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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

FDA approves Tivicay for HIV-1
HealthDay News -- The FDA has approved dolutegravir (Tivicay, GlaxoSmithKline) to treat HIV-1 infection in combination with other antiretroviral drugs.
“HIV-infected individuals require treatment regimens personalized to fit their condition and their needs,” said Edward Cox, MD, MPH, director of the Office of Antimicrobial Products in the FDA's Center for Drug Evaluation and Research. “The approval of new drugs like dolutegravir that add to the existing options remains a priority for the FDA.”
Some 50,000 Americans acquire HIV infection each year, and about 15,500 people died from the disease in 2010, CDC data indicate.
Dolutegravir belongs to a class of medications called integrase strand transfer inhibitors, which interfere with an enzyme that HIV needs to multiply. It is specifically indicated in treatment-naïve and in treatment-experienced adults, including those who have been treated with other integrase strand transfer inhibitors. Dolutegravir is also approved in children >12 years weighing >40kg who are treatment-naïve or treatment-experienced but have not previously taken other integrase strand transfer inhibitors.
Dolutegravir's approval was based on safety and effectiveness data from clinical studies involving 2,539 adults and children. Study results showed that dolutegravir-containing regimens were effective in viral load reduction.
A fifth trial established the pharmacokinetics, safety and activity of the drug as part of treatment regimens in children >12 years old weighing >40kg who have not previously taken integrase strand transfer inhibitors.
The most common side effects included difficulty sleeping and headache as well as more serious problems, including allergic-like reactions and abnormal liver function in people with hepatitis B or C.
TIVICAY Rx
Pharmacological Class:
HIV-1 integrase strand transfer inhibitor (INSTI).

Active Ingredient(s):
Dolutegravir 50mg; tablets.

Company
ViiV Healthcare
Indication(s):
In combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and children ≥12 years and ≥40kg.

Pharmacology:
Dolutegravir inhibits HIV-1 integrase by binding to the integrase active site and blocking the strand transfer step of retroviral deoxyribonucleic acid (DNA) integration which is essential for the HIV replication cycle.

Clinical Trials:
The efficacy of Tivicay was based on analyses of data from two trials, SPRING-2 and SINGLE, in treatment-naïve, HIV-1-infected subjects (n=1,641); one trial, SAILING, in treatment-experienced, INSTI-naïve HIV-1-infected subjects (n=715); and from VIKING-3 trial in INSTI-­experienced ­HIV-1-infected subjects (n=183) with virological failure and current or historical evidence of raltegravir and/or elvitegravir resistance.

In the SPRING-2 trial, once-daily Tivicay versus twice-daily raltegravir in 822 HIV-infected, treatment-naïve patients, both in combination with a fixed-dose dual-NRTI treatment were evaluated. At week 48, the proportion of subjects who were virologically suppressed (HIV-1 RNA <50 copies/mL) was 88% for the regimen containing Tivicay and 86% for the regimen containing raltegravir, meeting the 10% non-inferiority criteria.

In the SINGLE trial, once-daily Tivicay plus fixed-dose Epzicom versus the fixed-dose Atripla regimen in 833 HIV-infected, treatment-naïve patients were evaluated. At 48 weeks, the proportion of subjects who were virologically suppressed (HIV-1 RNA <50 copies/mL) was 88% for Tivicay regimen and 81% for Atripla which was statistically significant.

For more information on clinical trials, see full labeling.


Legal Classification:
Rx

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

Contraindication(s):
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 (Category B). Nursing mothers: not recommended.

Interaction(s)
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 Reaction(s)
Insomnia, headache; immune reconstitution syndrome, lab abnormalities.

How Supplied:
Tabs—30

LAST UPDATED:
8/30/2013

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