2010年6月22日，美国食品及药物管理局（FDA）已经批准由0.5 mg度他雄胺和0.4 mg坦索罗辛（Jalyn；葛兰素史克）组成的单胶囊药物，用于治疗良性前列腺增生症（BPH），这一处方药物预计可与2010年下半年上市。

BPH是一进展性疾病， 50岁以上的男性将近一半患有此病，而在80岁以上的男性中超过90%的人有此病痛。常见的尿路症状分为尿路刺激性症状（尿频，尿急，夜尿增多），或者梗阻性症状（尿等待，尿残余，尿中断和尿线无力）。

度他雄胺（Avodart，葛兰素史克）是一种5-&alPHa;还原酶抑制剂，用于治疗良性前列腺增生症，长时间应用后，其能够减小前列腺体积；它目前被FDA批准用于降低急性尿潴留的风险和前列腺相关的外科手术。坦索罗辛（Flomax；由Astellas 制药厂生产，Boehringer Ingelheim 公司销售）是一种α1肾上腺素受体阻滞剂，能够松弛膀胱和前列腺肌肉，从而治疗良性前列腺增生所引起的症状。
作为葛兰素史克公司的副总裁和医药研究发展负责人的安尼•菲利普斯博士，在公司新闻发布会上说：“这是第一次这些治疗能够通过每日一次一粒胶囊而实现，Jalyn在持续一段时间应用后，为改善症状和缩小前列腺体积提供了两种途径。”

FDA批准此药是建立在，结合了2年的Avodart研究数据和4年的坦索罗辛研究的资料基础之上的，这些研究包括4884名50岁以上血清前列腺特异性抗原水平在1.5 ng/mL至10 ng/mL的男性，且最大尿流率在5 mL/秒和15 mL/秒之间，最低排尿量125 mL，国际前列腺症状评分在12分以上与中度至重度良性前列腺增生症症状结合分析。

初步研究结果显示，每日联合应用0.5 mg度他雄胺和0.4 mg坦索罗辛要比单独应用其中一种药物明显减轻BPH症状。比较研究是建立在国际前列腺症状量表基线中点的改变（平均值，−6.2对 −4.9和−4.3；两者均P < .001），这种不同之处是通过9个月内观察到的并持续至24个月。

第二方面，度他雄胺/坦索罗辛结合与单独应用其中一种药物相比，明显提高了最大尿流率（平均值2.4 mL/秒对1.9 mL/秒和0.9 mL/秒，P = .003 和P < .0001 ），这种变化在6个月内观察到并持续至24个月。

研究发现的副作用与已知的度他雄胺和坦索罗辛的安全情况相一致，最常见的包括性功能障碍，性欲下降，乳腺疾病（包括乳腺增大和胀痛），射精障碍和头晕。
度他雄胺/坦索罗辛的推荐剂量是单药0.5 mg/0.4 mg胶囊，每天同一餐后约30分钟服用。药物相互作用，不能同时应用细胞色素P 450的同工酶3A4（CYP 3A4）的强抑制剂，如酮康唑。

警告提出，应慎重应用中等剂量的CYP 3A4抑制剂，强或中等的CYP 2D6抑制剂，或者华法令，或患者对CYP 2D6代谢较差时。因为度他雄胺/坦索罗辛能够降低血清总的前列腺特异性抗原浓度的50%，当患者在治疗时出现前列腺特异性抗原升高，应该评估发生前列腺癌的可能性。和其他α-1受体阻滞剂一样，坦索罗辛能引起体位性低血压，头晕，眩晕。患者应当心避免发生晕厥而受伤情况的发生。当同时使用其他的α-受体阻滞剂或5磷酸二酯酶抑制剂时，应避免增加低血压症状发生的风险。

临床意义
FDA已经批准由0.5 mg度他雄胺和0.4 mg坦索罗辛组成的单胶囊药物，用于治疗男性良性前列腺增生症，度他雄胺和坦索罗辛都为治疗BPH尿路症状的药物。度他雄胺/坦索罗辛的推荐剂量是单药0.5 mg/0.4 mg胶囊，每天同一餐后约30分钟服用，这一药物应避免同时应用CYP 3A4强抑制剂，其他α-受体阻滞剂或者5磷酸二酯酶抑制剂。度他雄胺/坦索罗辛治疗中相关的副作用包括性功能障碍，性欲降低，乳腺疾病，射精障碍和头晕，度他雄胺/坦索罗辛可能会增加伤害胎儿的风险，因此，应避免怀孕或打算怀孕女性接触此药。

制造商：
葛兰素史克制药公司

类药物：
I及II型5α-还原酶抑制剂+α1A受体阻滞剂。

活性成分（补）：
度他雄胺为0.5mg，盐酸坦索罗辛0.4mg;上限。

适应症（补）：
良性前列腺增生症（BPH）。

FDA Approves Dutasteride/Tamsulosin Combo Pill for Benign Prostatic Hyperplasia
June 18, 2010 (UPDATED June 21, 2010) — The US Food and Drug Administration (FDA) has approved a single-capsule formulation of 0.5-mg dutasteride and 0.4-mg tamsulosin (Jalyn; GlaxoSmithKline) for symptomatic benign prostatic hyperplasia (BPH) in men with an enlarged prostate. The prescription product is expected to be available during the second half of 2010.
 
BPH is a progressive disease that affects nearly half of all men aged 50 years and older, and more than 90% of those older than 80 years. Common urinary symptoms are classified as irritative (frequency, urgency, and nocturia) or obstructive (hesitancy, incomplete emptying, intermittency, and weak stream).
 
Dutasteride (Avodart; GlaxoSmithKline) is a 5-α-reductase inhibitor that treats BPH symptoms and can shrink the prostate over time; it is currently approved by the FDA to reduce the risk for acute urinary retention and prostate-related surgery. Tamsulosin (Flomax; Astellas Pharma, Inc, marketed by Boehringer Ingelheim) is an alpha1a-adrenergic blocker that relaxes bladder and prostate muscles and is indicated for the symptomatic treatment of BPH.
 
"This is the first time these therapies will be available together in a once-daily capsule," said Anne Phillips, MD, vice president, R&D Medicine Development Leader, GlaxoSmithKline, in a company news release. "Jalyn offers two mechanisms of action to provide symptom improvement and the ability shrink the prostate over a sustained time."
 
FDA approval was based on 2-year data from the Combination of Avodart and Tamsulosin 4-year study of 4884 men aged 50 years and older with a serum prostate-specific antigen level of 1.5 to 10 ng/mL; maximal urinary flow rate (Qmax) ranging from more than 5 mL/second to 15 mL/second with a minimum voided volume of 125 mL; and International Prostate Symptom scores of 12 or higher associated with moderate to severe BPH symptoms.
 
Primary results showed that daily use of the drug combination yielded significantly greater relief of BPH symptoms compared with either 0.5 mg dutasteride or 0.4 mg tamsulosin alone, as measured by point changes on the International Prostate Symptom scale from baseline (mean Δ, −6.2 vs −4.9 and −4.3; P < .001 for both). The difference was observed by month 9 and continued through month 24.
 
On secondary endpoints, dutasteride–tamsulosin was shown to significantly improve maximal urinary flow rate from baseline compared with either drug alone (mean Δ Qmax, 2.4 mL/second vs 1.9 mL/second and 0.9 mL/second; P = .003 and P < .0001, respectively) — a difference that was observed by month 6 and continued through month 24.
 
Adverse events reported in the study were consistent with the known safety profiles of dutasteride and tamsulosin and most commonly included impotence, decreased libido, breast disorders (including enlargement and tenderness), ejaculation disorders, and dizziness.
 
The recommended dose of dutasteride–tamsulosin is a single 0.5 mg/0.4 mg capsule taken approximately 30 minutes after the same meal each day. The combination drug should not be used with strong inhibitors of cytochrome P 450 isoenzyme 3A4 (CYP 3A4) such as ketoconazole. Caution is advised when using moderate CYP 3A4 inhibitors, strong/moderate CYP 2D6 inhibitors, or warfarin, or when treating patients known to be poor metabolizers of CYP 2D6.
 
Because dutasteride–tamsulosin decreases total serum prostate-specific antigen concentrations by about 50%, patients with increased prostate-specific antigen levels during therapy should be evaluated for the presence of prostate cancer.
 
As with other alpha-1 blockers, tamsulosin may cause postural hypotension, dizziness, and vertigo. Patients should be cautioned to avoid situations in which syncope could result in injury. Concomitant treatment with other alpha-blockers or phosphodiesterase type 5 inhibitors should be avoided because of the increased risk for symptomatic hypotension.
 
Patients should also be advised that alpha-1 blockers, including tamsulosin, have been associated with a risk for priapism and rare reports of intraoperative floppy iris syndrome during cataract surgery.
 
Dutasteride–tamsulosin capsules should not be handled by women who are, or may become, pregnant. Dutasteride is absorbed through the skin and could result in unintended fetal exposure, potentially inhibiting the normal development of external male genitalia. To protect pregnant women from transfusion-related exposure, men receiving dutasteride should not donate blood until 6 months after termination of therapy.

Jalyn approved for benign prostatic hyperplasia (BPH)