library.onepin.app/triptorelin Peptide Education Library
Education only, not medical advice 21+ Every dose is an example to finalize with a licensed provider

OnePin Peptide Library · Hormonal

Hormonal Peptide Prescription drug

Triptorelin

Decapeptyl · Trelstar · Diphereline · Gonapeptyl

Triptorelin is a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH), also known as luteinizing hormone-releasing hormone (LHRH). It differs from native GnRH by substitution of D-tryptophan at position 6, which makes it resistant to enzymatic degradation and significantly more potent than endogenous GnRH. Brand names include Trelstar, Decapeptyl, and Diphereline.,Triptorelin works through a biphasic mechanism. Initial administration causes a brief surge in LH, FSH, and downstream sex hormones (the 'flare' effect). With continuous or repeated depot administration, it downregulates GnRH receptors on pituitary gonadotropes, leading to profound suppression of LH and FSH secretion and consequently reducing testosterone and estradiol to castrate or prepubertal levels.,Triptorelin is FDA-approved for the palliative treatment of advanced prostate cancer (Trelstar depot formulations) and for central precocious puberty. It is also widely used in Europe for endometriosis, uterine fibroids, and assisted reproduction protocols. In off-label contexts, a single low-dose injection (typically 100 mcg) has been used for post-cycle therapy (PCT) in the bodybuilding community to restart the hypothalamic-pituitary-gonadal (HPG) axis after anabolic steroid use.

Quick Start
Route
Intramuscular (IM) or Subcutaneous (SubQ)
Start low
100mcg (PCT) or 3.75mg depot (clinical)
Frequency
Single dose (PCT) or monthly/3-month depot (clinical)
Timing
No specific requirement

Start here. Every protocol below is ordered lowest-first. Begin at the smallest effective dose, hold about a week to assess tolerance, and step up only if needed.

Tiered Protocols · lowest first
Quick Start
Conservative start
100mcg (PCT) or 3.75mg depot (clinical) · Intramuscular (IM) or Subcutaneous (SubQ) · Single dose (PCT) or monthly/3-month depot (clinical)
Lowest starting point. Hold about a week to assess tolerance before stepping up.
100mcg (PCT) or 3.75mg depot (clinical)
Single dose (PCT) or monthly/3-month depot (clinical)
Expert
HPTA Restart Protocol
100 mcg · SubQ · As needed
anecdotal · community
100 mcg
As needed
Research
Depot (Prostate cancer)
3.75 mg depot · Intramuscular · Monthly (every 28 days)
human clinical trial · Heidari Bateni et al. 2015 (Nephrourol Mon, PMID 26290848); FDA-approved depot label
3.75 mg depot
Monthly (every 28 days)
Reconstitution CalculatorU-100
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01

How it works

Acts as a GnRH superagonist with 100x greater potency than native GnRH. Initial binding to pituitary GnRH receptors causes a transient 'flare' of LH and FSH release (days 1-7), temporarily increasing sex hormone levels.,Continuous or depot administration causes GnRH receptor downregulation and desensitization of pituitary gonadotropes, leading to profound suppression of LH and FSH. This results in medical castration with testosterone falling to <50 ng/dL (prostate cancer) or estradiol to prepubertal levels.,Low single-dose use (PCT context): A single 50-100 mcg dose is proposed to cause a strong but transient LH/FSH surge without sustained suppression, theoretically kickstarting endogenous testosterone production after exogenous androgen use.

Acts as a GnRH superagonist with 100x greater potency than native GnRH. Initial binding to pituitary GnRH receptors causes a transient 'flare' of LH and FSH release (days 1-7), temporarily increasing sex hormone levels.,Continuous or depot administration causes GnRH receptor downregulation and desensitization of pituitary gonadotropes, leading to profound suppression of LH and FSH. This results in medical castration with testosterone falling to <50 ng/dL (prostate cancer) or estradiol to prepubertal levels.,Low single-dose use (PCT context): A single 50-100 mcg dose is proposed to cause a strong but transient LH/FSH surge without sustained suppression, theoretically kickstarting endogenous testosterone production after exogenous androgen use.

02

What to expect

Early
Days 1–7

Days 1-7: LH/FSH flare with transient increase in sex hormones. For PCT, this surge is the intended therapeutic effect. For cancer treatment, anti-androgen cover may be needed.

03

Evidence

HumanPresent
AnimalPresent
In-vitroPresent
1997A randomized comparison of the clinical and hormonal effects of two GnRH agonists in patients with prostate cancer · Heyns CF et al, European Urology ↗peer reviewed
2019Triptorelin · Lepor H, Reviews in Urology ↗review
2017An Update on Triptorelin: Current Thinking on Androgen Deprivation Therapy for Prostate Cancer · Lebret T et al, Advances in Therapy ↗review
2011Six-month gonadotropin releasing hormone (GnRH) agonist depots provide efficacy, safety, convenience, and comfort · Crawford ED, Hou AH, Cancer Management and Research ↗review
04

Interactions & stacking

What's safe to combine, and what belongs in a separate pin.

Safe & synergistic

BPC-157Tissue repair peptide does not interact with GnRH signaling
Thymosin Alpha-1Immune peptide and GnRH agonist act through entirely unrelated systems
AnastrozoleAI can manage estrogen during the initial testosterone flare from triptorelin
EnclomipheneFor PCT use - triptorelin single dose provides initial LH/FSH surge, followed by enclomiphene to sustain endogenous testosterone recovery

Keep separate

Nandrolone DecanoateExogenous anabolic steroids suppress the HPG axis that triptorelin aims to modulate - do not use concurrently
Testosterone CypionateExogenous testosterone suppresses LH/FSH, negating the purpose of GnRH agonist therapy for axis recovery
GnRH (Gonadorelin)Both act on GnRH receptors - co-administration causes unpredictable receptor dynamics and desensitization
KisspeptinKisspeptin stimulates endogenous GnRH release while triptorelin acts as a GnRH superagonist - overlapping and potentially conflicting HPG axis stimulation
05

Pharmacokinetics

Illustrative plasma concentration · 24 h
Half-life
~3-5 hours (non-depot); depot formulations provide sustained release over 1-6 months
Peak · Tmax
1-3 hours IM/SubQ (non-depot); depot release peaks vary by formulation
Elimination
~15-25 hours (non-depot); depot formulations sustain levels for 1-6 months
Activity
1-7 days (single low dose LH/FSH flare); 1-6 months (depot formulations provide sustained suppression)

Storage. Store refrigerated at 2-8C. Depot formulations: follow specific product instructions. Reconstituted non-depot solution should be used immediately.

06

Regulatory status

FDA-approved (Trelstar) for advanced prostate cancer and central precocious puberty. EMA-approved (Decapeptyl/Diphereline) for additional indications including endometriosis and IVF. Prescription only.

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The guide & community

The complete Triptorelin walkthrough, real protocol discussion and coaching live inside the BlessUp community on Skool.

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