FDA已批准Tivicay（dolutegravir）50mg片剂为治疗HIV-1感染新药
Tivicay为每日一次的口服药物，是HIV整合酶抑制剂，旨在与其他抗逆转录病毒制剂联合用于既往已治疗过、或初治HIV-1成人和12岁及以上体重至少40千克儿童感染者。
TIVICAY Rx   
Generic Name and Formulations:
Dolutegravir 50mg; tabs.
Company:
ViiV Healthcare
Viral infections
Viral infections
 
Indications for TIVICAY:
In combination with other antiretroviral agents for the treatment of HIV-1 infection.

Adult:
≥12yrs and ≥40kg: treatment-naïve or treatment-experienced INSTI-naïve: 50mg once daily. Treatment-naïve or treatment-experienced INSTI-naïve with concomitant certain UGT1A or CYP3A inducers: 50mg twice daily. INSTI-experienced with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance: 50mg twice daily.

Children:
<12yrs or <40kg, or INSTI-experienced with documented or clinically suspected resistance to other INSTIs (raltegravir, elvitegravir): not established.

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. Dialysis. Elderly. 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, St. John’s wort. Avoid etravirine unless coadministered with atazanavir/ritonavir, darunavir/ritonavir, or lopinavir/ritonavir. Concomitant efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, rifampin, or carbamazepine: adjust dose (see Adults). Concomitant cation-containing antacids, laxatives, sucralfate, oral iron/calcium supplements, and buffered drugs: give dolutegravir 2hrs before or 6hrs after. Limit concomitant metformin dose to 1000mg/day; adjust metformin dose when stopping dolutegravir; monitor closely.

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

Adverse Reactions:
Insomnia, fatigue, headache; immune reconstitution syndrome, fat redistribution, lab abnormalities, hypersensitivity reactions.

Generic Availability:
NO

How Supplied:
Tabs—30