每日一次的三药合一口服组合药bictegravir/emtricitabine/tenofovir alafenamide(简称BIC/F/TAF,商品名Biktarvy)的艾滋病新药问世。 近日，美国FDA批准新药bictegravir/emtricitabine/tenofovir alafenamide三药单片口服组合（简称BIC/F/TAF，商品名Biktarvy）上市，作为每日一次的单片片剂疗法，治疗HIV-1感染（艾滋病）。 Biktarvy由bictegravir（50mg）、emtricitabine（200mg）、与tenofovir alafenamide（25mg）三种成分组成。Biktarvy是一款全新的无助推（unboosted）整合酶链转移抑制剂（INSTI）。 批准日期：2018年2月8日 公司：Gilead Sciences BIKTARVY®(bictegravir，恩曲他滨，和泰诺福韦[tenofovir]alafenamide)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30 mL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28 mg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 包装提供/存储和处理 剂型和强度 每种BIKTARVY片剂含有50mg的bictegravir（BIC）（相当于52.5mg bictegravir钠），200mg emtricitabine（FTC）和25mg替诺福韦艾拉酚胺（TAF）（相当于28mg替诺福韦艾拉酚胺延胡索酸盐）。 药片呈紫褐色，胶囊状，薄膜包衣，一面用“GSI”压印，另一面用“9883”压印。 存储和处理 BIKTARVY片剂呈紫褐色，胶囊形状，并且在一面沉积有“GSI”且另一面沉积有“9883”的薄膜。 每个瓶子含有30片（NDC 61958-2501-1），一种硅胶干燥剂，聚酯线圈，并用防儿童封闭物封闭。 每种BIKTARVY片剂含有50mg的bictegravir（BIC），200mg的emtricitabine（FTC）和25mg的替诺福韦艾拉酚胺（TAF）。 低于30°C（86°F）。 BIKTARVY(bictegravir, emtricitabine, and tenofovir alafenamide) Important U.S. Safety Information for Biktarvy BOXED WARNING: POST TREATMENT ACUTE EXACERBATION OF HEPATITIS B Severe acute exacerbations of hepatitis B have been reported in patients who are coinfected with HIV-1 and HBV and have discontinued products containing emtricitabine (FTC) and/or tenofovir disoproxil fumarate (TDF), and may occur with discontinuation of Biktarvy. Closely monitor hepatic function with both clinical and laboratory follow-up for at least several months in patients who are coinfected with HIV-1 and HBV and discontinue Biktarvy. If appropriate, anti-hepatitis B therapy may be warranted. Contraindications Coadministration: Do not use Biktarvy with dofetilide or rifampin. Warnings and precautions Drug interactions: See Contraindications and Drug Interactions sections. Consider the potential for drug interactions prior to and during Biktarvy therapy and monitor for adverse reactions. Immune reconstitution syndrome, including the occurrence of autoimmune disorders with variable time to onset, has been reported. New onset or worsening renal impairment: Cases of acute renal failure and Fanconi syndrome have been reported with the use of tenofovir prodrugs. In clinical trials of Biktarvy, there have been no cases of Fanconi syndrome or proximal renal tubulopathy (PRT). Do not initiate Biktarvy in patients with estimated creatinine clearance (CrCl) <30 mL/min. Patients with impaired renal function and/or taking nephrotoxic agents (including NSAIDs) are at increased risk of renal-related adverse reactions. Discontinue Biktarvy in patients who develop clinically significant decreases in renal function or evidence of Fanconi syndrome. Renal monitoring: Prior to or when initiating Biktarvy and during therapy, assess serum creatinine, CrCl, urine glucose, and urine protein in all patients as clinically appropriate. In patients with chronic kidney disease, also assess serum phosphorus. Lactic acidosis and severe hepatomegaly with steatosis: Fatal cases have been reported with the use of nucleoside analogs, including FTC and TDF. Discontinue Biktarvy if clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity develop, including hepatomegaly and steatosis in the absence of marked transaminase elevations. Adverse reactions Most common adverse reactions (incidence ≥5%; all grades) in clinical studies were diarrhea (6%), nausea (5%), and headache (5%). Drug interactions Prescribing information: Consult the full prescribing information for Biktarvy for more information on Contraindications, Warnings, and potentially significant drug interactions, including clinical comments. Enzymes/transporters: Drugs that induce P-gp or induce both CYP3A and UGT1A1 can substantially decrease the concentration of components of Biktarvy. Drugs that inhibit P-gp, BCRP, or inhibit both CYP3A and UGT1A1 may significantly increase the concentrations of components of Biktarvy. Biktarvy can increase the concentration of drugs that are substrates of OCT2 or MATE1. Drugs affecting renal function: Coadministration of Biktarvy with drugs that reduce renal function or compete for active tubular secretion may increase concentrations of FTC and tenofovir and the risk of adverse reactions. Dosage and administration Dosage: 1 tablet taken once daily with or without food. Renal impairment: Not recommended in patients with CrCl <30 mL/min. Hepatic impairment: Not recommended in patients with severe hepatic impairment. Prior to or when initiating: Test patients for HBV infection. Prior to or when initiating, and during treatment: As clinically appropriate, assess serum creatinine, CrCl, urine glucose, and urine protein in all patients. In patients with chronic kidney disease, assess serum phosphorus. Pregnancy and lactation Pregnancy: There is insufficient human data on the use of Biktarvy during pregnancy. An Antiretroviral Pregnancy Registry (APR) has been established. Available data from the APR for FTC shows no difference in the rates of birth defects compared with a US reference population. Lactation: Women infected with HIV-1 should be instructed not to breastfeed, due to the potential for HIV-1 transmission. About Gilead Sciences Gilead Sciences is a biopharmaceutical company that discovers, develops and commercializes innovative therapeutics in areas of unmet medical need. The company’s mission is to advance the care of patients suffering from life-threatening diseases. Gilead has operations in more than 35 countries worldwide, with headquarters in Foster City, California. For nearly 30 years, Gilead has been a leading innovator in the field of HIV, driving advances in treatment, prevention, testing and linkage to care, and cure research. Today, it’s estimated that more than 10 million people living with HIV globally receive antiretroviral therapy provided by Gilead or one of the company’s manufacturing partners. Forward-Looking Statement This press release includes forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995 that are subject to risks, uncertainties and other factors, including the risk that physicians may not see the benefits of prescribing Biktarvy and the possibility of unfavorable results from additional clinical trials involving Biktarvy. These risks, uncertainties and other factors could cause actual results to differ materially from those referred to in the forward-looking statements. The reader is cautioned not to rely on these forward-looking statements. These and other risks are described in detail in Gilead’s Quarterly Report on Form 10Q for the quarter ended September 30, 2017, as filed with the U.S. Securities and Exchange Commission. All forward-looking statements are based on information currently available to Gilead, and Gilead assumes no obligation to update any such forward-looking statements.