Delving into the Latest Updates on Trilostane with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Abetafen, Modrastane, Modrefen

+ [9]

Target

ERβ

Action

modulators

Mechanism

ERβ modulators(Estrogen receptor beta modulators)

Therapeutic Areas

Endocrinology and Metabolic DiseaseOther Diseases

Active Indication

Cushing SyndromeHyperaldosteronism

Inactive Indication

Adenocarcinoma of prostateCastration-Resistant Prostatic CancerProstatic Cancer

Originator Organization

Sanofi

Active Organization

Mochida Pharmaceutical Co., Ltd.

Inactive Organization

Genzyme Corp.

Bioenvision, Inc.

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (31 Dec 1984),

Prostatic Cancer

Regulation-

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Structure/Sequence

Molecular FormulaC20H27NO3

InChIKeyKVJXBPDAXMEYOA-CXANFOAXSA-N

CAS Registry13647-35-3

In menstruation an effective shedding of the endometrial lining occurs. Both progesterone and estrogen levels fall sharply at this time. During medical abortion the endometrial shedding is sometimes ineffective causing an incomplete abortion which may cause prolonged bleeding or require surgical intervention. In medical abortion a progesterone antagonist is used as treatment but the estrogen levels are not targeted. The investigators wish to explore whether addition of letrozole or trilostane which target estrogen levels can lead to a more effective shedding of the endometrial lining.

Start Date01 May 2012

Sponsor / Collaborator

Karolinska Institutet

[+2]

EUCTR2004-004533-34-GB

/ Not yet recruitingPhase 4

A Phase IV Non-randomised Study of Modrenal® (Trilostane) in Post-menopausal Women with Advanced, Oestrogen Receptor Positive Breast Cancer for whom Prior Endocrine Therapies have Failed, One of which was an Aromatase Inhibitor

Start Date19 May 2005

Sponsor / Collaborator

Bioenvision, Inc.

NCT00181597

/ CompletedPhase 2

A Phase II Study of Trilostane for Androgen-Independent Prostate Cancer

The main purpose of this study is to test the safety of trilostane by looking at what effects, good and bad, it has on patients with androgen-independent prostate cancer.

Start Date01 Mar 2004

Sponsor / Collaborator

Genzyme Corp.

100 Clinical Results associated with Trilostane

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100 Translational Medicine associated with Trilostane

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100 Patents (Medical) associated with Trilostane

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606

Literatures (Medical) associated with Trilostane

01 Mar 2025·Infectious Medicine

Novel drug targets for monkeypox: From viral to host proteins

Article

Author: Feng, Shuidong ; Niu, Youya ; Yang, Fei ; Zhu, Zhaozhong ; Xu, Yunhai ; Sun, Qin

BackgroundThe ongoing threat of the monkeypox virus (MPXV) underscores the need for new antiviral treatments, yet drug targets and candidate therapies are limited.MethodsCalculating the centrality, conservation, and immunogenicity of MPXV proteins in the network to identify viral drug targets. Constructing the MIP-human protein interaction network and identifying key human proteins as potential drug targets through network topology analysis.ResultsWe constructed a comprehensive protein-protein interaction (PPI) network between MPXV and humans, using data from the P-HIPSTer database. This network included 113 viral proteins and 2 607 MPXV-interacting human proteins (MIPs). We identified three MPXV proteins (OPG054, OPG084, and OPG190) as key targets for antiviral drugs, as well as 95 critical MIPs (most interacting MIPs, MMIPs) within the MPXV-human PPI network. Further analysis revealed 31 MMIPs as potential targets for broad-spectrum antiviral agents, supported by their involvement in other viral interactions. Functional enrichment of MIPs indicated their roles in infection and immune-related pathways.ConclusionsIn total, we identified 112 drugs targeting MPXV proteins and 371 drugs targeting MMIPs, with fostamatinib, trilostane, and raloxifene being able to inhibit both viral and host proteins. This work provides critical insights into MPXV-human interactions and supports the development of targeted antiviral therapies.

01 Jan 2025·Journal of Reproduction and Development

Cortisol prevents the suppressive effect of LPS on bovine oocyte maturation <i>in vitro</i>

Article

Author: TAMURA, Mahiro ; TETSUKA, Masafumi ; MURANISHI, Yuki ; ADEMOLA, Omowumi ; PREMARATNE, Sameera

During the periovulatory period, local production of cortisol surges in the bovine cumulus-oocyte complex (COC), although its physiological significance is not well understood. As a potent anti-inflammatory agent, cortisol may protect the COC from inflammation caused by lipopolysaccharide (LPS), an endotoxin known to cause infertility in postpartum cows. This study examined the effect of cortisol, together with progesterone (P4), on LPS-challenged bovine oocyte maturation. COCs were aspirated from follicles 2-5 mm in diameter and subjected to in vitro maturation for 21 h with various combinations of LPS, cortisol, cortisone (a substrate for cortisol production), trilostane (a P4 synthesis inhibitor), and nomegestrol acetate (NA; a synthetic progestogen). LPS (0.001, 0.01, 0.1, 1 μg/ml) suppressed oocyte maturation in a dose-dependent manner, and this effect was reversed by concomitant treatment with cortisol (0.1 μM). COCs converted cortisone to cortisol, and the locally produced cortisol (approximately 0.01 μM) was capable of negating the suppressive effect of LPS (1 μg/ml) on oocyte maturation. Trilostane suppressed oocyte maturation by eliminating P4 production, indicating the crucial role of P4 in this process. LPS equally suppressed oocyte maturation, regardless of the presence or absence of P4 or the various doses of NA (0.001-1 μM). This suggests that P4 alone does not inhibit the action of LPS. However, in the absence of P4, cortisol could not suppress the LPS effect on oocyte maturation. Collectively, these findings suggest that the bovine COC can protect itself from the suppressive effects of LPS by producing cortisol, with P4 being essential for this function.

01 Jan 2025·Veterinary Clinics of North America: Exotic Animal Practice

Adrenal Disease in Small Mammals

Article

Author: Jekl, Vladimir

Adrenal gland disease has been described as a rare disease in pet rabbits and rodents. Hyperadrenocorticism with excessive secretion of corticosteroids is most commonly observed in guinea pigs and hamsters, with dermatologic signs similar to those seen in dogs. Diagnosis is based on clinical signs, diagnostic imaging such as abdominal ultrasound, and determination of the blood hormone concentrations. In guinea pigs, an adrenocorticotrophic hormone stimulation test with the measurement of salivary cortisol or corticosterone concentrations is recommended. The recommended treatment of adrenal disease in guinea pigs and hamsters is oral administration of trilostane or ketoconazole; surgical treatment is also possible.

100 Deals associated with Trilostane

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External Link

KEGG	Wiki	ATC	Drug Bank
D01180	Trilostane	H02CA01	DB01108

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Cushing Syndrome	Japan	Mochida Pharmaceutical Co., Ltd.	03 Feb 1986
Hyperaldosteronism	Japan	Mochida Pharmaceutical Co., Ltd.	03 Feb 1986

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Adenocarcinoma of prostate	Phase 1	United States	Genzyme Corp.	01 Mar 2004
Castration-Resistant Prostatic Cancer	Phase 1	United States	Genzyme Corp.	01 Mar 2004