MDI101

MDI 101

IMMEDIATE LICENSING OPPORTUNITY

Patented Retinoid Derivative for Dermatology

Development State: The IND was withdrawn so that MDI 101 could be launched as a cosmetic. Concert LLC was formed to commercialize our skin vitalizing formulas.

Indication: Anti-wrinkle, anti-acne cosmeceutical

Indications/Markets: A drug with the efficacy of Retin A without its irritation, MDI 101, has a $5 million safety testing investment. It is available for immediate licensing.

Patent Status: Patent Numbers US 4,885,311, US 4,994,491. 5,049,584 and US 5,124,356. Global patents issued under PCT filings.

IN VITRO CUTANEOUS DISTRIBUTION OF TOPICAL MDI 101

Jean-Philippe Laugier¹, Gary Henehan² and Howard Maibach¹

Departments of Dermatology¹ and Pharmaceutical Chemistry²

University of California, San Francisco, CA, USA

MDI 101 is a Retinoic Acid derivative which is being developed as a new topical anti-acne agent. Pre-clinical studies have shown lower teratogenicity and better local tolerance than all-trans retinoic acid prepartations.

Our study was aimed at measuring the distribution of the drug in the different layers of the skin after application of MDI 101 0.1% cream.

For this purpose 12, 13 ³H MDI 101 was synthesized from tritiated retinoic acid

and purified by HPLC. MDI 101 cream was spiked with the radioactive compound and applied on human skin from 4 different donors in an in vitro flow-through percutaneous cell system. Drug concentrations at skin surface, in statum corneum, epidermis, dermis and receptor fluid were measured at 6 different time points.

The results show a very low percutaneous penetration of the drug. After 24 hours, less than 0.3% of the dose was recovered in the receptor fluid (mean 0.15% + 0.031), while dermal distribution was 0.223% + 0.116. The percentage recovered in the epidermis is 0.994% + 0.133, and 1.89% + 0.65 in the stratum corneum. Most of the applied drug (96.79% + 0.92) remained on the skin surface at the end of the 24 hour application time.

This drug has a very low percutaneous penetration , but is distributed in the living layers of the skin, thus it has the ability to reach its intended target tissue with low teratogenic risk.