Quantcast

Subscribe to:
POZ magazine
E-newsletters
Join POZ: Facebook MySpace Twitter Pinterest
Tumblr Google+ Flickr MySpace
POZ Personals
Sign In / Join
Username:
Password:
Welcome, Guest. Please login or register.
April 25, 2014, 03:54:37 AM

Login with username, password and session length


Members
Stats
  • Total Posts: 621416
  • Total Topics: 46816
  • Online Today: 206
  • Online Ever: 585
  • (January 07, 2014, 02:31:47 PM)
Users Online
Users: 3
Guests: 172
Total: 175

Welcome


Welcome to the POZ/AIDSmeds Community Forums, a round-the-clock discussion area for people with HIV/AIDS, their friends/family/caregivers, and others concerned about HIV/AIDS.  Click on the links below to browse our various forums; scroll down for a glance at the most recent posts; or join in the conversation yourself by registering on the left side of this page.

Privacy Warning:  Please realize that these forums are open to all, and are fully searchable via Google and other search engines. If you are HIV positive and disclose this in our forums, then it is almost the same thing as telling the whole world (or at least the World Wide Web). If this concerns you, then do not use a username or avatar that are self-identifying in any way. We do not allow the deletion of anything you post in these forums, so think before you post.

  • The information shared in these forums, by moderators and members, is designed to complement, not replace, the relationship between an individual and his/her own physician.

  • All members of these forums are, by default, not considered to be licensed medical providers. If otherwise, users must clearly define themselves as such.

  • Forums members must behave at all times with respect and honesty. Posting guidelines, including time-out and banning policies, have been established by the moderators of these forums. Click here for “Am I Infected?” posting guidelines. Click here for posting guidelines pertaining to all other POZ/AIDSmeds community forums.

  • We ask all forums members to provide references for health/medical/scientific information they provide, when it is not a personal experience being discussed. Please provide hyperlinks with full URLs or full citations of published works not available via the Internet. Additionally, all forums members must post information which are true and correct to their knowledge.

  • Product advertisement—including links; banners; editorial content; and clinical trial, study or survey participation—is strictly prohibited by forums members unless permission has been secured from POZ.

To change forums navigation language settings, click here (members only), Register now

Para cambiar sus preferencias de los foros en español, haz clic aquí (sólo miembros), Regístrate ahora

Finished Reading This? You can collapse this or any other box on this page by clicking the symbol in each box.

Author Topic: New Antiretrovirals in development  (Read 1027 times)

0 Members and 1 Guest are viewing this topic.

Offline GoForIt

  • Member
  • Posts: 87
New Antiretrovirals in development
« on: October 22, 2013, 10:23:03 AM »
http://www.aidsmap.com/page/2782641/

Beginning with nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs), two new pro-drugs of tenofovir are being evaluated, tenofovir alafenamide (TAF) and CMX157. Tenofovir, a component of widely used co-formulations including Truvada, Eviplera and Atripla, is highly effective but can cause kidney and bone toxicity. TAF – now in phase 3 testing – produces higher drug levels in cells but allows for lower dosing with less effect on the kidneys and bones.

CMX157 also carries less risk of kidney toxicity and its long half-life in a phase 1 trial suggests once-weekly dosing may be possible.

Similarly, BMS-986001 is a new analogue of d4T (stavudine, Zerit). This drug is no longer used due to toxicities, with the exception of in some resource-limited settings, where it is a cheap option. BMS-986001 – now in phase 2b development – causes less mitochondrial toxicity, according to early studies.

Another NRTI in the pipeline, EFdA, is "the most potent antiretroviral reported to date" in laboratory studies, Raffi said. He also mentioned two other drugs in this class, elvucitabine and apricitabine, that have languished in the pipeline since the early 2000s.

Turning to non-nucleoside reverse transcriptase inhibitors (NNRTIs), MK-1439 "is the most promising candidate," according to Raffi. MK-1493 has several attractive properties, including activity against HIV that has developed resistance to older NNRTIs, and it has demonstrated good antiviral activity and tolerability in a phase 1b monotherapy study. Another novel NNRTI, AIC292, has also shown good activity against drug-resistant HIV.

Researchers are working on a new type of non-catalytic site integrase inhibitors, also known as lens epithelium-derived growth factor inhibitors or LEDGINs, that interfere with a protein (LEDGF/p75) that HIV uses to integrate its genetic material into host cell chromosomes.

Leaving the currently approved antiretroviral classes, Raffi reviewed some agents now in development that target other steps of the viral lifecycle. Cenicriviroc works as a CCR5 entry inhibitor (like maraviroc, Celsentri) but also blocks the CCR2 receptor. Data presented at this meeting demonstrated good antiviral activity and tolerability in a phase 2 clinical trial.

BMS-663068 interacts with HIV's gp120 envelope protein and interferes with binding to CD4 cells. Its mechanism of action resembles that of enfuvirtide (T-20, Fuzeon) but it is an oral pill rather than a daily injection.

While daily injections are clearly problematic, many people would be willing to take a single monthly or quarterly shot for HIV maintenance therapy or perhaps for pre-exposure prophylaxis (PrEP). Two such injectables are proceeding through the development pipeline: TMC278-LA, a long-acting form of rilpivirine (Edurant), and GSK1265744, a new integrase inhibitor that is also being tested as an oral medication.

In the near future, Raffi predicted, we will see more fixed-dose combinations and single-tablet regimens, including the first co-formulations containing HIV protease inhibitors and the first to incorporate abacavir/3TC (rather than tenofovir/emtricitabine) as the NRTI components.
08/09/2013   Diagnosed WB positive
08/20/2013   CD4-506(28%)  VL-10,800
09/12/2013   CD4-391(28%)  VL-14,900
09/17/2013   Start ART (Truvada & Tivicay)
10/11/2013   CD4-377(26%)  VL-UD
12/20/2013   CD4-590(??%)  VL-UD
03/18/2014   CD4-660(29%)  VL-UD

Offline Miss Philicia

  • Member
  • Posts: 23,582
  • celebrity poster, faker & poser
Re: New Antiretrovirals in development
« Reply #1 on: October 22, 2013, 10:35:08 AM »
Lots of great news in that article for everyone, though the one thing I find odd is the development of a pro-drug related to Zerit.
"I’ve slept with enough men to know that I’m not gay"

 


Terms of Membership for these forums
 

© 2014 Smart + Strong. All Rights Reserved.   terms of use and your privacy
Smart + Strong® is a registered trademark of CDM Publishing, LLC.