Basic Characteristics

Product Name	Afatinib
CAS Number	439081-18-2
Molecular Formula	C24H25ClFN5O3
Formula Weight	485.9
Synonyms	Afatinib; 439081-18-2; 850140-72-6; BIBW2992; Tovok.
Appearance	White crystalline powder
Storage and Handling	Store it at room temperature and away from excess heat and moisture.

 

Afatinib Description

Afatinib, 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.

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

 

Afatinib Mechanism of Action

Like lapatinib and neratinib, afatinib is a protein kinase inhibitor that also irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases. Afatinib 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 Application

Afatinib 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 Side Effects & Warning

Very common (>10% frequency)

▪ Diarrhea (>90%)

▪ Rash/dermatitis acneform

▪ Stomatitis

▪ Paronychia

▪ 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)

▪ Keratitis

▪ Interstitial lung disease

 

Reference

[1] “Gilotrif (afatinib) 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”. US Food and Drug Administration. 12 July 2013.[dead link] [5] “Giotrif Afatinib (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 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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