n CME : Your SA Journal of CPD - New antiretrovirals : what is on the way? : main article
|Article Title||New antiretrovirals : what is on the way? : main article|
|© Publisher:||Health and Medical Publishing Group (HMPG)|
|Journal||CME : Your SA Journal of CPD|
|Publication Date||May 2005|
|Pages||255 - 259|
|Keyword(s)||Drug development, New antiretrovirals, New nucleonic reverse transcriptase inhibitors and Resistant HIV strains|
There is a need for new ARTs. <br>Tenofovir disoproxil fumarate is a nucleotide analogue of adenosine 5'-monophosphate. It was registered in the USA in 2001, initially for patients failing previous therapies and more recently extended to first-line therapy. <br>FTC is a cytidine analogue closely related to 3TC but is administered once daily. The potency and resistance profiles of FTC and 3TC are similar. <br>SPD 754 is a de-oxycytidine analogue that has in vitro activity against HIV strains with the 3TC resistance-associated M184V mutation. <br>D-D4FC is another de-oxycytidine analogue with in vitro activity against NRTI-resistant HIV strains. <br>Amdoxovir (DAPD) is a guanine analogue with a potentially attractive resistance profile. <br>Capravirine is a second-generation NNRTI that requires multiple mutations to develop in vitro high-level resistance. <br>TMC-125 is a di-aminopyrimidine NNRTI with potent in vitro activity against HIV, including clinical isolates with highlevel resistance to current NNRTIs. <br>Atazanavir is an azopeptide PI free of cholesterol and triglyceride abnormalities. <br>Fosamprenavir is a pro-drug of amprenavir and is formulated into 476 mg tablets. Its side-effect profile is similar to that of the parent drug. <br>Tipranavir is a non-peptidic HIV protease inhibitor, with interest driven by in vitro data, indicating activity against highly PI-resistant strains of HIV. <br>TMC-114 has potent in vitro and in vivo activity against PI-resistant strains. <br>New classes of ARVs include fusion inhibitors, chemokine co-receptor blockers and integrase inhibitors.
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