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度鲁特韦片Tivicay(Dolutegravir Tablets)

新药编辑:新特药 更新时间:2015-04-25

Generic Name and Formulations:
Dolutegravir 50mg; tablets.

Company:
ViiV Healthcare

Indications for TIVICAY:
In combination with other antiretroviral agents for the treatment of HIV-1 infection.

Adult Dose for TIVICAY:
≥12 years and ≥40kg: treatment-naïve or treatment-experienced INSTI-naïve: 50mg once daily. Treatment-naïve or treatment-experienced INSTI-naïve with concomitant potent UGT1A/CYP3A inducers (eg, efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, or rifampin): 50mg twice daily. INSTI-experienced with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance: 50mg twice daily.

Children's Dose for TIVICAY:
<12 years or <40kg, or INSTI-experienced with documented or clinically suspected resistance to other INSTIs (raltegravir, elvitegravir): not established.

Pharmacological Class:
HIV-1 integrase strand transfer inhibitor (INSTI).

Contraindications:
Concomitant dofetilide.

Warnings/Precautions:
Discontinue if hypersensitivity reactions develop. Increased risk for worsening/development of elevated transaminases in patients with hepatitis B or C; monitor LFTs prior to starting and during therapy. Severe hepatic impairment: not recommended. INSTI-experienced patients (with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance) with severe renal impairment: decrease in dolutegravir concentrations may result in loss of efficacy and development of resistance. Pregnancy (Cat. B). Nursing mothers: not recommended.

Interactions:
May be affected by drugs that induce or inhibit UGT1A1, UGT1A3, UGT1A9, BCRP, and P-gp enzymes or transporters. Avoid concomitant nevirapine, oxcarbazepine, phenytoin, phenobarbital, carbamazepine, St. John’s wort. Avoid etravirine unless coadministered with atazanavir/ritonavir, darunavir/ritonavir, or lopinavir/ritonavir. Concomitant efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, or rifampin: adjust dose to 50mg twice daily. Concomitant cation-containing antacids, laxatives, sucralfate, oral iron/calcium supplements, and buffered drugs: give dolutegravir 2 hours before or 6 hours after. Concomitant metformin; monitor closely and adjust metformin dose if necessary.

Adverse Reactions:
Insomnia, headache; immune reconstitution syndrome, lab abnormalities.

How Supplied:
Tabs—30

Tivicay: a new once-daily HIV integrase inhibitor
Tivicay (dolutegravir) is a new once-daily integrase inhibitor licensed for the treatment of HIV-1 infection in combination with other antiretrovirals.
PHARMACOLOGY
Dolutegravir inhibits HIV integrase to block viral replication.1
CLINICAL STUDIES
Dolutegravir was investigated in 5 key pivotal studies for the treatment of HIV-1 infection in adults and children aged 12 years and older in combination with other antiretrovirals. In treatment-naïve patients, it was compared with raltegravir (SPRING-2), efavirenz (SINGLE) and darunavir (FLAMINGO).1–3
Once-daily dolutegravir has also been compared to raltegravir in treatment-experienced patients in the SAILING study and it was investigated administered twice-daily in highly pre-treated patients with evidence of integrase inhibitor resistance in the single-arm VIKING-3 study.4,5
Versus raltegravir
The SPRING-2 study showed that dolutegravir (50mg once daily) was non-inferior to raltegravir (400mg twice daily) when used in combination with a fixed-dose dual NRTI background regimen in 822 treatment-naïve patients with HIV-1 infection. At week 48, the percentage of patients with an undetectable viral load (HIV-1 RNA <50 copies/ml) was 88% in the dolutegravir group compared with 85% in the raltegravir group.2
Versus efavirenz
The SINGLE study (n=833) also recruited treatment-naïve HIV-1 infected patients but compared once-daily dolutegravir, in combination with lamivudine and abacavir, to efavirenz + emtricitabine + tenofovir (Atripla). A significantly higher proportion of patients achieved virological suppression (HIV-1 RNA <50 copies/ml) in the dolutegravir group compared with the triple combination tablet group at week 48: 88% vs 81% (p=0.003).3
Treatment-experienced patients
Dolutegravir was compared with raltegravir, both in combination with an optimised background regimen, in treatment-experienced patients with at least two-class drug resistance who had not yet received an integrase inhibitor in the SAILING study (n=719). On analysis after meeting the pre-specified non-inferiority criteria, dolutegravir (50mg once daily) was superior to raltegravir with a significantly higher proportion of patients with plasma HIV-1 RNA <50 copies/ml at week 48 (p=0.003).4
Dolutegravir displayed efficacy in highly pre-treated patients with resistance to multiple classes of antiretrovirals including integrase inhibitors (raltegravir and/or elvitegravir) in the single-arm, phase IIb VIKING-3 study (n=183). When dolutegravir (50mg twice daily) was added to their background regimen, 63% of patients achieved virological suppression (HIV-1 RNA <50 copies/ml).5
Versus darunavir
The open-label FLAMINGO study compared dolutegravir with ritonavir-boosted darunavir in 484 treatment-naïve patients. In the interim analysis at week 48, a significantly higher proportion of patients treated with dolutegravir had an HIV-1 RNA viral load of <50 copies/ml than patients treated with darunavir: 90% vs 83% (p=0.025).6
Safety profile
The adverse effects associated with dolutegravir showed similar incidences across all treatment populations. Nausea, diarrhoea and headache were most commonly observed.1

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