Bevirimat

• 3-O- (3 ', 3'- Dimethylsuccinyl ) - betulinic acid
• (3S)- 3-hydroxy- [ 3-O- (3 ', 3'- dimethylsuccinyl ) ] lup -20 ( 29) -en- 28 acid
• PA -457

Antiviral agent Matura Auditions inhibitor

Template: Infobox chemical / molecular formula search available

Bevirimat (PA -457, manufactured by Panacos ) is not yet approved drug for the treatment of HIV and its subsequent stages in a combination therapy for HIV.

It belongs to the group of Matura Auditions inhibitors.

History

After 2005, the first results of a small study of HIV-infected patients had been published, the end of 2005, the data of a placebo-controlled IIa trial have been published. Patients received ten days oral monotherapy with PA - 457th In the highest -dose 200 mg arm a decrease in viral load was achieved on average by 1.03 logs. In the 100 mg group, it was nevertheless still 0.48 logs. There were also patients in whom no significant effects were detected for the viral load.

Further studies are underway or are being planned.

Pharmacology

Bevirimat is a derivative of betulinic acid, which is isolated as triterpene from birch bark. Bevirimat inhibits replication at a late stage of the reproductive cycle, the so-called budding or maturation of virions. By bevirimat the conversion of the capsid precursor ( p25 ) in the mature capsid protein ( p24 ) is interrupted. It caused non-infectious viruses. Bevirimat acts synergistically with other anti-viral agents.

Pharmacokinetics

The compound has a long half-life. A daily single dose will definitely be possible.

Side effects

So far bevirimat was well tolerated.

Resistance

Bevirimat is also effective against resistant viruses. Resistance did not occur in man to date. In the laboratory, resistance mutations could be selected in the capsid and Gag target gene. These were point mutations. Therefore, a low resistance barrier is feared. However, resistant mutants appear to have a lower replication fitness than wild-type viruses. In January 2010, a study on the prediction of bevirimat - resistance based on the genotypes of HIV -1 has been published.