Decapeptide-12

Also known as: Lumixyl, Lumixyl peptide, YRSRKYSSWY

Evidence: Clinical

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Overview

Synthetic decapeptide (YRSRKYSSWY, Lumixyl) that competitively inhibits tyrosinase in vitro; a 5-person split-face placebo-controlled pilot and open-label studies report lighter melasma.

Decapeptide-12 came from an oligopeptide library screened by Hantash's group for tyrosinase inhibitors that are not toxic to melanocytes; the 10-residue hit inhibited mushroom tyrosinase with an IC50 of 40 microM (hydroquinone 680 microM) and cut melanocyte melanin 43% over 7 days (Abu Ubeid et al., 2009). It is sold as Lumixyl. Human data: a split-face, double-blind, placebo-controlled pilot in five women with melasma at 0.01% twice daily for 16 weeks (Hantash and Jimenez, 2009), then open-label studies of a regimen pairing it with 20% glycolic acid and sunscreen (Kassim et al., 2012; Ramírez et al., 2013). Most studies come from the developer.

Benefits

Melasma lightening (split-face RCT, n=5; open-label, n=33), photodamage pigment clearance (open-label, n=13), tyrosinase inhibition and lower melanocyte melanin (in vitro)

Dosing reference

Research dose: Topical, 0.01% (w/w) cream in all published human studies. No oral or injectable dose exists.

Topical cream applied to pigmented areas. Studies ran 16 to 24 weeks; most paired it with glycolic acid and sunscreen, so effects of the peptide alone come only from the five-person pilot.

Mechanism

Competitive inhibition of tyrosinase. In kinetic studies the decapeptide competitively inhibited mushroom tyrosinase (IC50 40 microM) and at 100 microM inhibited human tyrosinase by 25 to 35%, with substrate-dependent results suggesting two catalytic sites. Melanin in cultured human melanocytes fell 43% after 7 days without effects on proliferation or viability (Abu Ubeid et al., 2009). Claims of action at multiple steps of melanogenesis or superiority to hydroquinone in people have no published head-to-head data.

Evidence

Clinical: at least one published human trial or an approved drug

Inhibited mushroom tyrosinase (IC50 40 microM vs 680 microM for hydroquinone) and lowered melanocyte melanin 43% without cytotoxicity (Abu Ubeid et al., 2009)
Split-face, double-blind, placebo-controlled pilot: 0.01% twice daily for 16 weeks in five women with recalcitrant melasma, all improved, no irritation (Hantash and Jimenez, 2009)
Open-label, 33 Hispanic women: a 0.01% cream plus 20% glycolic acid and sunscreen lowered MASI scores 60% by week 16 (Ramírez et al., 2013)
Open-label, 13 women with photodamage pigment: 38.5% reached complete clearance at 24 weeks on the same regimen (Kassim et al., 2012)
Human-trial status: one randomized placebo-controlled pilot (n=5); other studies are open-label multi-product regimens, mostly from the developer's group

References

Side effects

No irritation or allergy in the five-person RCT (Hantash and Jimenez, 2009) and no adverse events in the 33-person open-label study (Ramírez et al., 2013). No cytotoxicity to cultured melanocytes at 100 microM (Abu Ubeid et al., 2009). Commonly reported (anecdotal): dryness or redness, mostly attributed to the glycolic acid in combined regimens.

Storage

Storage: Room temperature, away from light
Lyophilized: 2 years at room temp
Reconstituted: N/A (ready to use)

Pharmacology

Half-life: No published pharmacokinetic data in any species
Bioavailability: Not measured in any species; skin penetration of decapeptide-12 has not been published
Molecular weight: 1395.54 Da
Sequence: YRSRKYSSWY (Tyr-Arg-Ser-Arg-Lys-Tyr-Ser-Ser-Trp-Tyr)