A Phase 2a Randomized, Double-Blind, Placebo and Active Comparator-Controlled, Parallel Group, Dose-Range Finding Study of MVT-602 in Healthy Premenopausal Women Undergoing Controlled Ovarian Stimulation (COS) Using a Minimal Stimulation Protocol.

Start Date23 May 2018

Sponsor / Collaborator

Myovant Sciences GmbH

NL-OMON44304

/ CompletedNot Applicable

A Phase 1, Randomized, Blinded, Placebo-Controlled, Dose-Ranging Study of MVT-602 in Healthy Premenopausal Women - MVT-602-1001 (CS0288)

Start Date30 Oct 2017

Sponsor / Collaborator

Myovant Sciences GmbH

NCT02381288

/ TerminatedPhase 2

A Randomized, Single-Blind, Placebo-Controlled Phase 2a Study to Evaluate the Stimulatory Effects of TAK-448, a Kisspeptin Analog, Administered Intermittently in Middle-aged and Older Men With Low Testosterone

The purpose of this study is to evaluate the effects on serum testosterone (ST) after 6 weeks of subcutaneous (SC) administration of different doses and dosing frequencies of TAK-448 to middle-aged and older men with low ST levels.

Start Date10 Sep 2015

Sponsor / Collaborator

Takeda Pharmaceutical Co., Ltd.

100 Clinical Results associated with MVT-602

100 Translational Medicine associated with MVT-602

100 Patents (Medical) associated with MVT-602

Literatures (Medical) associated with MVT-602

16 Aug 2024·Science Advances

Structural basis for the ligand recognition and G protein subtype selectivity of kisspeptin receptor

Article

Author: Han, Runyuan ; Chen, Jing ; Gao, Wei ; Wu, Zhangsong ; Pan, Xin ; Du, Yang ; Jiang, Shirui ; Chen, Geng ; Zhang, Binghao ; Ning, Peiruo ; Qiu, Chen ; Shi, Tingyi ; Yan, Xiaoyi ; Zhang, Zhiyi ; Ye, Fang ; Liu, Yiming ; Xu, Jun ; Wang, Qian ; Li, Jiancheng ; Xu, Lezhi

Kisspeptin receptor (KISS1R), belonging to the class A peptide-GPCR family, plays a key role in the regulation of reproductive physiology after stimulation by kisspeptin and is regarded as an attractive drug target for reproductive diseases. Here, we demonstrated that KISS1R can couple to the G i/o pathway besides the well-known G q/11 pathway. We further resolved the cryo–electron microscopy (cryo-EM) structure of KISS1R-G q and KISS1R-G i complexes bound to the synthetic agonist TAK448 and structure of KISS1R-G q complex bound to the endogenous agonist KP54. The high-resolution structures provided clear insights into mechanism of KISS1R recognition by its ligand and can facilitate the design of targeted drugs with high affinity to improve treatment effects. Moreover, the structural and functional analyses indicated that conformational differences in the extracellular loops (ECLs), intracellular loops (ICLs) of the receptor, and the “wavy hook” of the Gα subunit may account for the specificity of G protein coupling for KISS1R signaling.

01 Jul 2024·Cell Reports

Structural basis for hormone recognition and distinctive Gq protein coupling by the kisspeptin receptor

Article

Author: He, Xinheng ; Cheng, Xi ; Wang, Dongxue ; Shen, Shiyi ; Chen, Juanhua ; Cao, Yinglong ; Li, Shujie ; Xu, H Eric ; Liu, Heng ; Duan, Jia

Kisspeptin signaling through its G protein-coupled receptor, KISS1R, plays an indispensable role in regulating reproduction via the hypothalamic-pituitary-gonadal axis. Dysregulation of this pathway underlies severe disorders like infertility and precocious puberty. Here, we present cryo-EM structures of KISS1R bound to the endogenous agonist kisspeptin-10 and a synthetic analog TAK-448. These structures reveal pivotal interactions between peptide ligands and KISS1R extracellular loops for receptor activation. Both peptides exhibit a conserved binding mode, unveiling their common activation mechanism. Intriguingly, KISS1R displays a distinct 40° angular deviation in its intracellular TM6 region compared to other G_q-coupled receptors, enabling distinct interactions with G_q. This study reveals the molecular intricacies governing ligand binding and activation of KISS1R, while highlighting its exceptional ability to couple with G_q. Our findings pave the way for structure-guided design of therapeutics targeting this physiologically indispensable receptor.

01 Jan 2024·Fertility and sterility

Endocrine profile of the kisspeptin receptor agonist MVT-602 in healthy premenopausal women with and without ovarian stimulation: results from 2 randomized, placebo-controlled clinical tricals

Article

Author: Berman, Lance ; Ezzati, Max ; Migoya, Elizabeth ; Ufer, Mike ; Ferreira, Juan Camilo Arjona ; Abbara, Ali ; Lee, Tien-Yi ; Wu, Rui ; Dhillo, Waljit S ; Voors-Pette, Christine

BACKGROUND:

Kisspeptin is an essential regulator of hypothalamic gonadotropin-releasing hormone release and is required for physiological ovulation. Native kisspeptin-54 can induce oocyte maturation during in vitro fertilization treatment, including in women who are at high risk of ovarian hyperstimulation syndrome. MVT-602 is a potent kisspeptin receptor agonist with prospective utility to treat anovulatory disorders by triggering oocyte maturation and ovulation during medically assisted reproduction (MAR). Currently, the endocrine profile of MVT-602 during ovarian stimulation is unreported.

OBJECTIVE:

To determine the endocrine profile of MVT-602 in the follicular phase of healthy premenopausal women (phase-1 trial), and after minimal ovarian stimulation to more closely reflect the endocrine milieu encountered during MAR (phase-2a trial).

DESIGN:

Two randomized, placebo-controlled, parallel-group, dose-finding trials.

SETTING:

Clinical trials unit.

PATIENTS:

Healthy women aged 18-35 years, either without (phase-1; n = 24), or with ovarian stimulation (phase-2a; n = 75).

INTERVENTIONS:

Phase-1: single subcutaneous dose of MVT-602 (0.3, 1.0, or 3.0 μg) or placebo, (n = 6 per dose). Phase-2a: single subcutaneous dose of MVT-602 (0.1, 0.3, 1.0, or 3.0 μg; n = 16-17 per dose), triptorelin 0.2 mg (n = 5; active comparator), or placebo (n = 5).

MAIN OUTCOME MEASURES:

Phase-1: safety/tolerability; pharmacokinetics; and pharmacodynamics (luteinizing hormone [LH] and other reproductive hormones). Phase-2a: safety/tolerability; pharmacokinetics; pharmacodynamics (LH and other reproductive hormones); and time to ovulation assessed by transvaginal ultrasound.

RESULTS:

In both the trials, MVT-602 was safe and well tolerated across the entire dose range. It was rapidly absorbed and eliminated, with a mean elimination half-life of 1.3-2.2 hours. In the phase-2a trial, LH concentrations increased dose dependently; mean maximum change from baseline of 82.4 IU/L at 24.8 hours was observed after administration of 3 μg MVT-602 and remained >15 IU/L for 33 hours. Time to ovulation after drug administration was 3.3-3.9 days (MVT-602), 3.4 days (triptorelin), and 5.5 days (placebo). Ovulation occurred within 5 days of administration in 100% (3 μg), 88% (1 μg), 82% (0.3 μg), and 75% (0.1 μg), of women after MVT-602, 100% after triptorelin and 60% after placebo.

CONCLUSIONS:

MVT-602 induces LH concentrations of similar amplitude and duration as the physiological midcycle LH surge with potential utility for induction of oocyte maturation and ovulation during MAR.

CLINICAL TRIAL REGISTRATION NUMBER:

EUDRA-CT: 2017-003812-38, 2018-001379-20.

News (Medical) associated with MVT-602

24 Oct 2022

·www.fiercebiotech.com

Sumitomo nets Myovant in $2.9B buyout, adding IVF asset to pipeline

A deal with Myovant will give Sumitomo control of a pipeline prospect, MVT-602. Sumitomo has landed its takeover target. After seeing Myovant turn down its original offer, the Japanese drugmaker has added almost 20% to its price to get the deal done and snag a phase 2 in vitro fertilization asset. Osaka-based Sumitomo became a major shareholder in Myovant in 2019 and, having seen its partner’s share price fall from above $20 to briefly below $10, made a move to buy the remaining 48% of the drug developer earlier this month. Myovant promptly knocked back the $22.75-a-share offer but left the door open to negotiations. Sumitomo returned with an offer of $27 a share and persuaded Myovant to sign. The deal centers on two commercial products, Orgovyx and Myfembree, but will also give Sumitomo control of a pipeline prospect, MVT-602. Takeda tried and failed to develop the oligopeptide kisspeptin-1 receptor agonist as a treatment for low levels of testosterone and other sex hormones. After missing the endpoints in phase 2 trials, Takeda offloaded the rights to the drug candidate as part of the deal with Roivant Sciences that birthed Myovant. While Takeda studied the molecule, then known as TAK-448, in men with sex hormone disorders, the new partners pitched it for use in female infertility at the time of their deal in 2016. Since then, Myovant has published phase 1 and phase 2a data on the candidate, linking it to a surge in luteinizing hormone associated with high and dose-dependent rates of ovulation. The company framed the data as evidence that MVT-602 could become a safe alternative egg-maturation trigger. Yet the progress of, and investment in, MVT-602 has stalled. In its 2021-22 financial year, Myovant racked up $318,000 in R&D costs specific to the candidate, down from $4.9 million in 2018-19. In theory, Sumitomo, a larger company, has the resources to kick-start development, but it made no mention of the molecule in its statement to disclose the Myovant merger.

Acquisition

18 Oct 2022

·www.globenewswire.com

Myovant Sciences Announces New Employment Inducement Grants Under NYSE Rule 303A.08

BASEL, Switzerland, Oct. 18, 2022 (GLOBE NEWSWIRE) -- Myovant Sciences (NYSE: MYOV), a biopharmaceutical company that aspires to redefine care for women and for men through purpose-driven science, empowering medicines, and transformative advocacy, today announced that it approved equity awards for 10 new employees with a grant date of October 17, 2022 pursuant to Myovant’s 2020 Inducement Plan. The equity awards were granted to the employees joining Myovant in accordance with NYSE’s Listed Company Manual Rule 303A.08. The new employees received, in the aggregate, restricted stock units (RSUs) to purchase 96,500 common shares of Myovant. One-fourth of the shares underlying each employee’s RSU will vest on the one-year anniversary of the grant date, with the balance of the common shares vesting in twelve equal quarterly installments thereafter, in each case, subject to each such employee’s continued employment with Myovant on such vesting dates. The RSUs are subject to the terms and conditions of the 2020 Inducement Plan and the applicable RSU agreements. ABOUT MYOVANT SCIENCESMyovant Sciences aspires to redefine care for women and for men through purpose-driven science, empowering medicines, and transformative advocacy. Founded in 2016, Myovant has executed five successful Phase 3 clinical trials across oncology and women’s health leading to three regulatory approvals by the U.S. Food and Drug Administration (FDA) for men with advanced prostate cancer, women with heavy menstrual bleeding associated with uterine fibroids, and premenopausal women with moderate to severe pain associated with endometriosis, respectively. Myovant also has received regulatory approvals by the European Commission (EC) and the United Kingdom Medicines and Healthcare Products Regulatory Agency (MHRA) for women with symptomatic uterine fibroids and for men with advanced hormone-sensitive prostate cancer. Myovant has a supplemental New Drug Application under review with the FDA for updates to the United States Prescribing Information (USPI) based on safety and efficacy data from the Phase 3 LIBERTY randomized withdrawal study (RWS) of MYFEMBREE in premenopausal women with heavy menstrual bleeding due to uterine fibroids for up to two years. Myovant also is conducting a Phase 3 study to evaluate the prevention of pregnancy in women with uterine fibroids or endometriosis. In addition, Myovant is developing MVT-602, an investigational oligopeptide kisspeptin-1 receptor agonist, which has completed a Phase 2a study for female infertility as part of assisted reproduction. Sumitovant Biopharma, Ltd., a wholly owned subsidiary of Sumitomo Pharma Co., Ltd., is Myovant’s majority shareholder. For more information, please visit www.myovant.com. Follow @Myovant on Twitter and LinkedIn. Myovant Sciences ContactsInvestor Contact:Uneek MehraChief Financial and Business OfficerMyovant Sciences, Inc.investors@myovant.com Media Contact:Noelle Cloud DuganVice President, Corporate CommunicationsMyovant Sciences, Inc.media@myovant.com

18 Oct 2022

·www.biospace.com

Myovant Sciences Announces New Employment Inducement Grants Under NYSE Rule 303A.08 - October 18, 2022

BASEL, Switzerland, Oct. 18, 2022 (GLOBE NEWSWIRE) -- Myovant Sciences (NYSE: MYOV), a biopharmaceutical company that aspires to redefine care for women and for men through purpose-driven science, empowering medicines, and transformative advocacy, today announced that it approved equity awards for 10 new employees with a grant date of October 17, 2022 pursuant to Myovant’s 2020 Inducement Plan. The equity awards were granted to the employees joining Myovant in accordance with NYSE’s Listed Company Manual Rule 303A.08. The new employees received, in the aggregate, restricted stock units (RSUs) to purchase 96,500 common shares of Myovant. One-fourth of the shares underlying each employee’s RSU will vest on the one-year anniversary of the grant date, with the balance of the common shares vesting in twelve equal quarterly installments thereafter, in each case, subject to each such employee’s continued employment with Myovant on such vesting dates. The RSUs are subject to the terms and conditions of the 2020 Inducement Plan and the applicable RSU agreements. ABOUT MYOVANT SCIENCES Myovant Sciences aspires to redefine care for women and for men through purpose-driven science, empowering medicines, and transformative advocacy. Founded in 2016, Myovant has executed five successful Phase 3 clinical trials across oncology and women’s health leading to three regulatory approvals by the U.S. Food and Drug Administration (FDA) for men with advanced prostate cancer, women with heavy menstrual bleeding associated with uterine fibroids, and premenopausal women with moderate to severe pain associated with endometriosis, respectively. Myovant also has received regulatory approvals by the European Commission (EC) and the United Kingdom Medicines and Healthcare Products Regulatory Agency (MHRA) for women with symptomatic uterine fibroids and for men with advanced hormone-sensitive prostate cancer. Myovant has a supplemental New Drug Application under review with the FDA for updates to the United States Prescribing Information (USPI) based on safety and efficacy data from the Phase 3 LIBERTY randomized withdrawal study (RWS) of MYFEMBREE in premenopausal women with heavy menstrual bleeding due to uterine fibroids for up to two years. Myovant also is conducting a Phase 3 study to evaluate the prevention of pregnancy in women with uterine fibroids or endometriosis. In addition, Myovant is developing MVT-602, an investigational oligopeptide kisspeptin-1 receptor agonist, which has completed a Phase 2a study for female infertility as part of assisted reproduction. Sumitovant Biopharma, Ltd., a wholly owned subsidiary of Sumitomo Pharma Co., Ltd., is Myovant’s majority shareholder. For more information, please visit . Follow @Myovant on Twitter and LinkedIn. Myovant Sciences Contacts Investor Contact: Uneek Mehra Chief Financial and Business Officer Myovant Sciences, Inc. investors@myovant.com Media Contact: Noelle Cloud Dugan Vice President, Corporate Communications Myovant Sciences, Inc. media@myovant.com

100 Deals associated with MVT-602

External Link

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R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Infertility, Female	Phase 2	Germany	Sumitomo Pharma Co., Ltd.	26 Oct 2020
Low testosterone levels	Phase 2	United States	Takeda Pharmaceutical Co., Ltd.	10 Sep 2015
Obesity	Phase 2	United Kingdom	Takeda Pharmaceutical Co., Ltd.	01 Feb 2015
secondary testicular failure	Phase 2	United Kingdom	Takeda Pharmaceutical Co., Ltd.	01 Feb 2015
Adenocarcinoma of prostate	Phase 2	France	Millennium Pharmaceuticals, Inc.	01 Nov 2010

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


SAT-211 (ENDO2019)	Not Applicable	Hypothalamic amenorrhoea	15	MVT-602 (Women with Hypothalamic Amenorrhoea)	uzceyemzcq(pnimuvxizg) = tkuhwwqjfw hjfebblghb (eqtaooafqv, 4.4) View more	Positive	30 Apr 2019
				MVT-602 (Healthy Women in Follicular Phase)	uzceyemzcq(pnimuvxizg) = edoticikpw hjfebblghb (eqtaooafqv, 1.6) View more
OR33-4 (ENDO2019)	Not Applicable	-	12	MVT-602	tkqdvbtare(bcjpudauks) = fvmrtwnker hemnmgcgvz (lemusmcnsc, 4.2) View more	Positive	30 Apr 2019
				KP54	tkqdvbtare(bcjpudauks) = mnjhubryzm hemnmgcgvz (lemusmcnsc, 5.3) View more
NCT02381288 (CTgov)	Phase 2	Low testosterone levels	17	TAK-448 Placebo+TAK-448	umawqaelum(pbuurqvjvw) = kfwlvjlpcb tnxoezmryg (ocwvftkoee, 29.186) View more	-	17 May 2017
NCT02369796 (CTgov)	Phase 2	secondary testicular failure \| Obesity	15	TAK-448 (TAK-448 3 µg Once Weekly)	gyvnvuahdl(fxcoxnvmwq) = juxgrdwxin ikdccfqyql (jkrcwtpska, 11.3) View more	-	31 Mar 2017
				TAK-448 (TAK-448 1 µg Once Weekly)	gyvnvuahdl(fxcoxnvmwq) = rsyaxirsvp ikdccfqyql (jkrcwtpska, 24.9) View more

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