Selective Receptor Modulators for Skin Depigmentation

Small-molecule compositions modulate non-canonical sex steroid receptors to decrease, prevent, or reverse skin pigmentation gain in mammalian subjects.
Problem:
Skin hyperpigmentation can arise from pregnancy, hormones, inflammatory conditions, or skin injury. Existing approaches may not address receptor pathways that regulate melanocyte pigmentation. Melanin reduction methods also need formulations suitable for skin delivery. Improved compositions are needed for localized treatment of pigmentary skin changes.
Solution:
The technology uses compounds that antagonize GPER or agonize PAQR7 to modulate skin pigmentation. These compounds are formulated in pharmaceutical compositions for topical or transdermal administration. In some embodiments, the compounds do not bind canonical nuclear estrogen or progesterone receptors. The compositions are described for decreasing, preventing, or reversing gain of skin pigmentation.
Technology:
The platform includes small molecules such as G-15 or G-36 as GPER antagonists and CH2P4 as a PAQR7 agonist. The compositions include pharmaceutically acceptable excipients and can include sun-blocking agents or sunscreen lotion. Topical formulations can be prepared as lotions, creams, ointments, pastes, solutions, suspensions, or transdermal patches. The methods apply these compositions to subjects with pigmentary skin changes associated with hormonal, inflammatory, or injury-related conditions.
Advantages:

• Uses non-canonical sex steroid receptor modulation to alter skin pigmentation.
• Supports both GPER antagonist and PAQR7 agonist compound classes.
• Enables topical or transdermal administration for localized skin treatment.
• Includes formulation options with pharmaceutically acceptable excipients and optional sun-blocking components.
• Describes compounds that do not bind canonical nuclear estrogen or progesterone receptors in certain embodiments.

Applications:

• Hyperpigmentation Treatment: Decreases, prevents, or reverses gain of skin pigmentation in subjects with pigmentary skin changes.
• Hormone-Associated Pigmentation: Treats pigmentary changes associated with pregnancy, oral contraceptive use, or endogenous estrogens in females.
• Inflammatory Skin Conditions: Addresses pigmentation changes associated with eczema, psoriasis, lupus, sarcoidosis, pityriasis, or lichen planus.
• Scar-Related Pigmentation: Reduces pigmentation associated with chemical burn scars, sun burn scars, or thermal burn scars.

Intellectual Property:

• US 11,236,074
• US 11,987,576

Docket : 16-7869
Desired Partnerships:

• License
• Co-Development