Researchers using a novel transdermal drug delivery system to deliver tranexamic acid deep into melasma patients’ skin found the technology-assisted treatment quickly and notably reduced the skin pigmentation of moderate-to-severe melasma.
The delivery platform called DYV600 (Dyve Biosciences) ushers drugs for therapeutic and aesthetic indications through two key transdermal doors: the stratum corneum lipid matrix and tight junctions, according to data presented from Dyve’s melasma drug candidate’s human proof-of-concept study presented in May at the Aesthetics Innovation Summit 2019.
The technology targets melasma at the source by targeting deep melanocytes — reaching beyond the ability of current topicals used to treat melasma, according to the presentation.
The company’s recent feasibility study for DYV600 showed resolution of moderate-to-severe melasma in as quickly as four weeks of treatment when used with or without turnover enhancers, according to Ryan Beal, M.D., Dyve Biosciences’ CEO and cofounder.
"Currently, there is only modest efficacy of existing topical options for the treatment of melasma. Dyve’s DYV600 is addressing those unmet needs, which affect 50% to 70% of post-partum women. Data from our most recently completed melasma human proof-of-concept trial demonstrates how we can modulate our technology to optimize transdermal drug delivery," says Dr. Beal. “We believe this has the potential to introduce a step-change in efficacy for the treatment of hyperpigmentation. The learnings we’ve made in the development of DYV600 are also enabling other disruptive innovations across therapeutic and aesthetic indications.”
Among the aesthetic programs in Dyve’s pipeline are human proof of concept data for the treatment of rhytids, adipolysis of the flanks and alopecia. Therapeutically, the company is studying the technology for over-the-counter analgesia and erythema. Dyve also has a late-stage clinical program, (DYV700) for the treatment of gout.
“Melasma is a difficult condition to treat. A lot of it is patient-dependent on absolute diligence with sun protection,” says Joel Cohen, M.D., director of AboutSkin Dermatology and DermSurgery, in Greenwood Village, Colo., and associate clinical professor of dermatology University of California at Irvine.
Dr. Cohen says topical treatments such as mainstay hydroquinone work. But concerns about the long-term use of hydroquinone have resulted in many dermatologists restricting hydroquinone treatment to three or four months at a time.
“People have long looked for hydroquinone alternatives that would be as effective. If we look specifically at some of the products out there, topical retinoids can be helpful for melasma. Topical kojic acid and some chemical peels, including glycolic acid, salicylic acid and Jessner solution, also can help,” says Dr. Cohen, a clinical trial investigator for Dyve. “But wouldn’t it be great to have a product that’s effective like hydroquinone that you could use long-term? Tranexamic acid has jumped onto the aesthetic radar, and people are looking for ways to effectively treat melasma by incorporating tranexamic acid. Dyve’s proprietary delivery system seems to enhance tranexamic acid penetration and efficacy, and it could be what we’re looking for.”
There is research to suggest tranexamic acid alone is as effective as topical hydroquinone for melasma treatment up to three months. In a study comparing the efficacy of topical 5% tranexamic acid solution to 3% hydroquinone cream in the treatment of melasma on Indian skin, researchers found that after 12 weeks of treatment the difference between the two groups was not significant. In the study of 100 patients, however, patient satisfaction scores were significantly higher in the tranexamic acid group, according to the study published in January-March 2019 Journal of Cutaneous and Aesthetic Surgery.
Dyve’s human proof-of-concept trial demonstrates how the company can modulate its technology to optimize transdermal drug delivery and offer patients an effective option to injections, oral drugs or ineffective topicals, according to Dr. Beal.
"We just completed enrollment in our current proof-of-concept study for DYV600 and look forward to a data read out in the second half of 2019. The study is aimed to non-invasively deliver active ingredients deep — to stop pigment production at its source. We want to create a fast-acting on-going use topical, without adverse events, that matches or exceeds current invasive and topical treatment efficacy," Dr. Beal says.
Janney MS, Subramaniyan R, Dabas R, Lal S, Das NM, Godara SK. A Randomized Controlled Study Comparing the Efficacy of Topical 5% Tranexamic Acid Solution versus 3% Hydroquinone Cream in Melasma. J Cutan Aesthet Surg. 2019;12(1):63-67.