What is Afatinib

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What is Afatinib

Basic Characteristics Product Name CAS Number Molecular Formula Formula Weight

Synonyms

Afatinib Powder 439081-18-2 C24H25ClFN5O3 485.9 Afatinib Powder; 439081-18-2; 850140-72-6; BIBW2992; Tovok.

Appearance Storage and Handling

White crystalline powder Store it at room temperature and away from excess heat and moisture.

Afatinib Powder Description Afatinib powder, sold under the brand name Gilotrif among others, is a medication used to treat non-small cell lung carcinoma (NSCLC).It belongs to the tyrosine kinase inhibitor family of medications.It is taken by mouth.

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Afatinib powder is mainly used to treat cases of NSCLC that harbour mutations in the epidermal growth factor receptor (EGFR) gene.

Afatinib Powder Mechanism of Action Like lapatinib and neratinib, afatinib powder is a protein kinase inhibitor that also irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases. Afatinib powder is not only active against EGFR mutations targeted by first generation tyrosine-kinase inhibitors (TKIs) like erlotinib or gefitinib, but also against less common mutations which are resistant to these drugs. However, it is not active against the T790M mutation which generally requires third generation drugs like osimertinib.Because of its additional activity against Her2, it is being investigated for breast cancer as well as other EGFR and Her2 driven cancers.

Afatinib Powder Application Afatinib powder has received regulatory approval for use as a treatment for non-small cell lung cancer,although there is emerging evidence to support its use in other cancers such as breast cancer.

Afatinib Powder Side Effects & Warning Very common (>10% frequency) Diarrhea (>90%) Rash/dermatitis acneform Stomatitis Paronychia 2

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Decreased appetite Nose bleed Itchiness Dry skin Common (1–10% frequency) Dehydration,Taste changes,Dry eye Cystitis,Cheilitis,Fever Runny/stuffy nose Low amount of potassium in the blood Conjunctivitis Increased ALT Increased AST Hand-foot syndrome Muscle spasms Kidney impairment and/or failure Uncommon (0.1-1% frequency) 3

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Keratitis Interstitial lung disease

Reference [1] “Gilotrif (afatinib powder) tablet, film coated”. DailyMed. Boehringer Ingelheim Pharmaceuticals, Inc. 18 October 2019. Retrieved 4 November 2020.

[2] Spreitzer H (13 May 2008). “Neue Wirkstoffe – Tovok”. Österreichische Apothekerzeitung (in German) (10/2008): 498 [3] Minkovsky N, Berezov A (December 2008). “BIBW-2992, a dual receptor tyrosine kinase inhibitor for the treatment of solid tumors”.

Current Opinion in Investigational Drugs. 9 (12): 1336–46. PMID 19037840.

[4] “Afatinib Powder”. US Food and Drug Administration. 12 July 2013.[dead link] [5] “Giotrif Afatinib Powder (as afatinib dimaleate)” (PDF). TGA eBusiness Services. Boehringer Ingelheim Pty Limited. 7 November 2013. Retrieved 28 January 2014.

[6] Vavalà T (2017). “Role of afatinib powder in the treatment of advanced lung squamous cell carcinoma”. Clinical Pharmacology. 9: 147–157. doi:10.2147/CPAA.S112715. PMC 5709991. PMID 29225480.

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