Authored By: B. V Waghmare

Thursday, August 22, 2013

Dolutegravir The Second drug in the class of HIV integrase inhibitors

Second drug in the class of HIV integrase strand transfer inhibitors approved by US FDA to treat HIV infection

Until 13-Aug-2013 there was only one drug Raltegravir available under the class of HIV integrase strand transfer inhibitors, on 13-Aug-2013 US FDA approved one more drug Tivicay (dolutegravir), HIV integrase strand transfer inhibitor to treat HIV infection. It is found to be effective in patients which develop resistance to earlier available drug Raltegravir and for patients who have not yet received any HIV drug therapy.

HIV infection is critical to treat because it causes integration of HIV viral gene in the form of provirus DNA in to human DNA , HIV forms its DNA through a mechanism of reverse transcription from the viral RNA. Thus using metabolic activities of a normal human cell for its (HIV) reproduction
In-order to control the viral load, drugs which inhibits the almost all stages of infection are used. This is the base for combination therapy.

Information on Tivicay (dolutegravir):

Drug Tivicay (dolutegravir) belongs to HIV integrase Inhibitor. Drug Tivicay (dolutegravir) is approved by US FDA under fast track approval process for drugs, its efficacy and safety was evaluated in clinical trial conducted on 2,539 patients, Tivicay (dolutegravir) was given along with Atripla, a fixed dose combination drug which contain efavirenz, emtricitabine and tenofovir, and results were found satisfactory in reducing HIV viral count and increasing CD4 counts in participants taking Tivicay (dolutegravir), it showed satisfactory results in reducing viral load, patient aged 12 year with at least 40 kg who has not taken any anti retroviral drug therapy ( Treatment Nave ) were also shown reduction in viral count.

Drug Drug Tivicay (dolutegravir) is also been studied for use along with Abacavir and Lamivudine, in a new new fixed dose combination for its effectiveness and safety in reducing HIV viral count.

Source : http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm364744.htm


Authored by : B.V.Waghmare

Last Updated : 22-Aug-2013

Antiretroviral drugs available to treat HIV infection

Details of Antiretroviral drugs. 
1) Nucleoside Reverse Transcriptase Inhibitors (NRTIs) : In this class there are about thirteen drugs available.
2) Nonnucleoside Reverse Transcriptase Inhibitors (NNRTIs) : In this category Five drugs are available
3) Protease Inhibitors (PIs) : In this category 10 Drugs are available.

4) Fusion Inhibitors : One drug is available

5) Entry Inhibitors - CCR5 co-receptor antagonist: One drug is available

6) HIV integrase strand transfer inhibitors : Two drugs are available.


Antiretroviral drugs used in the treatment of HIV infection

Following is the list of drugs used in the treatment of HIV Infection

A) Multi-class Combination Drugs.

1) Efavirenz, Emtricitabine and Tenofovir disoproxil fumarate
2) Emtricitabine, Rilpivirine, and Tenofovir disoproxil fumarate
3) Elvitegravir, Cobicistat, Emtricitabine, Tenofovir disoproxil fumarate

B) Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

1) Lamivudine and Zidovudine
2) Emtricitabine, FTC
3) Lamivudine, 3TC
4) Abacavir and Lamivudine
5) Zalcitabine, Dideoxycytidine, ddC
6) Zidovudine, Azidothymidine, AZT, ZDV
7) Abacavir, Zidovudine, and Lamivudine
8) Tenofovir disoproxil fumarate and Emtricitabine
9) Enteric coated didanosine, ddI EC
10) Didanosine, dideoxyinosine, ddI
11) Tenofovir disoproxil fumarate, TDF
12) Stavudine, d4T
13) Abacavir sulfate, ABC


C) Nonnucleoside Reverse Transcriptase Inhibitors (NNRTIs)
1) Rilpivirine
2) Etravirine
3) Delavirdine, DLV
4) Efavirenz, EFV
5) Nevirapine, NVP



D) Protease Inhibitors (PIs)
1) Amprenavir, APV
2) Tipranavir, TPV
3) Indinavir, IDV,
4) Saquinavir (no longer marketed)
5) Lopinavir and ritonavir, LPV/RTV
6) Fosamprenavir Calcium, FOS-APV
7) Ritonavir, RTV
8) Darunavir
9) Atazanavir sulfate, ATV
10) Nelfinavir mesylate, NFV


E) Fusion Inhibitors
1) Enfuvirtide, T-20

F) Entry Inhibitors - CCR5 co-receptor antagonist
1) Maraviroc
G) HIV integrase strand transfer inhibitors
1) Raltegravir
2) Dolutegravir

Source :
http://www.fda.gov/ForConsumers/ByAudience/ForPatientAdvocates/HIVandAIDSActivities/ucm118915.htm


Authored by : B.V.Waghmare

Last Updated : 22-Aug-2013