2018年5月25日，美国FDA批准了创新药Yonsa的上市申请。Yonsa是一种醋酸阿比特龙(abiraterone acetate)的创新药物配方，和甲泼尼龙(methylprednisolone)一起使用，用于治疗转移性去势抵抗性前列腺癌(mCRPC)患者。
前列腺癌是男性中最常见的癌症之一。通常前列腺癌生长缓慢，并且最初局限在前列腺中，但是某些类型的前列腺癌侵袭性很强，能够迅速转移。对于已经转移的前列腺癌，激素疗法是常见的治疗方法之一。因为前列腺癌细胞需要依靠雄性激素来帮助它们增生，切断雄性激素的供给会导致肿瘤细胞死亡或者延缓它们的生长。
醋酸阿比特龙正是一种抑制雄性激素合成的激素疗法。醋酸阿比特龙在体内会被转化成阿比特龙(abiraterone)，它是CYP17酶的抑制剂，CYP17酶在睾丸、肾上腺和前列腺癌组织中表达，是雄性激素生物合成必不可少的蛋白酶。
Yonsa的独特之处在于使用了Churchill公司的SoluMatrix Fine Particle Technology这一创新药物制造技术。这项技术将药物颗粒研磨成直径小于1微米的粉末，同时能够防止这些粉末重新聚集。使用这一技术生成的药物颗粒比传统药物颗粒小10-200倍，这大幅度增加了口服药物的可溶性和被人体吸收的效率。
用药方面，Yonsa可与或不与食物同服，只可吞服，不可压碎或咀嚼。
推荐用药剂量为：Yonsa 500mg(4片125mg)每日一次，配合每日2次口服甲泼尼龙4mg。
Yonsa(Abiraterone Acetate Tablets)
YONSA Rx
Generic Name and Formulations:
Abiraterone acetate 125mg; tabs.
Company:
Sun Pharmaceutical Industries
Indications for YONSA:
In combination with methylprednisolone for the treatment of metastatic castration-resistant prostate cancer (CRPC).
Adult:
Swallow whole with water. 500mg once daily (in combination with methylprednisolone 4mg twice daily). Also give concurrent GnRH analog or patient should have had bilateral orchiectomy. Baseline moderate hepatic impairment (Child-Pugh Class B): 125mg once daily; monitor closely; discontinue if ALT/AST >5xULN or total bilirubin >3xULN and do not re-treat. If concomitant strong CYP3A4 inducer necessary, increase abiraterone dose frequency to twice daily during co-administration period (eg, from 500mg once daily to 500mg twice daily); reduce back to previous dose/frequency when CYP3A4 inducer is discontinued.
Children:
Not established.
Contraindications:
Pregnancy.
Warnings/Precautions:
Not interchangeable with other abiraterone acetate products. Risk of mineralocorticoid excess; monitor BP, serum potassium, fluid retention at least monthly. Control hypertension and correct hypokalemia before and during treatment. Heart failure, recent MI, cardiovascular disease, ventricular arrhythmia; monitor closely. Monitor for adrenocortical insufficiency. Stress (may need higher corticosteroid dose). Monitor LFTs prior to starting treatment, every 2 weeks for the first 3 months, and monthly thereafter. Baseline moderate hepatic impairment (Child-Pugh Class B): monitor LFTs prior to initiation, weekly for the first month, every 2 weeks for the next 2 months, and monthly thereafter. Interrupt and reduce dose if hepatotoxicity (ALT/AST >5xULN or total bilirubin >3xULN) occurs; see full labeling. Permanently discontinue if concurrent ALT elevation >3xULN and total bilirubin >2xULN develops without biliary obstruction or other causes of elevation. Baseline severe hepatic impairment (Child-Pugh Class C): not recommended. Males with female partners of reproductive potential must use effective contraception during therapy and for 3 weeks after last dose. Nursing mothers: not for use in women.
Pharmacological Class:
CYP17 inhibitor.
Interactions:
Antagonized by strong CYP3A4 inducers (eg, phenytoin, carbamazepine, rifampin, rifabutin, rifapentin, phenobarbital); avoid (or see Adult). Potentiates CYP2D6 substrates (eg, dextromethorphan). Avoid concomitant CYP2D6 substrates with narrow therapeutic index (eg, thioridazine); if no alternatives, use caution and consider dose reduction of substrate. Concomitant CYP2C8 substrates with narrow therapeutic index (eg, pioglitazone): monitor closely for toxicity.
Adverse Reactions:
Fatigue, joint swelling/discomfort, edema, hot flush, diarrhea, vomiting, cough, hypertension, dyspnea, urinary tract infection, contusion, anemia, elevated LFTs, dyslipidemia, lymphopenia, hyperglycemia, hypophosphatemia, hypokalemia; hepatotoxicity (may be severe).
Generic Availability:
NO
How Supplied:
Tabs—120