Acyline
Also known as: Acylated GnRH antagonist, Acyline, GnRH antagonist (NIH), RS-68439, TA-001
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Summary
Acyline is a synthetic acylated GnRH antagonist investigated for male contraception and for lowering testosterone in hormone‑sensitive conditions. It is administered by subcutaneous injection and is not approved for clinical use.
Mechanism of Action
Competitive antagonism of pituitary GnRH receptors, suppressing LH and FSH secretion and thereby reducing gonadal steroid production.
Routes of Administration
Goals & Uses
- Precocious puberty treatment (research)Pediatric EndocrinologyLow
- Prostate cancer therapyOncologyLow
- Research tool for HPG axis studiesResearchHigh
- Endometriosis treatmentGynecologyLow
- Prostate cancer androgen suppressionOncologyModerate
- Testosterone suppressionOncology/EndocrinologyModerate
- Male contraceptionReproductive EndocrinologyModerate
- Suppression of gonadotropins (LH/FSH)EndocrinologyModerate
Contraindications
- known hypersensitivity to peptideImmunologicModerate
- Severe hepatic impairmentOrganModerateLiver function concerns
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- Hypersensitivity to GnRH analoguesAllergy/ImmunologyHigh
- Osteoporosis or significant bone lossMusculoskeletalModerate
Adverse Effects
- Mood changesPsychiatricUncommon
- Injection site reactionsLocalCommon
- Injection site painLocalCommonPain at the injection site
- HeadacheNeurologicUncommonPain in the head or upper neck
- Decreased libidoSexual / EndocrineUncommon
- Hot flashesEndocrine / VasomotorCommon
- Hypogonadism symptoms (hot flashes, reduced libido)Endocrine/ReproductiveCommon
- Bone mineral density reductionMusculoskeletalUncommon
Drug Interactions
- Testosterone replacement therapyModerate
- CYP3A4 inhibitorsLow
- Estrogen-containing contraceptivesModerate
- CYP450 inhibitorsLow
- Other GnRH analoguesModerate
- Testosterone (exogenous)Low
Population Constraints
- Women of child‑bearing potentialGenderAbsolute
- Pediatric patientsAgeAbsolute
- ElderlyAgeRelative
- Patients with pre-existing cardiovascular diseaseCardiovascularRelative
- Postmenopausal womenReproductive StatusRelative
Regulatory Status
- European UnionInvestigationalClinical studies ongoing; no EMA marketing authorization.
- United StatesInvestigationalPhase II trials completed; not FDA‑approved.
- United KingdomInvestigationalLimited trial use; not licensed.
Investigational product; no FDA, EMA, or MHRA approval. Clinical trials have evaluated safety and efficacy.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Acyline?
Acyline is a synthetic acylated GnRH antagonist investigated for male contraception and for lowering testosterone in hormone‑sensitive conditions. It is administered by subcutaneous injection and is not approved for clinical use.
What is Acyline used for?
Acyline is educationally associated with: Precocious puberty treatment (research), Prostate cancer therapy, Research tool for HPG axis studies, Endometriosis treatment, Prostate cancer androgen suppression, Testosterone suppression, Male contraception, Suppression of gonadotropins (LH/FSH). Educational only — not medical advice.
How is Acyline administered?
Recorded routes of administration: Subcutaneous.
What are the potential side effects of Acyline?
Reported adverse effects include: Mood changes, Injection site reactions, Injection site pain, Headache, Decreased libido, Hot flashes, Hypogonadism symptoms (hot flashes, reduced libido), Bone mineral density reduction. This list is not exhaustive — consult a qualified clinician.
Who should avoid Acyline?
Recorded contraindications: known hypersensitivity to peptide, Severe hepatic impairment, Pregnancy, Hypersensitivity to GnRH analogues, Osteoporosis or significant bone loss. Consult a qualified clinician before use.