Generic Name and Formulations:
Telaprevir 375mg; tabs.

Company:
Vertex Pharmaceuticals

Indications for INCIVEK:
Chronic hepatitis C genotype 1 infection, in combination with peginterferon alfa and ribavirin in patients with compensated liver disease, including cirrhosis, who are treatment-naïve or who have previously been treated with interferon-based therapy, including prior null responders, partial responders, and relapsers. Not for use as monotherapy.

Adult Dose for INCIVEK:
Take with food (not low fat). 750mg three times daily. Treat for 12 weeks (with peginterferon + ribavirin), then continue peginterferon + ribavirin according to HCV-RNA response at Weeks 4 and 12. Do not reduce dose or interrupt therapy. Discontinue if futile (see full labeling).

Children's Dose for INCIVEK:
≤18yrs: not established.

Pharmacological Class:
Hepatitis C virus NS3/4A protease inhibitor.

Contraindications:
Concomitant strong CYP3A inducers (eg, rifampin, St. John’s wort), or narrow therapeutic index CYP3A substrates (eg, alfuzosin, cisapride, ergots, lovastatin, pimozide, simvastatin, sildenafil/tadalafil for PAH, triazolam, oral midazolam). Pregnant women, or partners. Review peginterferon and ribavirin contraindications.

Warnings/Precautions:
Must have (–) pregnancy test before therapy, use 2 effective forms of contraception, and undergo monthly pregnancy test during treatment and for 6 months after. Risk of serious skin reactions (eg, Stevens-Johnson syndrome, DRESS, TEN); monitor. Moderate/severe hepatic impairment, decompensated liver disease: not recommended. Coinfection with HBV or HIV. Organ transplant recipients. Monitor hemoglobin and CBC with differential prior to and at weeks 2, 4, 8 and 12 during treatment. Monitor HCV-RNA at weeks 4 and 12, and clinical chemistry frequently. Elderly. Pregnancy (Cat. B). Nursing mothers: not recommended.

Interactions:
See Contraindications. Avoid concomitant atorvastatin. Concomitant colchicine w/renal or hepatic impairment, voriconazole; lopinavir, fosamprenavir, darunavir (all w/ritonavir): not recommended. May be potentiated by macrolides, azole antifungals. May be antagonized by anticonvulsants, rifabutin, dexamethasone, HIV protease inhibitors, efavirenz. May potentiate antiarrhythmics, digoxin, macrolides, carbamazepine, trazodone, azole antifungals, colchicine, rifabutin, alprazolam, midazolam, calcium channel blockers, corticosteroids, bosentan, atazanavir, tenofovir, immunosuppressants, salmeterol, PDE5 inhibitors for ED (reduce dose). May antagonize escitalopram, zolpidem, efavirenz, ethinyl estradiol, methadone. Monitor warfarin.

Adverse Reactions:
Rash (if serious; discontinue therapy and treat, do not restart), pruritus, anemia, GI upset, anorectal effects, dysgeusia, fatigue, hyperbilirubinemia, hyperuricemia.

Metabolism:
Hepatic (CYP3A4).

Elimination:
Fecal, renal.

Generic Availability:
NO

How Supplied:
Tabs—168 (7 blister strips x 6 tabs/ blister strip x 4 weekly cartons
2011年Vertex/强生的蛋白酶抑制剂特拉瑞韦（Incivek，telaprevir）相继在美国和欧盟获批上市。从已公布的Ⅲ期临床数据看来，特拉瑞韦治疗丙肝病毒感染疗效更具优势，特拉瑞韦与现行标准治疗药物合用，治愈率可达79。此外，特拉瑞韦在剂量方案和先前无应答患者治愈率方面也具有优势。
由于特拉瑞韦较高的治愈率并且给药方式快捷简单，上市后销售额屡破新高，在去年的5~10月，该药已实现销售额4.2亿美元，上市第一年即有可能达到“重磅炸弹”级地位。有如此好表现的抗病毒药前所未见，即使与业内其他“重磅炸弹”级药物相比，第一年就有如此业绩的也很少见。