Drug intelligence / Profile preview

acyline + testosterone

Development stage
Unknown
Lead developer
Merrion Pharmaceuticals
Modality
Peptides, Small Molecules
Administration
Subcutaneous, Intramuscular, Topical
01

Overview

The combination of acyline and testosterone is a hormonal regimen that has been studied primarily for male contraception and other endocrine-related conditions. Acyline is a GnRH antagonist that suppresses gonadotropin and testosterone production, while testosterone is administered to maintain normal hormonal function while suppressing spermatogenesis. ## Mechanism of Action Acyline works by blocking the gonadotropin-releasing hormone receptor (GnRHR), which leads to suppression of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary gland[2]. This results in decreased endogenous testosterone production. The exogenous testosterone is then administered to maintain normal serum testosterone levels while still suppressing spermatogenesis through negative feedback mechanisms[1][4]. Studies have shown that this combination significantly reduces intratesticular testosterone levels (to 1.9-2.6% of control levels) and suppresses germ cell development from type B spermatogonia onward[1]. The combination effectively creates a hormonal environment that inhibits sperm production while maintaining normal systemic testosterone levels. ## Clinical Studies Research has investigated various formulations of this combination: - Testosterone enanthate (TE) injections (100 mg weekly) combined with acyline (300 μg/kg twice weekly subcutaneously)[1] - Testosterone gel (Testim) with acyline[7] The combination has been studied for: - Male contraception (reaching Phase 3 trials)[6] - Androgen deficiency (Phase 2)[6] - Type 2 diabetes mellitus (Phase 2)[6] - Insulin resistance (Phase 2)[6] - Obesity (Phase 2)[6] ## Administration Acyline is typically administered via subcutaneous injection, while testosterone can be administered through various routes including intramuscular injection (testosterone enanthate) or topical application (testosterone gel)[1][7]. The combination creates a potent suppression of spermatogenesis and intratesticular steroids, making it potentially effective for hormonal male contraception and treatment of hormone-dependent conditions.

Other names
acyline oral + testosteroneacyline + Testim
02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)AR (Adrenergic receptors)

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