Delving into the Latest Updates on Triptorelin acetate with Synapse

Overview

Basic Info

Drug Type

Synthetic peptide

Synonyms

+ [4]

Target

GnRHR

Action

agonists

Mechanism

GnRHR agonists(Gonadotropin-releasing hormone receptor agonists)

Therapeutic Areas

NeoplasmsUrogenital DiseasesEndocrinology and Metabolic Disease

Active Indication

EndometriosisPuberty, PrecociousProstatic Cancer

Inactive Indication

HIV Infections

Originator Organization

Changchun Genescience Pharmaceuticals Co., Ltd.

Active Organization

Shandong Luye Pharmaceutical Co., Ltd.

Changchun Genescience Pharmaceuticals Co., Ltd.

Shanghai Livzon Pharmaceutical Co. Ltd.

+ [4]

Inactive Organization

ISR Immune System Regulation AB

License Organization

BL&H Co., Ltd.

China Resources Pharmaceutical Group Ltd.

PT Dexa Medica

+ [3]

Drug Highest PhaseApproved

First Approval Date

China (15 Sep 2004),

Prostatic Cancer

Regulation-

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Structure/Sequence

Molecular FormulaC66H86N18O15

InChIKeyHPPONSCISKROOD-OYLNGHKZSA-N

CAS Registry140194-24-7

Sequence Code 15218785

Source: *****

To investigate the pharmacokinetics of triprerelin acetate for injection and triprerelin acetate (Dufferin ®) for injection of reference preparation in patients with prostate cancer by single intramusculodynamic injection in fasting state, and to evaluate the bioequivalence of the two formulations in fasting state.

Start Date04 Dec 2024

Sponsor / Collaborator

The Affiliated Hospital of Qingdao University

[+8]

CTR20243425

/ RecruitingNot Applicable

注射用醋酸曲普瑞林人体生物等效性研究

[Translation] Study on the bioequivalence of triptorelin acetate for injection in healthy volunteers

研究空腹状态下单次肌肉注射受试制剂注射用醋酸曲普瑞林与参比制剂注射用醋酸曲普瑞林（达菲林®）在前列腺癌患者体内的药代动力学，评价空腹状态下两种制剂的生物等效性和安全性。

[Translation]

To study the pharmacokinetics of a single intramuscular injection of the test formulation triptorelin acetate for injection and the reference formulation triptorelin acetate for injection (Diphylline®) in patients with prostate cancer under fasting conditions and to evaluate the bioequivalence and safety of the two formulations under fasting conditions.

Start Date22 Oct 2024

Sponsor / Collaborator

Qilu Pharmaceutical Co., Ltd.

CTR20240796

/ RecruitingPhase 3

一项多中心、开放、单臂 III 期临床试验：评估注射用醋酸曲普瑞林微球治疗儿童中枢性性早熟的有效性和安全性

[Translation] A multicenter, open-label, single-arm phase III clinical trial to evaluate the efficacy and safety of triptorelin acetate microspheres for injection in the treatment of central precocious puberty in children

评价注射用醋酸曲普瑞林微球治疗中枢性性早熟（CPP）受试者的临床疗效。

[Translation]

To evaluate the clinical efficacy of triptorelin acetate microspheres for injection in the treatment of subjects with central precocious puberty (CPP).

Start Date14 Jul 2024

Sponsor / Collaborator

Lizhu Group Lizhu Medicine Research Institute

[+1]

100 Clinical Results associated with Triptorelin acetate

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100 Translational Medicine associated with Triptorelin acetate

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100 Patents (Medical) associated with Triptorelin acetate

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930

Literatures (Medical) associated with Triptorelin acetate

21 Apr 2025·Future Oncology

Study of persistence and adherence to ADT in prostate cancer: relugolix, degarelix, and GnRH agonists in the US

Article

Author: Kinkead, Frédéric ; Hafron, Jason ; McKay, Rana R. ; Romdhani, Hela ; Hong, Agnes ; Flanders, Scott C. ; Ryan, Michael J.

AIMSAndrogen deprivation therapy (ADT) is standard for advanced prostate cancer. Relugolix, a gonadotropin-releasing hormone (GnRH) receptor antagonist, is the only oral ADT, with limited real-world data on therapy persistence and adherence. This retrospective study evaluates persistence and adherence of relugolix, degarelix, and GnRH agonists (leuprolide, goserelin, triptorelin, histrelin) using data from the IBM MarketScan Research Database (Jan 2017 - Dec 2022).METHODSThe IBM MarketScan Research Database (1 January 2017 - 31 December 2022) was used for enrollment history and claims. ADT adherence was measured by the proportion of days covered (PDC) at 3, 6, and 12 months, calculated as days on ADT divided by period duration. Kaplan-Meier analysis assessed treatment persistence by measuring time to treatment discontinuation.RESULTSRelugolix had higher adherence (PDC ≥ 80%) at 12 months (60.8%) compared to degarelix (13.0%) and GnRH agonists (46.3%). Median time to discontinuation was also longer for relugolix (13.5 months) than degarelix (3.1 months) and GnRH agonists (8.8 months). Persistence and adherence rates were higher in metastatic prostate cancer.CONCLUSIONSFindings support relugolix use as an oral treatment due to its favorable persistence and long-term adherence profiles.

22 Mar 2025·Cell journal

Diagnosis Prostate Cancer via Molecular Computed Tomography Imaging based on Targeted Gold Nanoparticles.

Article

Author: Rabani, Fatemeh ; Abbasi, Samaneh ; Ghorbani, Farzaneh ; Khademi, Sara ; Montazerabadi, Alireza

OBJECTIVENanocomplexes, as targeted contrast agents, have been developing for diagnostic imaging, especially in computed tomography (CT). The present study aimed to investigate a novel approach using Triptorelin-conjugated Alginate-coated Gold Nanoparticles (TAuNPs) for early prostate cancer diagnosis through molecular CT imaging.MATERIALS AND METHODSIn the current experimental study, AuNPs and TAuNPs were synthesized and then characterized using transmission electron microscopy (TEM), fourier transform infrared (FTIR) spectroscopy, and dynamic light scattering (DLS), and the AuNPs cytotoxicity and the cell viability were also assessed using the 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) assay. The intensity of X-ray attenuation and contrast to noise ratio (CNR) for nontargeted and targeted nanoparticles were measured for tube voltages of 90.0, 120.0, and 140.0 kVp at different mAs, and the four different concentrations, including 25.0, 50.0, 75.0, and 100.0 μg/ml.RESULTSThe synthesized TAuNPs are non-toxic within the concentration range of 25-100 μg/ml, at tube potentials of 90.0, 120.0, and 140.0 kVp, and 145.0 as well as 266.0 mA. Also, the X-ray attenuation of targeted cells was 1.74, 2.23, and 2 times higher, respectively, than that of non-targeted cells for a concentration of 100 μg/ml. Furthermore, the CNR values for TAuNPs compared to AuNPs at tube potentials of 90.0, 120.0, and 140.0 kVp, and 266.0 mA, were 1.65, 3.35, and 2.57 c/ϭ, respectively.CONCLUSIONThe current study demonstrates that synthesized TAuNPs are emerged as a contrast agent, which is targeted for molecular CT imaging of prostate cancer cells, expressing the gonadotropin-releasing hormone (GnRH) receptor.

25 Feb 2025·British Journal of Hospital Medicine

Efficacy of Triptorelin Combined with Recombinant Human Growth Hormone (rhGH) on Serum Sex Hormones, Bone Age, and Clinical Outcomes in Girls with Precocious Puberty

Article

Author: Yao, Xinmei ; Zhao, Lihong ; Lao, Xiaofei ; Chen, Huichao ; Zhu, Xiaoqiang

Aims/Background Triptorelin effectively delays bone age progression in children with precocious puberty but may suppress pituitary growth hormone response, affecting growth hormone-binding protein secretion and overall growth rate. This study aimed to evaluate the efficacy and safety of triptorelin alone versus in combination with recombinant human growth hormone (rhGH) in treating girls with precocious puberty. Methods This retrospective study examined 82 girls with precocious puberty treated at The First People’s Hospital of Tongxiang from January 2021 to June 2023. Patients treated with triptorelin alone were assigned to the control group (n = 42), while those treated with triptorelin combined with rhGH formed the study group (n = 40). Both groups received continuous treatment for one year. Outcomes, including efficacy and safety, were compared between the groups. Results Following treatment, height and body mass in the study group were significantly higher than those in the control group (t = 2.126, p = 0.037; t = 2.419, p = 0.018). The bone age/chronological age (BA/CA) ratio in the study group was significantly lower than that in the control group (t = 2.185, p = 0.032). Levels of estradiol (E2), luteinizing hormone (LH), and follicle-stimulating hormone (FSH) in the study group were also significantly reduced compared to the control group (t = 2.208, p = 0.030; t = 4.492, p < 0.001; t = 2.952, p = 0.004). Furthermore, left and right ovarian volumes and uterine volume were significantly lower in the study group than those in the control group (t = 2.740, p = 0.008; t = 2.936, p = 0.004; t = 2.520, p = 0.014). After one year, the effective treatment rate in the study group was higher than that in the control group (97.50% vs 80.95%, p < 0.05). No serious adverse reactions were observed in either group during the treatment period. Conclusion The combination of triptorelin and rhGH demonstrates a clear therapeutic in girls with precocious puberty, which effectively delays bone age growth, regulates sex hormone levels, and reduces ovarian and uterine volumes without severe adverse effects.

100 Deals associated with Triptorelin acetate

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R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Endometriosis	China	Livzon Pharmaceutical Group, Inc.	26 Sep 2024
Puberty, Precocious	Australia	Ferring Pharmaceuticals Pty Ltd.	04 Mar 2015
Prostatic Cancer	China	Changchun Genescience Pharmaceuticals Co., Ltd.	15 Sep 2004

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Puberty, Precocious	NDA/BLA	China	Changchun Genescience Pharmaceuticals Co., Ltd.	18 Apr 2024
Endometriosis	NDA/BLA	China	Shanghai Livzon Pharmaceutical Co. Ltd.	24 Aug 2023
Prostatic Cancer	Discovery	China	Shanghai Livzon Pharmaceutical Co. Ltd.	06 Apr 2020
HIV Infections	Discovery	Sweden	ISR Immune System Regulation AB	19 Sep 2018
HIV Infections	Discovery	Germany	ISR Immune System Regulation AB	19 Sep 2018

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ESPE2023	Not Applicable	Puberty, Precocious	148	Subcutaneous Triptorelin Acetate	hweqktzikt(lcahazdhks) = ckkkayavyi djlzuwbqam (zxfvwtyvjn )	-	21 Sep 2023
ESPE2018	Not Applicable	Puberty, Precocious	-	Leuprorelin Acetate	cqcykvtgmf(eazxsviqoq) = dmolbrrszf yptttaqvje (gstdupdlbl ) View more	Positive	27 Sep 2018
				Triptorelin Acetate	cqcykvtgmf(eazxsviqoq) = vqxsoshpbi yptttaqvje (gstdupdlbl ) View more
ASCO2017	Phase 2	Breast Cancer Neoadjuvant	41	Letrozole 2.5mg daily	(wxgocdybse) = gemitokjhg jxzpfwrwsj (totjrjwcdc ) View more	Positive	30 May 2017
				Combined with triptorelin in premenopausal patients	(wxgocdybse) = fpunnwrecj jxzpfwrwsj (totjrjwcdc ) View more
ASCO_GU2016	Not Applicable	Prostatic Cancer Neoadjuvant \| Adjuvant	670	Buserelin	lqrpijbdrl(ujtmqyycge) = tutazlbrvq ylscihygck (krzoarjrcn )	-	10 Jan 2016
				Goserelin	lqrpijbdrl(ujtmqyycge) = jajorgvipf ylscihygck (krzoarjrcn )
ESPE2014	Not Applicable	Puberty, Precocious	14	Triptorelin acetate	(bsxcpecvpn) = hohvtmllwr qhsgqybnat (rwlgilbjos )	-	18 Sep 2014
ASCO2008	Not Applicable	Breast Cancer Neoadjuvant	-	GnRH agonist (triptorelin)	dmszyyalyu(dijrzkmild) = kqhgatwiig vhkzgvipar (xxqlhjvgbq )	-	20 May 2008
				No triptorelin (control)	dmszyyalyu(dijrzkmild) = volnabhrrf vhkzgvipar (xxqlhjvgbq )

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Biosimilar

Competitive landscape of biosimilars in different countries/locations. Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3.

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