Clinical Review & Education
From The Medical Letter on Drugs and Therapeutics
Dolutegravir (Tivicay) for HIV The FDA has approved dolutegravir (doll-you-TEG-rah-veer; Tivicay – Viiv Healthcare), an integrase strand transfer inhibitor (INSTI), for treatment of HIV-1 infection in adults and in children ⱖ12 years old who weigh at least 40 kg. It is the third INSTI to be approved by the FDA; raltegravir and elvitegravir were approved earlier (Table 1).1,2
Table 2. Some Clinical Studies
a
Comparator Therapy Antiretroviral-Naive
Table 1. Integrase Strand Transfer Inhibitors Drug Dolutegravir – Tivicay (Viiv Healthcare)
Usual Adult Dosage 50 mg once/db
Cost, $a
150/150/200/300 mg once/d
2342.47
Raltegravir – Isentress (Merck)
400 mg bid
1074.08
a
Wholesale acquisition cost (WAC) for 30-days’ treatment. Source: $ource® Monthly (Selected from FDB MedKnowledge™) September 5, 2013. Reprinted with permission by FDB, Inc. All rights reserved. ©2013. www.fdbhealth.com /policies/drug-pricing-policy. Actual retail prices may be higher.
b
Dose for INSTI-naive patients.
INSTIs INSTIs block the activity of HIV-1 integrase, preventing viral DNA from integrating with cellular DNA. Raltegravir is generally well tolerated and is not metabolized by CYP3A, but must be taken twice daily and is not available in a fixed-dose combination with NRTIs. Elvitegravir is only available in combination (Stribild) with the NRTIs emtricitabine and tenofovir and the CYP3A inhibitor cobicistat, which permits once-daily dosing of elvitegravir, but interacts with many other drugs. Stribild must be taken with food and should not be used in patients with renal insufficiency. HIV strains that become resistant to raltegravir are often cross-resistant to elvitegravir, and vice versa.
88% vs 86%
Efavirenzc (n=833)
88% vs 81%d
Darunavir/ritonavire,f (n=484)
90% vs 83%d
Raltegravirg (n=715)
71% vs 64%d
a
Both dolutegravir and the comparators were given in addition to 2 NRTIs.
b
F Raffi et al. Lancet 2013; 381:735.
c
S Walmsley et al. Presented at 52nd Interscience Conference on Antimicrobial Agents and Chemotherapy. San Francisco, CA; September 9-12, 2012. Available at www.natap.org/2012/ICAAC/ICAAC_06.htm.
d
P
From The Medical Letter on Drugs and Therapeutics
Dolutegravir (Tivicay) for HIV The FDA has approved dolutegravir (doll-you-TEG-rah-veer; Tivicay – Viiv Healthcare), an integrase strand transfer inhibitor (INSTI), for treatment of HIV-1 infection in adults and in children ⱖ12 years old who weigh at least 40 kg. It is the third INSTI to be approved by the FDA; raltegravir and elvitegravir were approved earlier (Table 1).1,2
Table 2. Some Clinical Studies
a
Comparator Therapy Antiretroviral-Naive
Table 1. Integrase Strand Transfer Inhibitors Drug Dolutegravir – Tivicay (Viiv Healthcare)
Usual Adult Dosage 50 mg once/db
Cost, $a
150/150/200/300 mg once/d
2342.47
Raltegravir – Isentress (Merck)
400 mg bid
1074.08
a
Wholesale acquisition cost (WAC) for 30-days’ treatment. Source: $ource® Monthly (Selected from FDB MedKnowledge™) September 5, 2013. Reprinted with permission by FDB, Inc. All rights reserved. ©2013. www.fdbhealth.com /policies/drug-pricing-policy. Actual retail prices may be higher.
b
Dose for INSTI-naive patients.
INSTIs INSTIs block the activity of HIV-1 integrase, preventing viral DNA from integrating with cellular DNA. Raltegravir is generally well tolerated and is not metabolized by CYP3A, but must be taken twice daily and is not available in a fixed-dose combination with NRTIs. Elvitegravir is only available in combination (Stribild) with the NRTIs emtricitabine and tenofovir and the CYP3A inhibitor cobicistat, which permits once-daily dosing of elvitegravir, but interacts with many other drugs. Stribild must be taken with food and should not be used in patients with renal insufficiency. HIV strains that become resistant to raltegravir are often cross-resistant to elvitegravir, and vice versa.
88% vs 86%
Efavirenzc (n=833)
88% vs 81%d
Darunavir/ritonavire,f (n=484)
90% vs 83%d
Raltegravirg (n=715)
71% vs 64%d
a
Both dolutegravir and the comparators were given in addition to 2 NRTIs.
b
F Raffi et al. Lancet 2013; 381:735.
c
S Walmsley et al. Presented at 52nd Interscience Conference on Antimicrobial Agents and Chemotherapy. San Francisco, CA; September 9-12, 2012. Available at www.natap.org/2012/ICAAC/ICAAC_06.htm.
d
P
