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Afatinib

  • #LGM Pharma is a Afatinib CAS# 850140-72-6 API supplier distributor based in the USA. Inquire about DMF, cGMP, price, availability, delivery, purity, and more.
  • #Questions? Call our customer API support number 1-(800)-881-8210.
  • #LGM Pharma offers this active ingredient but not the finished dosage forms.

Product Details:

  • CAS No: 850140-72-6
  • AHFC code: 10:00
  • Synonyms: (2E)-N-(4-(3-chloro-4-fluoroanilino)-7-(((3S)-oxolan-3-yl)oxy)quinoxazolin-6-yl)-4-(dimethylamino)but-2-enamide, Afatinib, BIBW 2992, BIBW2992, Tomtovok, Tovok, UNII-41UD74L59M
  • ATC Code: L01XE13
  • Chemical Formula: C24-H25-Cl-F-N5-O3
  • Molecular Weight: 485.9445
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB08916
  • SMILES: CN(C)C/C=C/C(=O)Nc1cc2c(cc1O[C,H]3CCOC3)ncnc2Nc4ccc(c(c4)Cl)F
  • InChl: 1S/C24H25ClFN5O3/c1-31(2)8-3-4-23(32)30-21-11-17-20(12-22(21)34-16-7-9-33-13-16)27-14-28-24(17)29-15-5-6-19(26)18(25)10-15/h3-6,10-12,14,16H,7-9,13H2,1-2H3,(H,30,32)(H,27,28,29)/b4-3+/t16-/m0/s1
  • PubChem:
  • IUPAC: 2-Butenamide, N-(4-((3-chloro-4-fluorophenyl)amino)-7-(((3S)-tetrahydro-3-furanyl)oxy)-6-quinazolinyl)-4-(dimethylamino)-, (2E)-

Additional Details

Indication:
Afatinib is a kinase inhibitor indicated for the first-line treatment of patient with metastatic non-small cell lung cancer (NSCLC) whose tumours have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test.
Pharmacodynamics:
Afatinib did not effect the QTc interval.
Mode of Action:
Afatinib is an irreversible kinase inhibitor and binds to the kinase domains of EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4) to inhibit tyrosine kinase autophosphorylation. This results in a downregulation of ErbB signalling and subsequent inhibition of proliferation of cell lines expressing wild-type EGFR, selected EGFR exon 19 deletion mutations, or exon 21 L858R mutations. It also inhibited in vitro proliferation of cell lines overexpressing HER2. Overall, tumour growth was inhibited.
Metabolism:
Enzymatic metabolism of afatinib is minimal. Covalent adducts to proteins are the major circulating metabolites.
Toxicity:
Most common adverse reactions (≥20%) are diarrhea, rash/dermatitis, acneiform, stomatitis, paronychia, dry skin, decreased appetite, pruritus.
General Reference:
FDA label
Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

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