VesilutevsGonadorelin (GnRH)

Molecular Formula

C₉H₁₄N₂O₇

Molecular Weight

262.2 g/mol

Half-Life

Short plasma half-life typical of dipeptides (minutes); biological effects persist for weeks to months through epigenetic gene regulation; metabolized to constituent amino acids via standard pathways

Bioavailability

High oral bioavailability for a dipeptide — absorbed intact by intestinal peptide transporter PepT1 (SLC15A1); ultra-short structure enables efficient cellular uptake and nuclear penetration

CAS Number

3918-84-1

Molecular Formula

C₅₅H₇₅N₁₇O₁₃

Molecular Weight

1182.3

Half-Life

2-4 minutes

Bioavailability

Varies by route: ~5-20% (intranasal), 100% (IV/IM injections)

CAS Number

34973-08-5

Common

• Mild gastrointestinal discomfort
• Increased urinary frequency initially
• Mild headache
• Minor fatigue

Uncommon

• Injection site irritation

Serious

• No documented serious adverse effects

Common

• Mild headache
• Local injection site reactions (redness, swelling)
• Temporary hot flashes
• Mood changes or emotional sensitivity
• Nausea or mild stomach upset
• Allergic skin reactions
• Dizziness or lightheadedness
• Temporary changes in vision
• Joint or muscle aches
• Insomnia or sleep disturbances
• Severe allergic reactions (difficulty breathing, swelling)
• Severe hormonal imbalance symptoms
• Ovarian hyperstimulation syndrome (OHSS)
• Signs of blood clots (chest pain, leg swelling)
• Severe mood changes or depression

Serious

• Severe allergic reaction

Evidence Level

Moderate human trials (Phase 1-2)

FDA Status

Research compound

Safety Overview

Vesilute (fibroin-derived peptide from Bombyx mori silk) demonstrates favorable biocompatibility from cosmetic ingredient testing with minimal allergic or irritant potential despite its animal protein origin. Limited systemic absorption occurs topically, confining effects to dermal layers with low risk of systemic toxicity. Silk-derived peptides have been used in cosmetics for >20 years without documented serious adverse events in published literature. Theoretical hypersensitivity risk exists for individuals with silk allergy, though cross-reactivity with purified peptide is low.

Contraindications

• xKnown hypersensitivity to peptide bioregulators or constituent amino acids (glutamic acid, aspartic acid)
• xPregnancy and breastfeeding — insufficient reproductive safety data
• xActive urinary tract infection requiring antibiotic treatment — treat infection first
• xBladder or prostate malignancy — proliferative effects of peptide bioregulators may be contraindicated

Evidence Level

Moderate human trials (Phase 1-2)

FDA Status

FDA approved for this use

Safety Overview

Gonadorelin is native GnRH and carries the safety profile established over 40+ years of clinical use in reproductive endocrinology. As the body's natural hormone, it produces minimal local side effects when dosed appropriately. The critical safety concern with gonadorelin is the initial flare effect within 24-48 hours of first dose—temporary elevation in FSH and LH—which can paradoxically suppress sex hormones before the desired stimulation occurs. This flare makes gonadorelin unsuitable for some conditions and explains why synthetic analogs (agonists, antagonists) are preferred in many modern fertility protocols.

Contraindications

• xPregnancy or breastfeeding
• xHormone-sensitive cancers (breast, prostate, ovarian)
• xSevere pituitary or hypothalamic disease
• xUndiagnosed abnormal vaginal bleeding
• xKnown hypersensitivity to GnRH