Pharmacological Class:
Nucleoside reverse transcriptase inhibitors (NRTIs) + integrase strand transfer inhibitor (INSTI).

Active Ingredient(s):
Abacavir 600mg, dolutegravir 50mg, lamivudine 300mg; tablets.

Company
ViiV Healthcare
Indication(s):
HIV-1 infection. Limitations of use: not recommended alone in patients with current or history of resistance to any of the components; or alone in resistance-associated integrase substitutions or INSTI resistance due to insufficient dolutegravir dose in Triumeq in these subpopulations.

Pharmacology:
Dolutegravir inhibits HIV integrase by binding to the active site and blocking the strand transfer step of retroviral DNA integration. Abacavir inhibits the activity of HIV-1 reverse transcriptase by competing with the natural substrate deoxyguanosine-5'-triphosphate and by its incorporation into viral DNA. Lamivudine inhibits HIV reverse transcriptase via DNA chain termination after incorporation of the nucleotide analog.

Clinical Trials:
The efficacy of Triumeq is supported by data from a randomized, controlled trial in antiretroviral treatment-naïve subjects, SINGLE, and other trials in treatment-naïve subjects. The efficacy of dolutegravir, in combination with ≥2 active background regimens in treatment-experienced, INSTI-naïve subjects is supported by data from SAILING.

For clinical trials data, see full labeling for Triumeq and Tivicay.
Legal Classification:
Rx

Adults:
1 tablet daily. Concomitant efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, rifampin: give additional dolutegravir 50mg separated by 12 hours from Triumeq.

Children:
Not established.

Contraindication(s):
Presence of HLA-B*5701 allele. Previous hypersensitivity reaction to any of the components. Concomitant dofetilide. Moderate or severe hepatic impairment.

Warnings/Precautions:
See full labeling re: fatal hypersensitivity reactions with abacavir; discontinue as soon as suspected; do not restart. eva luate for presence of HLA-B*5701 allele prior to starting therapy or reinitiation; if (+), abacavir is contraindicated; discontinue permanently if hypersensitivity cannot be ruled out even if other diagnoses are possible, regardless of HLA-B*5701 status. If stopped for reasons other than hypersensitivity, restart only if medical care can be readily accessed; monitor. Suspend if lactic acidosis or hepatotoxicity occurs. Increased risk for worsening/development of elevated transaminases in patients with hepatitis B or C; monitor LFTs prior to starting, during therapy, and for at least several months after stopping treatment (discontinuing may exacerbate HBV infection). Decompensated liver disease; monitor. Immune reconstitution syndrome. Fat redistribution. Myocardial infarction: consider CHD risk before starting therapy and minimize modifiable risk factors (eg, HTN). Renal impairment (CrCl <50mL/min): not recommended. Use individual components if lamivudine or abacavir dose reductions are required. Elderly. Pregnancy (Cat.C). Nursing mothers: not recommended.

Interaction(s)
Concomitant other abacavir- or lamivudine-containing products: not recommended. Ethanol may increase abacavir levels. Abacavir may increase clearance of methadone. Dolutegravir may be affected by drugs that induce or inhibit UGT1A1, CYP3A, UGT1A3, UGT1A9, BCRP, and P-gp enzymes or transporters. Avoid concomitant nevirapine, oxcarbazepine, phenytoin, phenobarbital, carbamazepine, St. John’s wort. Potentiates metformin; consider reducing metformin dose. Concomitant etravirine without atazanavir/ritonavir, darunavir/ritonavir, or lopinavir/ritonavir: not recommended. Concomitant efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, rifampin: requires extra dolutegravir dose (see Adults). Concomitant cation-containing antacids or laxatives, sucralfate, buffered drugs, oral calcium/iron supplements, multivitamins; give Triumeq 2hrs before or 6hrs after; alternatively, oral calcium/iron can be used at the same time when taken with food. Monitor for toxicities with IFN-α ± ribavirin (consider reducing dose or discontinue one or both drugs).

Adverse Reaction(s)
Insomnia, headache, fatigue.

How Supplied:
Tabs—30

LAST UPDATED:
12/2/2014

新的抗艾滋病三合一固定剂量复方制剂Triumeq获准
葛兰素史克控制多半股权、以艾滋病治疗为重点的ViiV医疗保健公司的三合一药丸于 8月22日获得FDA批准，并有意向吉利德科学公司发起挑战领导地位。
该药将以Triumeq商品名销售，由阻止人免疫缺陷病毒复制的阿巴卡韦（abacavir）和拉米夫定（lamivudine），与抑制有助于HIV破坏宿主DNA的一种酶的dolutegravir（整合酶抑制剂）组成。每个组份均已获得FDA批准，但葛兰素史克、辉瑞和日本盐野义制药共有的ViiV公司相信三合一制剂能使给药变得简单方便，从而提高患者的依从性。
在这一复合制剂的III期计划中，它成功地击败了吉利德公司三合一“鸡尾酒”Atripla（Efavirenz-Emtricitabine-Tenofovir Disoproxil Fumarate，依法韦仑-恩曲他滨-富马酸替诺福韦酯。2006-7-12获美国FDA批准），在第96周病毒学抑制达到80％统计学上显著，相比之下Atripla为72％。吉利德的Atripla在该类固定剂量制剂中占据主导地位，2013年为吉利德带来36亿美元销售收益。
“Triumeq的获准为美国艾滋病患者提供了首个含dolutegravir的三合一固定剂量制剂，”公司首席执行官Dominique Limet说。