每天服用1次的艾滋病药物Complera获FDA批准
日前, 美国食品药品管理局FDA批准了吉利德科学公司每天1次服用的艾滋病治疗药物Complera。
Complera 是鲁瓦达 (含有核苷类逆转录酶抑制剂恩曲他滨和替诺福韦) 和非核甘类逆转录酶抑制剂利匹韦林的复合制剂。鲁瓦达于2004年上市, 被称为是“艾滋病鸡尾酒疗法”, 利匹韦林是今年5月份获批准上市的。
Complera是治疗以前未接受其他艾滋病药物治疗的成人艾滋病感染一线药物, 每天一次用药从而, 增加了患者使用的依从性。不过, 与其他艾滋病药物一样,Complera 同样具有严重的副作用, 如乳酸酸中毒和严重肝损害。
Generic Name and Formulations:
Emtricitabine 200mg, tenofovir disoproxil fumarate 300mg, rilpivirine 25mg; tabs.
Company:
Gilead Sciences, Inc.
 
Select therapeutic use: Viral infections
Indications for COMPLERA:
As a complete regimen to treat HIV-1 infection in antiretroviral treatment-naive adults with HIV-1 RNA ≤100,000 copies/mL at the start of therapy and in certain virologically-suppressed (HIV-1 RNA <50 copies/mL) adults on a stable antiretroviral regimen at start of therapy in order to replace their current antiretroviral treatment regimen. See full labeling.

Adult:
Take with a meal. ≥12yrs (and ≥35kg): 1 tab once daily. After replacement: do additional monitoring of HIV-1 RNA to assess for potential virologic failure or rebound. Renal impairment (CrCl<50mL/min): not recommended. If concomitant with rifabutin regimen: take additional rilpivirine 25mg once daily.

Children:
<12yrs or <35kg: not established.

Contraindications:
Concomitant carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, rifapentine, esomeprazole, dexlansoprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole, systemic dexamethasone (more than single dose), St. John's wort.

Warnings/Precautions:
Risk of lactic acidosis or severe hepatomegaly with steatosis; suspend if occurs. Women, obesity, prolonged nucleoside exposure, other risk factors for hepatic dysfunction: increased risk of toxicity. Not for treating chronic hepatitis B; test for HBV before starting therapy and monitor patients coinfected with HIV-1 and HBV during and for several months after stopping treatment (discontinuing therapy may exacerbate HBV infection). Assess CrCl prior to initiating therapy in all patients. Monitor CrCl, serum phosphorus, urine glucose and protein prior to initiation and periodically during therapy in patients at risk for renal impairment. Discontinue immediately if severe skin or hypersensitivity reactions develop. Severe hepatic impairment. Increased risk of hepatotoxicity; monitor LFTs before and during therapy for all patients. May prolong QTc interval with supratherapeutic doses. History of bone fractures or other risks for osteoporosis or bone loss: monitor bone mineral density (BMD); consider Vit.D and calcium supplementation. Pregnancy (Cat.B). Nursing mothers: not recommended.

Interactions:
Avoid concomitant drugs that contain emtricitabine, tenofovir, lamivudine, or adefovir dipivoxil. Avoid concomitant or recent use of nephrotoxic agents. Tenofovir levels increased by concomitant ledipasvir/sofosbuvir; monitor for toxicity. Emtricitabine/tenofovir: monitor drugs that reduce renal function or compete for renal tubular secretion (eg, adefovir dipivoxil, cidofovir, acyclovir, valacyclovir, ganciclovir, valganciclovir, aminoglycosides, high-dose or multiple NSAIDs). Rilpivirine: potentiated by CYP3A inhibitors; antagonized by CYP3A inducers (see Contraindications). Rilpivirine levels decreased by concomitant rifabutin (see Adults). May antagonize azole antifungals (monitor for breakthrough fungal infections), methadone (monitor). May be potentiated by clarithromycin, erythromycin, telithromycin. Separate dosing of antacids by at least 2hrs before or at least 4hrs after rilpivirine; or H2-receptor antagonists by at least 12hrs before or 4hrs after rilpivirine; drugs that increase gastric pH may result in decreased plasma concentrations. Caution with drugs with a known risk for torsades de pointes.

Pharmacological Class:
Nucleoside analogue reverse transcriptase inhibitors + non-nucleoside reverse transcriptase inhibitor.

Adverse Reactions:
Depressive disorders, insomnia, headache, diarrhea, nausea, fatigue, dizziness, depression, abnormal dreams, rash; fat redistribution, immune reconstitution syndrome, lactic acidosis, severe hepatomegaly with steatosis, hepatotoxicity.

Generic Availability:
NO

How Supplied:
Tabs—30