EGFR and HER2 kinase activity.

• 정의

  ChEBI: Afatinib dimaleate is a maleate salt obtained by combining afatinib with two molar equivalents of maleic acid. Used for the first-line treatment of patients with metastatic non-small cell lung cancer. It has a role as a tyrosine kinase inhibitor and an antineoplastic agent. It contains an afatinib.

• 생물학적 활성

  Afatinib dimaleate is an orally bioavailable and irreversible dual-specific inhibitor of the ErbB family (EGFR and HER2). IC50 are 0.4, 0.5, 10, 14, 1 nM for EGFR^L858R, EGFR^wt, EGFR ^L858R/T790M, ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib dimaleate is available for cancer (esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer) studies.

• 부작용

  Afatinib dimaleate is similar to afatinib in terms of side effects. Common side effects include: diarrhoea, fever, difficulty urinating, burning or pain, redness, swelling or pain in the skin, discharge or excessive tearing, burning, dryness or itching of the eyes, and skin ulcers. Occasional symptoms of coughing and difficulty breathing. A very small number of patients may have bloody stools, black stools or tarry stools, indigestion, nausea, severe abdominal pain, cramping or burning sensation, and vomiting of a substance that looks like coffee grounds. Please contact your doctor promptly if any serious adverse reactions occur.

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