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Product Name | SETIPIPRANT |
CAS No. | 866460-33-5 |
Molecular Formula | C24H19FN2O3 |
Molecular Weight | 402.42 |
Colour | white |
Form | powder |
Introduction
Setipiprant (INN) (developmental code names ACT-129,968, KYTH-105) is a drug originally developed by Actelion which acts as a selective, orally available antagonist of the prostaglandin D2 receptor 2 (DP2). It was initially researched as a treatment for allergies and inflammatory disorders, particularly asthma, but despite being well tolerated in clinical trials and showing reasonable efficacy against allergen-induced airway responses in asthmatic patients, it failed to show sufficient advantages over existing drugs and was discontinued from further development in this application.However, following the discovery in 2012 that the prostaglandin D2 receptor (DP/PGD2) is expressed at high levels in the scalp of men affected by male pattern baldness, the rights to setipiprant were acquired by Kythera with a view to potentially developing this drug as a novel treatment for baldness, with a previously unexploited mechanism of action. While it is too early to tell whether setipiprant will be an effective treatment for this condition, the favorable pharmacokinetics and relative lack of side effects seen in earlier clinical trials mean that fresh clinical trials for this new application can be conducted fairly quickly.
A phase 2A study is underway to evaluate the safety, tolerability, and efficacy of oral setipiprant relative to a placebo and the active comparator, finasteride, in 18 to 41 years old males with androgenetic alopecia.
Function
1. For maximum effect, the solution should be in contact with the scalp for hours before being washed out. It does not seem capable of reducing DHT or the enzyme responsible for its accumulation around the hair follicle, 5-aliha reductase,
2. which are the main causes of male pattern baldness in genetically susceptible individuals. Therefore, when treatment is stopped, the DHT already accumlated around the follicle has its expected effect, and the follicle usually shrinks again and
eventually dies.
3. Setipiprant powder can promote hair regrowth,slow or stop hair loss and treat high blood pressure.
Setipiprant needs to be applied once or twice daily for hair to be maintained.
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