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Glossary Setipiprant

Setipiprant is an investigational oral medication that acts as a selective antagonist of the prostaglandin D2 receptor (DP2), which is implicated in hair loss, particularly androgenetic alopecia. By blocking this receptor, setipiprant aims to inhibit the signaling pathways that contribute to hair follicle miniaturization and hair thinning. Its relevance lies in its potential to promote hair regrowth and improve hair density in individuals experiencing hair loss, distinguishing it from other treatments that may target different biological mechanisms. Ongoing clinical trials are assessing its efficacy and safety in the context of hair restoration.

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research Does Inhibition of Aldose Reductase Contribute to the Anti-Inflammatory Action of Setipiprant?

6 citations , August 2017 in “Physiological Research”

This study suggests that setipiprant's inhibitory effect on aldose reductase may contribute to its anti-inflammatory properties, adding a possible mechanism beyond its known action on the prostaglandin D2 receptor.

research Verification of the Major Metabolic Oxidation Path for the Naphthoyl Group in Chemoattractant Receptor-Homologous Molecule Expressed on Th2 Cells (CRTh2) Antagonist 2-(2-(1-Naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic Acid (Setipiprant/ACT-129968)

6 citations , September 2015 in “Journal of Medicinal Chemistry”

This study synthesized and verified the structures of Setipiprant's major and minor metabolites, confirming their regio- and enantioselectivity from earlier proposals in a clinical study.

research Setipiprant for Androgenetic Alopecia in Males: Results from a Randomized, Double-Blind, Placebo-Controlled Phase 2a Trial

3 citations , October 2021 in “Clinical, Cosmetic and Investigational Dermatology”

This study found that oral setipiprant was safe but did not improve scalp hair growth compared to placebo in men with androgenetic alopecia.

research A bald statement - Current approaches to manipulate miniaturisation focus only on promoting hair growth

30 citations , May 2018 in “Experimental Dermatology”

This article reviews the cellular dynamics affecting dermal papilla size in androgenetic alopecia and suggests targeting DP size could improve therapies, but it presents no new clinical data.

research New drugs under investigation for the treatment of alopecias

26 citations , January 2019 in “Expert Opinion on Investigational Drugs”

This review explored the new and emerging treatments for androgenetic alopecia and alopecia areata, finding that JAK inhibitors show promise for alopecia areata, while advancements in stem-cell research may eventually lead to new and improved treatments for androgenetic alopecia.

research The state‐of‐the‐art in the management of androgenetic alopecia: A review of new therapies and treatment algorithms

1 citations , July 2022 in “JEADV Clinical Practice”

This abstract outlines a guide reviewing both FDA-approved and off-label therapies for androgenetic alopecia and proposes treatment algorithms based on scientific research, highlighting a gap in common treatments for this prevalent condition.

research Topical Prostaglandin Analogues in Androgenetic Alopecia: A Systematic Review of Clinical Evidence

April 2026 in “International Journal of Drug Delivery Technology”

This review concluded that while topical prostaglandin analogues show some potential in treating androgenetic alopecia, evidence is still limited and no products have regulatory approval.

research The physiological and pharmacological roles of prostaglandins in hair growth

October 2022 in “The Korean Journal of Physiology and Pharmacology”

This review discusses the roles of prostaglandins in hair loss and highlights their potential as targets for new alopecia treatments, but reports no new clinical findings.

research peri ‐Xanthenoxanthene (PXX): a Versatile Organic Photocatalyst in Organic Synthesis

11 citations , April 2021 in “Advanced synthesis & catalysis”

This study reports that the dye peri-xanthenoxanthene (PXX) can act as an efficient photocatalyst for various radical reactions, including complex dual catalytic processes and the synthesis of an investigational drug intermediate.

research ADVANCEMENTS IN TREATMENT STRATEGIES FOR ANDROGENETIC ALOPECIA: NOVEL THERAPIES AND FUTURE PERSPECTIVES

December 2025 in “International Journal of Innovative Technologies in Social Science”

This review identified emerging therapies for androgenetic alopecia, such as low-dose oral minoxidil and stem cell-based treatments, which show promise for improved hair loss management but require standardized protocols and large-scale trials for further validation.

research Androgenetic Alopecia: An Update of Treatment Options

110 citations , August 2016 in “Drugs”

Minoxidil is the only FDA-approved topical drug for treating male or female pattern hair loss, and other medications like finasteride and dutasteride can also increase hair growth.

research Female pattern hair loss: A clinical, pathophysiologic, and therapeutic review

66 citations , June 2018 in “International Journal of Women's Dermatology”

This article discusses treatments for female pattern hair loss, highlighting that oral antiandrogens and topical minoxidil can effectively arrest progression and reverse miniaturization in many patients with mild-to-moderate cases, but it reports no new clinical results.

research A review of the treatment of male pattern hair loss

53 citations , February 2020 in “Expert Opinion on Pharmacotherapy”

This review discusses pharmacologic and non-pharmacologic treatments for androgenetic alopecia, noting that current medications like finasteride and minoxidil can slow hair loss but only partially restore hair growth, with early treatment offering better outcomes.

research The therapeutic potential of CRTH2/DP2 beyond allergy and asthma

24 citations , August 2017 in “Prostaglandins & Other Lipid Mediators”

This review discusses the potential roles of prostaglandin D2 and its receptor CRTH2 in various diseases beyond allergies and asthma and reports no new clinical results.

research Conventional and novel stem cell based therapies for androgenic alopecia

22 citations , August 2017 in “Stem cells and cloning”

This review analyzes therapies used for androgenic alopecia, highlighting potential advances from stem cell technologies and regenerative medicine, and reports no new clinical results.

research Novedades terapéuticas en tricología

20 citations , January 2017 in “Actas Dermo-Sifiliográficas”

This review discusses recent therapeutic advances in treating various types of hair loss, including androgenetic alopecia, alopecia areata, frontal fibrosing alopecia, and hair transplant technologies, but reports no new clinical results.

research Treatments options for alopecia

17 citations , August 2015 in “Expert Opinion on Pharmacotherapy”

This article discusses the social and psychological impact of hair disorders and the challenges in their treatment, but reports no new clinical results.

research Structure optimization of tetrahydropyridoindole-based aldose reductase inhibitors improved their efficacy and selectivity

13 citations , October 2017 in “Bioorganic & Medicinal Chemistry”

This study found that compound 3, a tetrahydropyridoindole carboxymethylated at position 5, significantly inhibited sorbitol accumulation in both rat eye lenses and tissues affected by diabetes, indicating its potential as a lead compound for ALR2 inhibition.

research Experimental and early investigational drugs for androgenetic alopecia

11 citations , July 2017 in “Expert Opinion on Investigational Drugs”

This review discusses current and emerging therapeutic strategies for androgenetic alopecia, noting limited evidence but suggesting areas such as prostaglandin analogs, PRP, and progenitor cell therapies as promising future directions.

research Development of Novel Indole-Based Bifunctional Aldose Reductase Inhibitors/Antioxidants as Promising Drugs for the Treatment of Diabetic Complications

9 citations , May 2021 in “Molecules”

This review discusses indole-based bifunctional aldose reductase inhibitors and antioxidants for diabetic complications and chronic inflammation-related pathologies, but reports no new clinical results.

research Prostaglandins in androgenetic alopecia in 12 men and four female

8 citations , February 2019 in “Journal of The European Academy of Dermatology and Venereology”

This letter to the editor about prostaglandins in androgenetic alopecia in men and women reports no new research findings.

research New Treatments for Hair Loss

7 citations , March 2017 in “Actas Dermo-Sifiliográficas”

This review summarizes recent therapeutic advancements in treating various forms of alopecia, including new applications of oral minoxidil, dutasteride, finasteride, Janus kinase inhibitors, and novel hair transplant techniques, without presenting original research results.

research Therapeutic implications of topical cetirizine 1% in treatment of male androgenetic alopecia: A case‐controlled study

5 citations , January 2021 in “Journal of Cosmetic Dermatology”

This study found that topical cetirizine treatment significantly improved hair regrowth and patient satisfaction in male patients with androgenetic alopecia compared to a placebo, highlighting its potential role in treatment.

research Biotechs target stagnant baldness market

3 citations , February 2016 in “Nature Biotechnology”

New drug shows promise for better hair growth in baldness treatment.

research Androgenetic Alopecia

1 citations , July 2018 in “Elsevier eBooks”

This review covers androgenetic alopecia's epidemiology, pathogenesis, current management options, and research trends, concluding that no definitive cure exists despite extensive interest and ongoing genetic research efforts.

research Clinical Trials and Hair Loss

1 citations , July 2018 in “Elsevier eBooks”

This review explores the current treatments for different types of alopecia, emphasizing the need for well-designed clinical trials and highlighting that most therapies are used off-label, as only androgenetic alopecia has FDA-approved drugs.

research Treat androgenetic alopecia with antiandrogens, as well as other pharmacological and non-pharmacological interventions

1 citations , April 2017 in “Drugs & Therapy Perspectives”

This review discusses current treatment options for androgenetic alopecia, noting that most lack robust evidence for efficacy and safety, highlighting the need for more comprehensive studies.

research Use of Castor Oil in Dermatology: A Narrative Review

February 2026 in “Cureus”

This review highlights that castor oil has potential dermatological uses, including enhancing hair luster, reducing hyperpigmentation, and improving skin hydration and elasticity, although rare side effects like contact dermatitis occur, necessitating further research to confirm its effectiveness in these applications.

research A decade of progress in androgenetic alopecia management: Emerging therapies and multimodal strategies

December 2025 in “IP Indian Journal of Clinical and Experimental Dermatology”

This review reports that the treatment of androgenetic alopecia is shifting from single therapies to personalized, multimodal approaches incorporating both traditional and emerging pharmacologics, regenerative strategies, nutraceuticals, cosmeceuticals, and device-based interventions, with combination regimens showing improved outcomes.

research Trends and techniques: a statistical review of hair care product evaluation research

August 2025 in “International Journal of Research in Dermatology”

This review systematically analyzed 22 clinical trials on hair care, finding that while most studies employed appropriate statistical methods, significant inconsistencies in reporting test assumptions and effect sizes may hinder reproducibility, highlighting a need for better standardization and transparency in these research practices.