Stivarga (Regorafenib Tablets)

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Stivarga获准治疗晚期胃肠道间质瘤
STIVARGA (regorafenib) 40mg tablets by Onyx and Bayer HealthCare The FDA has expanded the approved use of Stivarga (regorafenib; Bayer Healthcare) to treat patients with advanced gastrointestinal stromal tumors (GIST) that cannot be surgically removed and no longer respond to Gleevec (imatinib; Novartis) and Sutent (sunitinib; Pfizer).

The safety and efficacy of Stivarga for this use were evaluated in a clinical study of 199 patients with GIST that could not be surgically removed and progressed after treatment with Gleevec or Sutent. Patients were randomized to Stivarga or placebo. Results showed patients who took Stivarga had a delay in tumor growth (progression-free survival) that was, on average, 3.9 months later than patients who were given placebo.

Stivarga is a kinase inhibitor already indicated for the treatment of patients with metastatic colorectal cancer (CRC) who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, an anti-EGFR therapy.

Generic Name and Formulations:
Regorafenib 40mg; tablets.

Company:
Bayer Healthcare Pharmaceuticals Inc.
RECENT UPDATES
04/05/13
GIST indication added

Indications for STIVARGA:
Treatment of patients with metastatic colorectal cancer who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, an anti-EGFR therapy. Treatment of patients with locally advanced, unresectable or metastatic gastrointestinal stromal tumor (GIST) who have been previously treated with imatinib mesylate or sunitinib malate.

Adult Dose for STIVARGA:
Swallow whole with a low-fat breakfast (contains <30% fat). 160mg once daily for the first 21 days of each 28-day cycle; until disease progression or unacceptable toxicity. Dose modifications: see full prescribing information.

Children's Dose for STIVARGA:
<18yrs: not established.

Pharmacological Class:
Kinase inhibitor.

Warnings/Precautions:
Risk of severe hepatotoxicity (may be fatal). Monitor hepatic function before starting and at least every 2 weeks during first 2 months of treatment; interrupt and reduce or discontinue if hepatotoxicity or hepatocellular necrosis occurs. Severe hepatic impairment: not recommended. Increased risk of hemorrhage; permanently discontinue if severe or life-threatening. Interrupt and reduce or permanently discontinue if dermatological toxicity occurs (eg, hand-foot skin reaction [a.k.a. palmar-plantar erythrodysesthesia], rash). Ensure BP is controlled before starting; monitor weekly for the first 6 weeks then every cycle or as clinically indicated; withhold if severe or uncontrolled. Myocardial ischemia/infarction: withhold if new or acute onset develops; resume when resolved. Discontinue if reversible posterior leukoencephalopathy syndrome or GI perforation/fistula develops. Wound healing complications: stop treatment at least 2 weeks before surgery; discontinue if wound dehiscence occurs. Fetal toxicity. Pregnancy (Category D); use effective contraception during treatment and up to 2 months after completion. Nursing mothers: not recommended.

Interactions:
Avoid concomitant strong CYP3A4 inducers (eg, rifampin, phenytoin, carbamazepine, phenobarbital, St. John’s Wort). Avoid concomitant strong CYP3A4 inhibitors (eg, clarithromycin, grapefruit juice, itraconazole, ketoconazole, posaconazole, telithromycin, voriconazole). Monitor INR levels with concomitant warfarin.

Adverse Reactions:
Asthenia/fatigue, decreased appetite and food intake, hand-foot skin reaction, diarrhea, mucositis, weight loss, infection, hypertension, dysphonia, GI and abdominal pain, rash, fever, nausea; hepatotoxicity, hemorrhage, GI perforation.

Metabolism:
Hepatic (CYP3A4, UGT1A9); 99.5% protein bound.

Elimination:
Fecal (major), renal.

Generic Availability:
NO

How Supplied:
Tabs—84 (3 x 28)
2013年2月25日，美国食品药品管理局(FDA)宣布，已批准Stivarga(regorafenib，瑞格非尼)用于治疗不能手术切除且对格列卫(伊马替尼)和索坦(舒尼替尼)治疗无应答的晚期胃肠道间质瘤(GIST)。后两者是FDA已批准的另外2种治疗GIST的药物。Stivarga是一种多种激酶抑制剂，已于2012年9月获准用于结直肠癌治疗。
    一项纳入199例不能手术切除且在格列卫或索坦治疗后出现进展的GITS患者的临床研究中评价了Stivarga新适应症的有效性和安全性。患者被随机分入Stivarga组或安慰机组，所有患者还接受最佳支持性治疗。受试者在出现癌症进展或不能耐受的不良反应之前，一直接受Stivarga治疗或安慰剂。结果显示，与安慰机组相比，Stivarga组患者无进展生存期平均延长3.9个月。安慰机组患者一旦癌症出现进展，可转为Stivarga治疗。
接受Stivarga治疗的患者最常见不良反应包括虚弱、乏力、手足综合征、腹泻、食欲下降、高血压、口腔溃疡、感染、音量或音质改变、疼痛、体重下降、腹痛、皮疹、发热以及恶心。
严重不良反应包括肝损伤、严重出血、皮肤起泡和脱皮、需要急诊治疗的严重高血压、心肌梗死和肠穿孔。