近日，艾滋病新药Biktarvy是由bictegravir（50mg）、emtricitabine（200mg）、与tenofovir alafenamide（25mg）三种成分组成（简称BIC/F/TAF，商品名Biktarvy）,作为每日一次的单片片剂疗法，获FDA批准治疗HIV-1感染。
批准日期：2018年2月10日 公司：吉利德(Gilead Sciences)
BIKTARVY(bictegravir,emtricitabine,and tenofovir alafenamide)三药合一单片，为口服使用
美国初次批准: 2018
警告:
治疗后乙型肝炎的急性加重见完整处方资料对完整黑框警告见完整处方资料.
与 HIV-1和HBV共感染患者曽报道乙型肝炎的严重急性加重和曽终止含恩曲他滨(FTC)产品和/或泰诺福韦disoproxil富马酸盐(TDF)，和可能发生BIKTARVY的终止。如适宜在这些患者严密地监视肝功能。抗乙型肝炎治疗可能被允许.
作用机制
BIKTARVY是一种抗逆转录病毒药bictegravir(BIC)，恩曲他滨(FTC)，和泰诺福韦alafenamide(TAF)固定剂量组合[见微生物学]。
适应证和用途
BIKTARVY是一种bictegravir(BIC)，一种人免疫缺陷病毒类型1(HIV-1)整合酶的链转移抑制剂(INSTI)，和恩曲他滨[emtricitabine](FTC)和泰诺福韦alafenamide(TAF)，两者都是HIV-1核苷酸类似物逆转录酶抑制剂(NRTIs)的三-药组合，或取代当前抗逆转录病毒方案在患者是病毒学上被遏制的(HIV-1 RNA低于50拷贝每mL)用一个稳定的抗逆转录病毒方案共至少3个月与无治疗失败史和无已知取代伴随对BIKTARVY的个体组分抗性和被适用于作为一个完全方案为无抗逆转录病毒治疗史成年中HIV-1感染的治疗.
剂量和给药方法
测试:
BIKTARVY测试对乙型肝炎病毒感染前或当开始时。BIKTARVY前或开始时，和治疗期间，当临床上适用在所有患者中评估血清肌酐，估算肌酐清除率，尿糖，和尿蛋白。在有慢性肾病患者中，也评估血清磷。
推荐剂量: 一片服用每天1次有或无食物。
肾受损：在有估算的肌酐清除率低于30mL每分钟患者中不推荐BIKTARVY。
肝受损：在有严重肝受损患者中不推荐BIKTARVY。
剂型和规格
片: 50mg的bictegravir(等同于52.5mg的bictegravir钠)，200mg的恩曲他滨，和25mg泰诺福韦alafenamide(等同于28mg泰诺福韦alafenamide富马酸盐)。
禁忌症
BIKTARVY与下列两药禁忌共同给予：多非利特[dofetilide]和利福平[rifampin]。
警告和注意事项
免疫重建综合证：可能需要进一步评价和治疗。
肾受损的发作或变坏：所有患者，当开始和治疗期间当临床上适宜时评估血清肌酐，估算肌酐清除率。糖和尿蛋白。在有慢性肾病患者中还评估血清磷。
乳酸酸中毒/严重肝肿大有脂肪变性：在患者发生症状或实验室发现提示乳酸酸中毒或显著的肝毒性时终止治疗。
不良反应
最常见不良反应(发生率大于或等于5%，所有级别)为腹泻，恶心，和头痛。
药物相互作用
因为BIKTARVY是一个完整方案，不推荐为HIV-1感染与其他抗逆转录病毒药物共同给药。
对重要药物相互作用在治疗前和期间咨询完整处方资料。
在特殊人群中使用
哺乳：有HIV感染妇女应被指导不要哺乳由于传播HIV的潜能。

Biktarvy(bictegravir, emtricitabine, tenofovir alafenamide)
General Information
Biktarvy is a once daily single tablet regimen combining the novel, unboosted integrase strand transfer inhibitor (INSTI) bictegravir, with the demonstrated safety and efficacy profile of the Descovy (FTC/TAF) dual nucleoside reverse transcriptase inhibitor (NRTI) backbone.
Biktarvy is specifically indicated as a complete regimen for the treatment of HIV-1 infection in adults who have no antiretroviral treatment history or to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA <50 c/mL) on a stable antiretroviral regimen for at least three months with no history of treatment failure and no known substitutions associated with resistance to the individual components of Biktarvy.
Biktarvy is supplied as a tablet for oral administration. The recommended dose is one tablet once daily with or without food.
BIKTARVY Rx
Generic Name and Formulations:
Bictegravir 50mg, emtricitabine 200mg, tenofovir alafenamide 25mg; tabs.
Company:
Gilead Sciences, Inc.
Indications for BIKTARVY:
A complete regimen for the treatment of HIV-1 infection in adults with no antiretroviral treatment history or to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral regimen for ≥3 months with no history of treatment failure and no known substitutions associated with resistance to the individual components of Biktarvy.
Adult:
Test for HBV infection prior to initiation. 1 tab once daily.
Children:
<18yrs: not established.
Contraindications:
Concomitant dofetilide, rifampin.
Warnings/Precautions:
Test for HBV before starting therapy and closely monitor patients co-infected with HBV and HIV for several months after stopping treatment (discontinuing therapy may exacerbate HBV infection); if appropriate, anti-hepatitis B therapy may be warranted (esp. in those with advanced liver disease or cirrhosis). Suspend therapy if lactic acidosis or hepatotoxicity (eg, hepatomegaly, steatosis) occurs. Monitor serum creatinine, CrCl, urine glucose, urine protein, and serum phosphorus (in patients at risk for chronic renal disease); discontinue if significant renal dysfunction or Fanconi syndrome occurs. Severe renal impairment (CrCl <30mL/min): not recommended. Severe hepatic impairment (Child-Pugh Class C): not recommended. Pregnancy. Nursing mothers: not recommended.
Interactions:
See Contraindications. Concomitant other antiretrovirals: not recommended. May potentiate concomitant OCT2 and MATE1 substrates (eg, dofetilide). May be affected by drugs that induce or inhibit CYP3A and UGT1A1. Concomitant drugs that strongly affect P-gp and BCRP activity may lead to changes in TAF absorption. May be potentiated by drugs that decrease renal function or compete for active tubular secretion (eg, acyclovir, cidofovir, ganciclovir, valacyclovir, valganciclovir, aminoglycosides, NSAIDs). May be antagonized by anticonvulsants (eg, carbamazepine, oxcarbazepine, phenobarbital, phenytoin); consider alternatives. Concomitant rifabutin, rifapentine, St. John's wort: not recommended. Concomitant cation-containing antacids, laxatives, sucralfate, and buffered drugs: give Biktarvy 2hrs before. Concomitant oral iron/calcium supplements: may take together with food. Routine coadministration with, or 2hrs after, cation-containing antacids or oral iron/calcium supplements: not recommended. May potentiate metformin (refer to metformin labeling).
Pharmacological Class:
HIV-1 integrase strand transfer inhibitor (INSTI) + nucleoside analog reverse transcriptase inhibitors (NRTIs).
Adverse Reactions:
Diarrhea, nausea, headache; HBV exacerbation, new onset or worsening renal impairment, immune reconstitution syndrome, lactic acidosis, hepatomegaly.
Note:
Register pregnant patients in the Antiretroviral Pregnancy Registry (APR) by calling (800) 258-4263.
Generic Availability:
NO
How Supplied:
Tabs—30