Results of the asteroid (assess safety and efficacy of vilaprisan in patients with uterine fibroids) 1 study: a phase 2, placebo-controlled dose finding study

Bradley, Linda D.; Ren, Xiaowei; Groettrup-Wolfers, Esther; Petersdorf, Kathrin; Seitz, Christian

doi:10.1016/j.fertnstert.2016.07.278

Cited by 11 publications

(15 citation statements)

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“…The incidence of amenorrhea observed in this study (>70% at dosages >1 mg/day) was similar to that observed in the above‐described POC study and in the ASTEROID1 study in patients with uterine fibroids …”

Section: Discussionsupporting

confidence: 89%

“…In a proof‐of‐concept (POC) study, Schütt et al showed that VPR effectively suppresses menstrual bleeding in healthy women when given at dosages of 1 to 5 mg/day over 12 weeks . This finding was confirmed in a subsequent phase 2 study (ASTEROID1): in this study, VPR 0.5 to 4 mg/day over 12 weeks effectively induced amenorrhea and showed a beneficial effect on fibroid volumes and health‐related quality of life in patients with heavy menstrual bleeding due to fibroids …”

supporting

confidence: 60%

“…The incidence of amenorrhea observed in this study (>70% at dosages >1 mg/day) was similar to that observed in the above-described POC study 2 and in the ASTEROID1 study in patients with uterine fibroids. 3 As previously seen with ulipristal, 4 VPR did not cause relevant effects on the cervix as deduced from lack of difference in Insler score between pretreatment and the first treatment cycle.…”

Section: Discussionmentioning

confidence: 54%

“…Vilaprisan (VPR) is a novel, promising selective progesterone receptor modulator (SPRM) that is currently being developed for the long‐term treatment of uterine fibroids.…”

mentioning

confidence: 99%

“…2 This finding was confirmed in a subsequent phase 2 study (ASTEROID1): in this study, VPR 0.5 to 4 mg/day over 12 weeks effectively induced amenorrhea and showed a beneficial effect on fibroid volumes and health-related quality of life in patients with heavy menstrual bleeding due to fibroids. 3 Other known effects of SPRMs beside their effects on menstrual bleeding are changes in hormone concentrations and follicular development. 4 The time courses of the concentrations of estradiol (E 2 ) and progesterone (P) in serum as well as the sizes of folliclelike structures (FLS) observed in the above POC study with VPR suggest that treatment with VPR leads to inhibition of ovulation.…”

mentioning

confidence: 99%

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Effect of the Novel Selective Progesterone Receptor Modulator Vilaprisan on Ovarian Activity in Healthy Women

Schütt

Schultze‐Mosgau

Draeger

et al. 2017

The Journal of Clinical Pharma

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This randomized, double‐blind, parallel‐group study in healthy young women investigated the effect of treatment with vilaprisan (0.5, 1, 2, or 4 mg/day for 12 weeks) on ovarian function by assessing the Hoogland score, which is based on the size of follicle‐like structures as determined by transvaginal ultrasound and on estradiol and progesterone serum concentrations. Ovulation inhibition (ie, Hoogland score <6 in treatment weeks 1‐4 and 8‐12) was observed in >80% of the subjects receiving vilaprisan ≥1 mg/day. The effect was dose dependent. With a Bayesian approach, the percentage of subjects with ovulation inhibition was estimated to increase from 37% in subjects receiving 0.5 mg/day vilaprisan to 76%, 86%, and 88% in subjects receiving 1, 2, and 4 mg/day, respectively. Follicle growth was not suppressed during treatment. The majority of subjects receiving ≥1 mg/day had a Hoogland score of 4 (active follicle‐like structures, ie, follicle diameter >13 mm, estradiol >27.2 pg/mL, no progesterone increase) both at beginning and end of treatment. Mean average estradiol as well as mean maximum progesterone concentrations were noticeably decreased during treatment with vilaprisan ≥1 mg/day compared to pretreatment, but estradiol concentrations remained >80 pg/mL. Both hormones returned to pretreatment levels after the end of treatment, indicating a rapid resumption of normal ovarian activity. Amenorrhea occurred in the majority of subjects during treatment at dosages ≥1 mg/day. The adverse events observed in this study confirm the known safety profile of vilaprisan. All in all, the results of this study support the development of vilaprisan for the long‐term treatment of uterine fibroids.

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Section: Discussionsupporting

confidence: 89%

supporting

confidence: 60%

Section: Discussionmentioning

confidence: 54%

“…Vilaprisan (VPR) is a novel, promising selective progesterone receptor modulator (SPRM) that is currently being developed for the long‐term treatment of uterine fibroids.…”

mentioning

confidence: 99%

mentioning

confidence: 99%

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Effect of the Novel Selective Progesterone Receptor Modulator Vilaprisan on Ovarian Activity in Healthy Women

Schütt

Schultze‐Mosgau

Draeger

et al. 2017

The Journal of Clinical Pharma

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Pharmacokinetics and Safety of the Selective Progesterone Receptor Modulator Vilaprisan in Chinese Healthy Postmenopausal Women

Jiang

Chen

et al. 2020

Clinical Pharm in Drug Dev

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Vilaprisan is a novel selective progesterone receptor modulator for the long-term treatment of uterine fibroids and endometriosis. This study investigated the pharmacokinetics, safety, and tolerability of vilaprisan in healthy Chinese postmenopausal women. Twelve participants received multiple doses of vilaprisan once daily over 14 days as a 2-mg tablet. Plasma vilaprisan concentrations were determined using liquid chromatography-tandem mass spectrometry. The main pharmacokinetic parameters of vilaprisan were assessed with noncompartmental analysis, including maximum observed concentration (C max ), systemic exposure (area under the plasma concentration-time curve), time to reach C max and terminal half-life. Safety assessments include the documentation of adverse events, measurement of clinical/anthropometric parameters and vital signs, electrocardiogram, and physical and gynecologic examination. The participants had a mean age of 53.3 (± 4.2) years and a body mass index of 23.8 ± 2.8 kg/m 2 . Median time to reach C max was 1.5 hours after both single and multiple vilaprisan administration. Mean C max values obtained after multiple dosing (23.3 μg/L [standard deviation (SD) = 6.73]) were 1.92-fold (SD = 0.554) higher compared to single dosing (12.5 μg/L [SD = 3.04]). Mean area under the plasma concentration-time curve in the dosing interval increased with an accumulation factor of 2.98 (SD = 0.767) between single (91.3 μg • h/L [SD = 20.4]) and multiple dosing (276 μg • h/L [SD = 109]). The mean terminal half-life of vilaprisan was 44.5 hours (SD = 10.3) after multiple dosing. Mild to moderate adverse events were observed similar to previous studies. Overall, daily oral administration of the therapeutic dose of 2 mg of vilaprisan over 14 days was safe and well tolerated by all participants.

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New Horizons in Fibroid Management

Chodankar

Allison

2018

Curr Obstet Gynecol Rep

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Purpose of Review Review of the latest advances in the treatment of uterine fibroids. Addressing conservative management, medical therapy, interventional radiological procedures (non-surgical alternatives or non-excisional procedures) and conservative or radical endoscopic or open surgery (myomectomy, hysterectomy). Recent Findings Newer medical therapy relied on the use of selective progesterone receptor modulators (SPRMs) (Esmya/UPA) for management of heavy menstrual bleeding (HMB) associated with fibroids. However, the drug is currently under investigation for a link with hepatic damage associated with its use. Other SPRMs currently showing promise include vilaprisan and telapristone. New medical therapy also includes oral small molecule GnRH antagonists such as Relugolix, Elagolix and Lizagolix which are undergoing phase 2 and 3 trials and have shown promise. The new NICE guidance on HMB also suggests limited effectiveness of pharmacological methods in fibroids > 3 cm and therefore referral to an expert with possible consideration of surgery as a first-line treatment. Non-excisional procedures include the use of uterine artery embolisation which is currently being compared to myomectomy and its effect on the quality of life in the FEMME study. With regard to excisional therapies, controversy still surrounds the use of laparoscopic power morcellators (LMPs). A white paper has been issued by the US FDA in December 2017 on the matter, and a PneumoLiner still remains the only containment device approved by the US FDA for use with LMPs. With advancing surgical expertise and use the bipolar sealing devices, TLHs are increasingly being performed for larger uteri (> 12 weeks or > 280 g). Hysteroscopic retrieval systems (HRTs) are found to be increasingly used successfully for type 2 submucous myomas as one-step procedures. Summary Many treatments are available for fibroids that can help women reach the age of menopause prior to embarking on radical surgery. It seems sensible to start with conservative (medical) measures; however, for women with large fibroids, often non-excisional or surgical solution is needed. Which technique is chosen will depend upon local expertise as well as patient preference, especially the need for uterine/fertility preservation, following a detailed discussion regarding risks and benefits.

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Results of the asteroid (assess safety and efficacy of vilaprisan in patients with uterine fibroids) 1 study: a phase 2, placebo-controlled dose finding study

Cited by 11 publications

References 0 publications

Effect of the Novel Selective Progesterone Receptor Modulator Vilaprisan on Ovarian Activity in Healthy Women

Effect of the Novel Selective Progesterone Receptor Modulator Vilaprisan on Ovarian Activity in Healthy Women

Pharmacokinetics and Safety of the Selective Progesterone Receptor Modulator Vilaprisan in Chinese Healthy Postmenopausal Women

New Horizons in Fibroid Management

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