Product Name

Cobicistat

CAS Number

1004316-88-4

LGM Pharma is an API distributor. LGM Pharma can supply CGMP and/or DMF products, subject to availability and manufacturer requirements. LGM Pharma does not sell or supply APIs or finished dosage products to individual patients, doctors, pharmacies, or any pharmaceutical companies.

Questions? Call our customer API support number 1-(800)-881-8210

Product Name:
Cobicistat
CAS Number:
1004316-88-4
Indication:
Cobicistat is a CYP3A inhibitor indicated to increase systemic exposure of atazanavir or darunavir (once daily dosing regimen) in combination with other antiretroviral agents in the treatment of HIV-1 infection. It is not interchangeable with ritonavir to increase systemic exposure of darunavir 600 mg twice daily, fosamprenavir, saquinavir, or tipranavir due to lack of exposure data. The use of cobicistat is not recommended with darunavir 600 mg twice daily, fosamprenavir, saquinavir or tipranavir. Complex or unknown mechanisms of drug interactions preclude extrapolation of ritonavir drug interactions to certain cobicistat interactions. Cobicistat and ritonavir when administered with either atazanavir or darunavir may result in different drug interactions when used with concomitant medications.
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:
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

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.

LGM currently offers Monoclonal Antibodies (mAbs) for non-GMP/R&D use. Please inquire about Monoclonal Antibodies produced under GMP conditions.

Questions? Call our customer API support number 1-(800)-881-8210. 

Ask us about this product

API’s From Quality Manufacturers:

  • Streamlined API supply towards initial research stages as well as larger quantities of cGMP material for clinical trials and product commercialization
  • Premium quality GMP certified and fully accredited API manufacturing plants
  • Technical packages as well as access to filed DMF, ASMF or CEP (subject to availability)
  • Regulatory and technical assistance towards any submission type based on specific customer requirements

Find an API Product

Search
Generic filters