Osphena(ospemifene)是一种性交痛（性交）的口服处方药。于2013年2月26日获FDA批准的治疗性生活疼痛(dyspareunia)药物，主要针对绝经后阴道萎缩的妇女。商品名Osphena,开发商Shionogi Inc。
Osphena (ospemifene) is an estrogen agonist/antagonist with tissue selective effects. It binds to estrogen receptors, resulting in the activation of estrogenic pathways in some tissues and the blockade of estrogenic pathways in other tissues.
Osphena is specifically indicated for the treatment of moderate to severe dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause.
Osphena is supplied as a tablet for oral administration. The recommended dose is one 60 mg tablet with food once daily. Use of Osphena should be for the shortest duration consistent with treatment goals and risks. For postmenopausal woman with a uterus, the addition of a progestin should be considered to reduce the risk of endometrial cancer. A woman without a uterus does not need a progestin.
Generic Name: ospemifene
Dosage Form: tablet, film coated
Medication Class: Selective Estrogen Receptor Modulator
FDA Approval Date: February 2013
Pharmacological Class:
Estrogen (agonist/antagonist).

Active Ingredient(s):
Ospemifene 60mg; tabs.
Company
Shionogi, Inc.
Indication(s):
Treatment of moderate-to-severe dyspareunia due to menopause.
Pharmacology:
The mechanism of action of Ospemifene is mediated through binding to estrogen receptors. This binding results in activation of estrogenic pathways in some tissues (agonism) and blockade of estrogenic pathways in others (antagonism).
Clinical Trials:
The safety and effectiveness of Osphena on moderate-to-severe symptoms of vulvar and vaginal atrophy in postmenopausal women were assessed in three placebo-controlled clinical trials.
The first trial was a 12-week, randomized, double-blind, placebo-controlled, parallel-group study that enrolled 826 postmenopausal women (41–81 years old) who at baseline had ≤5% superficial cells on a vaginal smear, a vaginal pH >5.0, and who identified at least one moderate-to-severe vaginal symptom that was considered the most bothersome to her (vaginal dryness, pain during intercourse [dyspareunia], or vaginal irritation/itching). Treatment groups included Osphena 30mg (n=282), Osphena 60mg (n=276), and placebo (n=268). Improvement in the mean change from baseline to Week 12 was assessed for the co-primary efficacy variables of the most bothersome symptom (MBS) of vulvar and vaginal atrophy (defined as the individual moderate-to-severe symptom that was identified by the woman as most bothersome at baseline), percentage of vaginal superficial and vaginal parabasal cells on a vaginal smear, and vaginal pH. Following completion of 12-weeks, women with an intact uterus were allowed to enroll in a 40-week double-blind extension study, and women without an intact uterus were allowed to enroll in a 52-week open-label extension study.
The second trial was a 12-week, randomized, double-blind, placebo-controlled, parallel-group study that enrolled 919 postmenopausal women (41–79 years old) who at baseline had ≤5% superficial cells on a vaginal smear, a vaginal pH >5.0, and who identified either moderate-to-severe vaginal dryness (dryness cohort) or moderate-to-severe dyspareunia (dyspareunia cohort) as most bothersome to her at baseline. Treatment groups included Osphena 60mg (n=463) and placebo (n=456). Primary endpoints were similar to those in Trial 1.
The third trial was a 52-week, randomized, double-blind, placebo-controlled, long-term safety study that enrolled 426 postmenopausal women (49–79 years old) with an intact uterus. Treatment groups included Osphena 60mg (n=363) and placebo (n=63).
In the first and second trial, the modified intent-to-treat population of women treated with Osphena demonstrated a statistically significant improvement (least square mean change from baseline to Week 12) in moderate-to-severe bothersome symptoms (MBS) of dyspareunia (Trial 1: [-1.39 (0.11); P=0.0012]; Trial 2: [-1.55 (0.06); P<0.0001] when compared to placebo. A statistically significant increase in the proportion of superficial cells and a corresponding statistically significant decrease in the proportion of parabasal cells on a vaginal smear was also demonstrated (P <0.0001 for both). The mean reduction in vaginal pH between baseline and Week 12 was also statistically significant (P <0.0001).
Legal Classification:
Rx
Adults:
60mg once daily with food.
Children:
Not studied.
Contraindication(s):
Undiagnosed abnormal genital bleeding. Known or suspected estrogen-dependent neoplasia. Active DVT, pulmonary embolism, or history of. Active arterial thromboembolism (eg, stroke, MI, or history of). Known or suspected pregnancy (Category X).
Warnings/Precautions:
Use for shortest duration consistent with treatment goals and risks. Increased risk of cardiovascular disorders, arterial vascular disease, and/or venous thromboembolism. Discontinue if thromboembolic or hemorrhagic stroke is suspected or occur. Discontinue at least 4–6 weeks before surgery type associated with increased risk of thromboembolism or during prolonged immobilization. Increased risk of endometrial cancer. Consider the addition of a progestin in patients with an intact uterus to reduce endometrial hyperplasia risk. Known, suspected, or history of breast cancer: do not use. Severe hepatic impairment: not recommended. Reeva luate periodically. Nursing mothers.
Interaction(s)
Avoid concomitant other estrogens or estrogen agonists/antagonists. Antagonized by rifampin. Potentiated by fluconazole (avoid), ketoconazole. May affect or be affected by highly protein-bound drugs. May increase risk of adverse reactions with concomitant CYP3A4 and CYP2C9 inhibitors.
Adverse Reaction(s)
Hot flush, vaginal or genital discharge, muscle spasms, hyperhidrosis.
How Supplied:
Tabs—100
Blister pack—30 (2 X 15)
LAST UPDATED:
7/22/2013
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8462d6ab-e3cd-4efa-a360-75bf8f917287
FDA批准奥培米芬Osphena(ospemifene)治疗女性性交痛
2013年2月26日，美国食品与药物管理局（FDA）批准了奥培米芬(通用名ospemifene)用于治疗女性中至重度性交困难的患者，以缓解一些女性因绝经激素水平下降导致的外阴和阴道内萎缩。
奥培米芬为每日餐时服用一次的药片，在阴道组织发挥类似激素的作用。它是一种新型的选择性雌激素受体调节剂，可使阴道组织较厚和不太脆弱，使得妇女的性交疼痛次数减少。
纳入1889例有外阴和阴道萎缩的绝经后女性的3项临床试验确定了奥培米芬用于性交痛的安全性和有效性，患者被随机分为接受奥培米芬治疗组或安慰剂组。
治疗12周后，前两项试验结果显示，与安慰剂组患者相比，奥培米芬治疗组患者的性交困难有显著改善。第3项研究的结果支持该药长期治疗性交困难是安全的。
黑框警告
FDA提示，奥培米芬有一项黑框警告，它有类似雌激素对阴道组织的作用，已被证明可刺激子宫内膜并导致内膜增厚。绝经女性如果发生任何意外的出血，应当拜访医疗专业人士，因为这可能是子宫内膜癌的症状，该药可引起子宫内膜癌。FDA建议，该药应处方以最短的治疗时间。
黑框警告还指出了血栓和出血性卒中的发病率（分别为0.72‰和1.45‰）和深静脉血栓的发病率（1.45‰）。在雌激素单药治疗中，与卒中和深静脉血栓形成的风险相比，这些发病率被认为是低风险。
奥培米芬在临床试验中报道的常见不良反应包括：潮热/潮红、阴道分泌物增多、肌肉痉挛、外阴分泌物和出汗过多。