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Cobicistat

  • # LGM Pharma is a Cobicistat CAS# 1004316-88-4 API supplier distributor based in the USA. Inquire about DMF, cGMP, price, availability, samples, sourcing, purity and more.
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  • # LGM Pharma offers this active ingredient but not the finished dosage forms.
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Product Details:

  • Product Name: Cobicistat
  • CAS #: 1004316-88-4
  • Mode of Action:

    Cobicistat is a mechanism-based inhibitor of cytochrome P450 3A (CYP3A) isoforms. Inhibition of CYP3A-mediated metabolism by cobicistat increases the systemic exposure of CYP3A substrates atazanavir and darunavir and therefore enables increased anti-viral activity at a lower dosage. Cobicistat does not have any anti-HIV activity on its own.

  • Metabolism:

    Cobicistat is metabolized by CYP3A and to a minor extent by CYP2D6 enzymes and does not undergo glucuronidation.

  • Toxicity:

    The most common adverse reactions reported during clinical trials were jaundice (13%), ocular icterus (15%), and nausea (12%).

  • IUPAC: (1, 3-thiazol-5-yl)methyl N-[(2R, 5R)-5-[(2S)-2-{[methyl({[2-(propan-2-yl)-1, 3-thiazol-4-yl]methyl})carbamoyl]amino}-4-(morpholin-4-yl)butanamido]-1, 6-diphenylhexan-2-yl]carbamate
  • ATC: V03AX03
  • DrugBank: DB09065
  • Formula: C40-H53-N7-O5-S2
  • Molecular Mass: 776.0347
  • SMILES: C(=O)(N[C@H](CC[C@@H](NC(=O)[C@@H](NC(=O)N(Cc1nc(sc1)C(C)C)C)CCN1CCOCC1)Cc1ccccc1)Cc1ccccc1)OCc1scnc1
  • AHFS Code: 93:32:00
  • General Reference:

    1. German P, Warren D, West S, Hui J, Kearney BP: Pharmacokinetics and bioavailability of an integrase and novel pharmacoenhancer-containing single-tablet fixed-dose combination regimen for the treatment of HIV. J Acquir Immune Defic Syndr. 2010 Nov;55(3):323-9. doi: 10.1097/QAI.0b013e3181eb376b. Pubmed
    2. Mathias AA, German P, Murray BP, Wei L, Jain A, West S, Warren D, Hui J, Kearney BP: Pharmacokinetics and pharmacodynamics of GS-9350: a novel pharmacokinetic enhancer without anti-HIV activity. Clin Pharmacol Ther. 2010 Mar;87(3):322-9. doi: 10.1038/clpt.2009.228. Epub 2009 Dec 30. Pubmed
    3. Larson KB, Wang K, Delille C, Otofokun I, Acosta EP: Pharmacokinetic enhancers in HIV therapeutics. Clin Pharmacokinet. 2014 Oct;53(10):865-72. doi: 10.1007/s40262-014-0167-9. Pubmed
    4. Lepist EI, Phan TK, Roy A, Tong L, Maclennan K, Murray B, Ray AS: Cobicistat boosts the intestinal absorption of transport substrates, including HIV protease inhibitors and GS-7340, in vitro. Antimicrob Agents Chemother. 2012 Oct;56(10):5409-13. doi: 10.1128/AAC.01089-12. Epub 2012 Jul 30. Pubmed

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