Peptides Studied for Skin & Hair

Histrelin is a synthetic GnRH agonist nonapeptide analog (MW ~1323.5 g/mol) with a D-His(benzyl) substitution at position 6. It is FDA-approved as a subdermal implant for advanced prostate cancer (Vantas, 50 mg implant releasing ~50 mcg/day for 12 months) and central precocious puberty (Supprelin LA, 50 mg implant releasing ~65 mcg/day for 12 months). The hydrogel implant technology provides consistent drug delivery for a full year, offering the longest interval between doses of any GnRH agonist formulation.

Afamelanotide is a 13-amino-acid synthetic analog of alpha-melanocyte-stimulating hormone (alpha-MSH) with a molecular weight of approximately 1646.9 g/mol. It was FDA-approved in October 2019 (Scenesse) to increase pain-free light exposure in adults with a history of phototoxic reactions from erythropoietic protoporphyria (EPP). Afamelanotide is administered as a subcutaneous implant that releases the peptide over approximately 10 days, stimulating eumelanin production to provide photoprotection.

Melanotan I (afamelanotide, Scenesse) is a synthetic linear analog of alpha-MSH that stimulates MC1R to increase eumelanin production. Unlike Melanotan II, it is MC1R-selective and does not significantly affect sexual function or appetite. It is FDA and EMA-approved for erythropoietic protoporphyria (EPP).

Glutathione is a tripeptide (Glu-Cys-Gly, MW ~307.3 g/mol) and the most abundant intracellular antioxidant in mammalian cells. It is critical for Phase II detoxification, free radical scavenging, immune function, and cellular redox homeostasis. Injectable (SC/IV) glutathione bypasses the poor oral bioavailability (~3%) issue and achieves clinically meaningful plasma levels. It has been studied for conditions ranging from non-alcoholic fatty liver disease to Parkinson disease.

Epidermal Growth Factor (EGF) is a 53-amino acid protein discovered by Stanley Cohen, who shared the 1986 Nobel Prize in Physiology or Medicine for this work. EGF plays a fundamental role in cell growth, proliferation, and differentiation. In medicine, recombinant human EGF (rh-EGF) is used in wound healing products and is approved in several countries (South Korea, Cuba, China) for diabetic foot ulcers and other wound indications. In cosmetics, it is marketed as oligopeptide-1 or sh-oligopeptide-1 for anti-aging. The wound healing evidence is strong; cosmetic anti-aging evidence is more limited.

Pexiganan (MSI-78) is a 22-amino-acid synthetic analog of magainin 2, an antimicrobial peptide originally isolated from the skin of the African clawed frog (Xenopus laevis). It has broad-spectrum bactericidal activity and was developed as a topical cream (Locilex) for infected diabetic foot ulcers. Despite reaching Phase III clinical trials, pexiganan was not approved by the FDA, which determined it was not superior to existing treatments.

Brilacidin (PMX-30063) is a synthetic small-molecule defensin-mimetic (MW ~564 g/mol) developed by Innovation Pharmaceuticals (formerly Cellceutix). It is a peptidomimetic, not a true peptide, designed to mimic the amphipathic structure and antimicrobial mechanism of host defense peptides (defensins). Brilacidin has been investigated in Phase II clinical trials for acute bacterial skin and skin structure infections (ABSSSI) and oral mucositis, and was explored for COVID-19.

GHK is a naturally occurring tripeptide first isolated from human plasma. It declines significantly with age. Even without copper complexation, GHK demonstrates gene-regulatory activity affecting over 4,000 genes related to tissue repair, immune function, and anti-inflammatory responses.

GHK is a naturally occurring tripeptide (Gly-His-Lys) that serves as the base form of GHK-Cu. Found in human plasma, saliva, and urine, its concentration declines with age. Researched for wound healing, tissue repair, and gene expression modulation related to tissue remodeling and collagen synthesis.

TB-500 is a synthetic fragment of thymosin beta-4 (Tβ4), a naturally occurring 43-amino-acid peptide found throughout human tissues. TB-500 contains the active healing region (sequence: Ac-LKKTETQ, MW ~889 g/mol) responsible for cell migration and tissue repair. It has a handful of human RCTs for wound healing and dry eye, plus a dedicated safety trial in 40 healthy adults showing minimal adverse effects. Despite this, it remains unapproved for human therapeutic use in all major markets and is banned by WADA and in horse racing.

KPV is a naturally occurring tripeptide (Lys-Pro-Val, MW ~342.4 g/mol) derived from the C-terminal region (positions 11–13) of alpha-melanocyte-stimulating hormone (α-MSH). It retains potent anti-inflammatory and antimicrobial properties of the full-length hormone without activating melanocortin receptors responsible for skin pigmentation or sexual arousal. KPV suppresses NF-κB activation and is transported into intestinal epithelial cells via the PepT1 transporter, which is upregulated during gut inflammation — creating a self-targeting mechanism. Its small size enables oral bioavailability, which is unusual for peptides. It was among the 12 peptides removed from FDA Category 2 on April 15, 2026.

AHK (Alanyl-Histidyl-Lysine) is a tripeptide related to GHK that shares copper-binding properties. It has been studied for its ability to stimulate hair follicle growth and promote wound healing through collagen synthesis and growth factor upregulation. Evidence is limited to in vitro studies and animal models.

AHK-Cu is the copper-complexed form of the AHK tripeptide. The addition of copper enhances its biological activity, particularly in stimulating dermal papilla cells for hair growth and wound healing applications. Used in topical cosmetic formulations.

Decapeptide-12 is a synthetic 10-amino-acid peptide that inhibits melanin production by suppressing tyrosinase activity. It is used in cosmetic formulations for skin brightening and hyperpigmentation treatment, marketed as a safer alternative to hydroquinone.

Melanostatin-DM (Nonapeptide-2) is a synthetic peptide that acts as an MSH antagonist. It reduces melanin transfer and production for skin brightening and hyperpigmentation treatment in cosmetic formulations.

Nonapeptide-1 competes with alpha-MSH at the MC1 receptor on melanocytes, reducing melanin synthesis. It is used in cosmetic skin-lightening products as an alternative to traditional depigmenting agents.

OS-01 is a proprietary peptide developed by OneSkin that targets cellular senescence in skin cells. It was identified through a high-throughput screen of peptide libraries for senolytic/senomorphic activity. Used in the OneSkin topical product line.

Pentapeptide-18 (Leuphasyl) mimics enkephalin activity at presynaptic membranes, reducing neurotransmitter release at the neuromuscular junction for a mild botox-like effect on expression lines. Often combined with Argireline for synergistic effects.

Rigin reduces IL-6 secretion by keratinocytes after UVB exposure, helping reduce chronic low-grade inflammation in aging skin (inflammaging). It is a key component of the Matrixyl 3000 complex alongside Palmitoyl Oligopeptide.

SYN-AKE is a synthetic tripeptide that mimics waglerin-1 from Temple Viper venom. It acts as a muscular nicotinic acetylcholine receptor antagonist, reducing muscle contraction frequency for wrinkle smoothing.