BAY 1002670: a novel, highly potent and selective progesterone receptor modulator for gynaecological therapies

Wagenfeld, Andrea; Bone, Wilhelm; Schwede, Wolfgang; Fritsch, Martin; Fischer, Oliver M.; Moeller, Carsten

doi:10.1093/humrep/det247

Cited by 41 publications

(30 citation statements)

References 36 publications

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“…Another approach is to modulate ER activity, either by ER-b ligands (CLI or OBHS) already used in clinical practice [261] or by selective ER modulators (arzoxifene, bazedoxifene [262], raloxifene [263]) which are still tested in experimental models. In the regulation of progesterone action, P4 antagonists (mifepristone, RU-486 [264]) and selective PR modulators (asoprisnil, BAY 1002670) [265], PF-02413873 [266]) have shown promising results in endometriosis therapy in either clinical application or in rodent experiments. In order to eliminate the systemic side effects, Mirena coil (levonorgestrel-releasing intrauterine system) has been added to the therapy [267].…”

Section: Novel Approaches and Therapeutic Agents In Endometriosismentioning

confidence: 99%

Endometriosis — insights into a multifaceted entity

Amălinei

Păvăleanu

Lozneanu

et al. 2018

Folia Histochem Cytobiol.

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Firstly described at the end of nineteenth century, endometriosis remains an enigmatic disease, from etio-pathogenesis to specific markers of diagnosis and its ability to associate with malignancies. Our review has been designed from a historical perspective and steps up to an updated understanding of the disease, facilitated by relatively recent molecular and genetic progresses. Although the histopathological diagnosis is relatively simple, the therapy is difficult or ineffective. Experimental models have been extremely useful as they reproduce the human disease and allow the testing of different potential modulators or treatment options. Due to molecular resemblance to carcinogenesis, applications of anti-cancer agents are currently under scrutiny. The desired goal of an efficient therapy against symptomatic disease, along with associated infertility and malignancies, needs a deeper insight into the complex mechanisms involved in endometriosis initiation, development, and progres-sion. Current trends in genomic and proteomic approaches are useful for a more accurate classification and for the identification of new therapeutic targets.

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Section: Novel Approaches and Therapeutic Agents In Endometriosismentioning

confidence: 99%

Endometriosis — insights into a multifaceted entity

Amălinei

Păvăleanu

Lozneanu

et al. 2018

Folia Histochem Cytobiol.

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“…Vilaprisan (VPR) is a selective progesterone receptor modulator (SPRM) [4][5][6][7], which is currently being tested in phase III clinical trials for the long-term treatment of patients with uterine fibroids. The pharmacokinetic (PK) properties of VPR have been well characterized, as described by Schultze-Mosgau et al [8,9].…”

Section: Introductionmentioning

confidence: 99%

CYP3A4‐mediated effects of rifampicin on the pharmacokinetics of vilaprisan and its UGT1A1‐mediated effects on bilirubin glucuronidation in humans

Chattopadhyay

Kanacher

Casjens

et al. 2018

Brit J Clinical Pharma

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

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confidence: 99%

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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BAY 1002670: a novel, highly potent and selective progesterone receptor modulator for gynaecological therapies

Abstract: The studies took place at Bayer Pharma AG. All authors are employees of Bayer Pharma AG. No external funding declared.

Cited by 41 publications

References 36 publications

Endometriosis — insights into a multifaceted entity

Endometriosis — insights into a multifaceted entity

CYP3A4‐mediated effects of rifampicin on the pharmacokinetics of vilaprisan and its UGT1A1‐mediated effects on bilirubin glucuronidation in humans

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

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