Chemistry:BI 224436
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Short description: Chemical compound
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| Elimination half-life | 7 hrs (simulated)[1] |
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| Formula | C27H26N2O4 |
| Molar mass | 442.515 g·mol−1 |
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BI 224436 was 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 its 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]
Clinical trials were abandoned in advance of Phase 1.[5]
References
- ↑ "Pharmacodynamics of BI 224436 for HIV-1 in an in vitro hollow fiber infection model system.". 51st Interscience conference on antimicrobial agents and chemotherapy. Chicago. 17 September 2011. pp. 17–20. http://www.natap.org/2011/ICAAC/ICAAC_33.htm.
- ↑ "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.". 51st Interscience Conference on Antimicrobials and Chemotherapy. Chicago: ICAAC. 17 September 2011. http://www.natap.org/2011/ICAAC/ICAAC_34.htm.
- ↑ "Gilead Negotiates Worldwide License to BI's Early Clinical Stage HIV Program". Genetic Engineering and Biotechnology News.. 6 October 2011. http://www.genengnews.com/gen-news-highlights/gilead-negotiates-worldwide-license-to-bi-s-early-clinical-stage-hiv-program/81245786/.
- ↑ "ICAAC: New Integrase Inhibitor BI 224436 Active against Raltegravir-Resistant HIV". HIVandHepatitis.com.. 7 October 2011. http://www.hivandhepatitis.com/hiv-aids/hiv-aids-topics/hiv-treatment/3268-icaac-new-integrase-inhibitor-bi-224436-active-against-raltegravir-resistant-hiv.
- ↑ Clinical trial number NCT01276990 for "Safety and Pharmacokinetics of Multiple Rising Oral Doses of BI 224436 in Healthy Male Volunteers." at ClinicalTrials.gov
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