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TARGRETIN胶囊
Generic Name for TARGRETIN
Bexarotene 75mg; caps.
Legal Classification:
Rx
Pharmacological Class for TARGRETIN
Retinoid.
Manufacturer of TARGRETIN
Eisai Pharmaceuticals
Indications for TARGRETIN
Cutaneous manifestations of cutaneous T-cell lymphoma in patients who are refractory to at least one prior systemic therapy.
Adult dose for TARGRETIN
Take with food. Initially 300mg/m2 once daily; may increase after 8 weeks to 400mg/m2 once daily if no tumor response and if well tolerated; monitor carefully. If toxicity occurs, reduce to 200mg/m2 then 100mg/m2 once daily, or suspend therapy.
Children's dosing for TARGRETIN
Not recommended.
Contraindications for TARGRETIN
Pregnancy (Cat.X).
Warnings/Precautions for TARGRETIN
Be fully familiar with this drug's toxicity before use. Pancreatitis or risk of pancreatitis (eg, history of pancreatitis, uncontrolled hyperlipidemia, excess alcohol consumption, uncontrolled diabetes, biliary tract disease, drugs that can cause pancreatitis). Counsel patients monthly about need for contraception. Women of childbearing potential: obtain reliable negative pregnancy test within 1 week of start; repeat monthly. Start therapy on 2nd or 3rd day of normal menstrual period. Use two effective forms of contraception 1 month prior to, during, and for 1 month after therapy. Max 1 month/℞. Men with partners who are or may become pregnant: use condoms during and for at least 1 month after therapy. Monitor lipids before treatment, weekly until stable, then every 8 weeks; try to keep triglycerides <400mg/dL; treat hyperlipidemia, or reduce or suspend bexarotene if needed. Hepatic or renal insufficiency. Monitor liver function at baseline, 1, 2, and 4 weeks after start, then (if stable) at least every 8 weeks during therapy; consider suspending or discontinuing treatment if SGOT/AST, SGPT/ALT, or bilirubin >3xULN occurs. Monitor WBC with differential and thyroid function at baseline and during treatment; treat hypothyroidism if needed. Avoid sun and UV light. Nursing mothers: not recommended.
Interactions for TARGRETIN
Concomitant gemfibrozil: not recommended. Levels may be increased by CYP3A4 inhibitors (eg, ketoconazole, itraconazole, erythromycin, grapefruit juice). Levels may be reduced by CYP3A4 inducers (eg, rifampin, phenobarbital, phenytoin). May potentiate antihyperglycemics (eg, insulin, sulfonylureas, thiazolidinediones); monitor. May potentiate or be potentiated by protein-bound drugs. May antagonize tamoxifen, hormonal contraceptives, other CYP3A4 substrates. Limit Vit. A supplements to avoid toxicity. May increase CA125 assay values.
Adverse Reactions for TARGRETIN
Lipid abnormalities, headache, hypothyroidism, asthenia, leukopenia, anemia, rash, GI disturbances, peripheral edema, dry skin, exfoliative dermatitis, alopecia, insomnia, fatigue, abnormal liver function tests, pancreatitis, pruritus, photosensitivity.
How is TARGRETIN supplied?
Caps—100
Related Disease:
Lymphoma, cutaneous T-cell
国外临床研究和使用情况
①．贝沙罗汀软胶囊的临床疗效
在第一项研究中，对至少两种治疗方法无反应或不能耐受的早期皮肤T-细胞淋巴瘤病人服用本品一日300mg/m2后，28例病人中有15例（54%）获得全部或部分反应（改善至少达50%以上），而更高剂量组反应率为10例/15例（67%），此外，一日300mg/m2组中有2例病人在25周内复发。
在第二项研究中，94例至少一种全身性治疗方法无效的晚期皮肤T-细胞淋巴瘤病人中，56例接受本品一日300mg/m2后有25例（45%）获得反应，另外35例接受较高剂量本品，有21例（55%）获得反应；低剂量组有反应的病人中有9例经中位时间19周复发。
在研究中，共有84例病人接受本品一日300mg/m2，其中3例（4%）获得完全反应，40例（48%）获得部分反应；在高剂量组中，完全反应率为9例/53例（17%）。
贝沙罗汀软胶囊作为生物活性制剂与化疗药物联合应用前景看好。
目前，美国Ligand制药公司正在进行试验评价贝沙罗汀与传统化疗药在非小细胞肺癌中的疗效。
另外，贝沙罗汀对恶性细胞株有诱导凋亡作用，在化学预防中起作用，目前正在验证贝沙罗汀在肺癌中的预防和治疗作用。
43例Ⅳ期肺癌病人联合服用贝沙罗汀、顺铂、长春瑞宾合计400mg/m2/day，18.6%d的病人获得反应。
该药对乳腺癌、牛皮癣等症状的Ⅱ、Ⅲ期临床试验。该药已被列为正在开发中的治疗牛皮癣的新药。
148例晚期乳腺癌病人（多中心研究）服用本品200mg/m2/day，经8-10周所有病人均获得反应。
50例中-重度牛皮癣病人（多中心研究）服用本品35-240mg/m2/day，经12-24周治疗，有46%的病人有>50%的改善。
②．贝沙罗汀凝胶的临床疗效：
贝沙罗汀凝胶用于治疗早期的或对其他治疗方法无反应或不能耐受的皮肤T-细胞淋巴瘤病人：在一项67名CTCL病人参加的Ⅰ/Ⅱ期临床研究中，局部应用贝沙罗汀凝胶至少4周，63％（42名）的病人显示有效，50％病人临床症状得到改善。21％病人（13名）完全显效。局部皮肤损害得到中等程度的改善一般在给药开始后24周，包括红斑、斑块隆起、脱屑以及瘙痒。给药起效的中位时间为20周（范围为4-86周）。平均治疗时间为315天，接受治疗的最长时间为4.25年且尚在治疗中。疗效持续的中位时间为428天，最短的为2个月，范围为57-428天。给予病人治疗浓度的1％贝沙罗汀凝胶，87％的病人（58名）显示出对其有良好的局部耐受性。副作用主要发生在使用部位，而且轻微。包括皮疹（73%），瘙痒（33%），疼（在应用部位的烧灼感24%），没有严重的副作用产生。
一项Ⅲ期临床试验（多中心），美国50例难治性早期皮肤T-细胞淋巴瘤患者，贝沙罗汀凝胶的有效率是44%（8%获完全有效）。中期治疗时间165天，最长治疗687天。副作用包括皮疹（72%），瘙痒（32%），在应用部位疼（22%），皮肤失调（16%），接触性皮（12%）。
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产地国家: 美国
原产地英文商品名:
TARGRETIN
原产地英文药品名:
bexarotene capsules
包装规格: 75毫克/胶囊, 100胶囊/瓶
中文参考商品译名:
塔革雷汀 贝沙罗汀软胶囊
生产厂家英文名:
Ligand Pharmaceuticals | 
