{"id":20318,"date":"2012-10-01T12:00:35","date_gmt":"2012-10-01T12:00:35","guid":{"rendered":"http:\/\/i-base.info\/htb\/?p=20318"},"modified":"2020-02-17T16:22:46","modified_gmt":"2020-02-17T16:22:46","slug":"merck-acquires-cmx157-and-efda-and-starts-phase-2-study-for-new-nnrti","status":"publish","type":"post","link":"https:\/\/i-base.info\/htb\/20318","title":{"rendered":"Merck acquires CMX157 and EFdA and starts phase 2 study for new NNRTI"},"content":{"rendered":"

Simon Collins, HIV i-Base<\/strong><\/p>\n

On 24 July 2012, a press release from Merck announced that the company had signed licensing agreement for the development of two new nucleoside analogues and is about to launch a phase 2 study for its in house NNRTI. [1]<\/strong><\/p>\n

CMX157 is a nuceloside analogue in development at Chimerix that reported promising phase 1 results over four years ago and has been waiting for a financial backer since. [2] The compound is a prodrug of tenofovir (tenofovir diphosphate as the active moiety), with an improved pharmacokinetic profile to tenofovir and initial results suggesting a potential for once-weekly dosing. The in vitro resistance profile includes sensitivity to K65R with some but not all thymidine analogue mutations. This was a compound that was expected to be picked up several years ago.<\/p>\n

EFdA (4′-ethynyl-2-fluoro-2′-deoxyadenosine) is a compound in development with the Japanese biotech division of the Yamasa Corporation (who have a history that includes brewing soy sauce since the time of the English civil war) and which has been studied with amFAR and US NIH support. A poster presented at the 19th IAS conference in Washington this summer reported a significantly stronger in vitro resistance profile compared to tenofovir following multiple passaging with a mixture of 11 multinucleoside resistant viral mutations.<\/p>\n

Merck also used the opportunity to announce its in-house NNRTI compound MK1439 is about to enroll treatment naive patients into a phase 2 dose-finding study (from 25 mg to 200 mg) using efavirenz as a comparitor and tenofovir\/FTC as background nukes.<\/p>\n

comment<\/h2>\n

It is promising news that Merck is developing an active programme of research for new HIV drugs to in parallel to development of integrase inhibitors.\u00a0<\/strong><\/p>\n

Although less well publicised, Merck is also one of the companies investing in cure research.<\/strong><\/p>\n

References:<\/p>\n

    \n
  1. Merck press release. Merck signs two deals for novel HIV drug candidates and initiates phase II clinical trial of MK-1439 for HIV. (24 July 2012).
    \nhttp:\/\/www.merck.com\/newsroom\/news-release-archive\/research-and-development\/2012_0724.html<\/a><\/li>\n
  2. Lanier ER et al. Hexadecyloxpropyl tenofovir (CMX157) has enhanced potency in vitro against NRTI resistant HIV relative to tenofovir and a favorable preclinical profile. XVII IHDRW 2008, Sitges. Poster 4.
    \n    https:\/\/i-base.info\/htb\/598<\/a><\/li>\n
  3. Maeda\u00a0 K et al. Delayed emergence of HIV-1 variants resistant to 4′-ethnyl-2-fluoro-2′-deoxyadenosine (EFdA): comparative sequential passage study with tenofovir, emtricitabine and festinavir. 19th IAC, 22-25 July 2012, Washington. Poster abstract TUPE017.
    \n    http:\/\/pag.aids2012.org\/abstracts.aspx?aid=18620<\/a><\/li>\n
  4. A dose-ranging study to compare MK-1439 plus Truvada versus efavirenz plus Truvada in human immunodeficiency virus (HIV)-1 infected participants (MK-1439-007 AM5).
    \n    http:\/\/clinicaltrials.gov\/ct2\/show\/NCT01632345<\/a><\/li>\n<\/ol>\n","protected":false},"excerpt":{"rendered":"

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