BI 224436
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| Systematic (IUPAC) name | |
| (2S)-[4-(3,4-Dihydro-2H-chromen-6-yl)-3-quinolinyl][(2-methyl-2-propanyl)oxy]acetic acid | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | Investigational |
| Pharmacokinetic data | |
| Half-life | 7 hrs (simulated)[1] |
| Identifiers | |
| ATC code | None |
| ChemSpider | 27289461 |
| Chemical data | |
| Formula | C24H25NO4 |
| Mol. mass | 391.460 g//mol |
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BI 224436 is an investigational new drug under development for the treatment of HIV infection. BI 224436 is the first non-catalytic site integrase inhibitor (NCINI). It inhibits HIV replication via binding to a conserved allosteric pocket of the HIV integrase enzyme. This makes the drug distinct in mechanism of action compared to raltegravir and elvitegravir, which bind at the catalytic site.[2] In October 2011, Gilead Sciences purchased exclusive rights to develop BI 224436 and several related compounds under investigation in Boehringer Ingelheim’s noncatalytic site integrase inhibitor program.[3][4]
References [edit]
- ^ Pharmacodynamics of BI 224436 for HIV-1 in an in vitro hollow fiber infection model system
- ^ Levin, Jules. BI 224436, a Non-Catalytic Site Integrase Inhibitor, is a potent inhibitor of the replication of treatment-naïve and raltegravir-resistant clinical isolates of HIV-1. Conference Reports for NATAP. ICAAC Chicago Sept 17-20 2011.
- ^ Gilead Negotiates Worldwide License to BI’s Early Clinical Stage HIV Program. Genetic Engineering and Biotechnology News. 6 Oct 2011.
- ^ Highleyman, Liz. ICAAC: New Integrase Inhibitor BI 224436 Active against Raltegravir-Resistant HIV. HIVandHepatitis.com. 7 Oct 2011.
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