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WO-2026093364-A1 - AN ACTIVATOR OF PIK3CA FOR STIMULATING HAIR FOLLICLE FORMATION AND CYCLING

WO2026093364A1WO 2026093364 A1WO2026093364 A1WO 2026093364A1WO-2026093364-A1

Abstract

Inventors observed that local application of minoxidil was able to modestly increase the growth of the hair following shaving compared to controls. However, UCL-TRO-1938 application was associated with a significant acceleration of hair growth as assessed by the surface covered by hair following shaving compared to vehicle and minoxidil. They also observed that UCL-TRO-1938 application was associated with a significantly higher number of hair follicles per mm2 and a higher proliferation rate Consistently, immunofluorescence experiments showed an increased phosphorylation rate for AKT on the residue Ser 473 in the UCL-TRO-1938 treatment group compared to others, as well as an increased proliferation assessed with BRDU and finally more expression of hair follicle cells as assessed with CD34, SOX9 and SOX2. The invention relates to a method for stimulating hair follicle formation and cycling in a subject in need thereof comprising a step of administering the subject with a therapeutically effective amount of an activator of PIK3CA.

Inventors

  • CANAUD, Guillaume
  • DIAS CASSACA, Rubina Vanessa

Assignees

  • Institut National de la Santé et de la Recherche Médicale
  • CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
  • ASSISTANCE PUBLIQUE-HÔPITAUX DE PARIS (APHP)
  • UNIVERSITÉ PARIS CITÉ

Dates

Publication Date
20260507
Application Date
20251029
Priority Date
20241030

Claims (15)

  1. 1. A method for stimulating hair follicle formation and cycling in a subject in need thereof comprising a step of administering the subject with a therapeutically effective amount of an activator of PIK3CA.
  2. 2. The method according to claims 1, wherein the PIK3CA activator is UCL-TRO- 1938 or its pharmaceutically acceptable salts.
  3. 3. The method according to claim 1, wherein the subject is afflicted with or susceptible to be afflicted with at least one of health condition selected from the group consisting of but not limited to: aging and hormonal changes, poor nutrition, physical and emotional stress, diseases such as, medications such as chemotherapy.
  4. 4. The method according to claims 1 to 3, wherein the subject is afflicted with or susceptible to be afflicted with alopecia.
  5. 5. The method according to claims 1 to 3, wherein the subject is afflicted with or susceptible to be afflicted with chemotherapy.
  6. 6. The method according to claims 1 to 2, wherein the activator of PIK3CA is administered topically.
  7. 7. The method according to claims 1 to 2, wherein the activator of PIK3CA is formulated as a cream.
  8. 8. A PIK3CA activator and ii) a classical treatment as a combined preparation for simultaneous, separate or sequential use in a method for stimulating hair follicle formation and cycling in a subject in need thereof.
  9. 9. The combined preparation according to claim 8, wherein the classical treatment is selected from the group consisting of but not limited to: minoxidil, finasteride, Dutasteride, Scalp microneedle therapy, also known as micro needling or derma rolling for the scalp, Hair transplantation, Fractional radiofrequency (FRF) therapy, Light therapy (photo biomodulation therapy, cold laser therapy, or red light therapy), Excimer lamp, CO2 laser, Regenerative medicine -based therapy (PRP therapy, Stem cell therapy), Dietary supplementation with natural plant extracts, or controlled shampoo use.
  10. 10. A cosmetic composition comprising an activator of PIK3CA for stimulating hair follicle formation and cycling in a subject in need thereof.
  11. 11. The cosmetic composition according to claim 10, wherein the activator of PIK3CA is UCL-TRO-1938.
  12. 12. A pharmaceutical composition comprising a PIK3CA activator for stimulating hair follicle formation and cycling in a subject in need thereof.
  13. 13. The pharmaceutical composition according to claim 12, wherein the subject is afflicted with or susceptible to be afflicted with alopecia.
  14. 14. A pharmaceutical composition comprising a PIK3CA activator and a classical treatment as a combined preparation for simultaneous, separate or sequential use for stimulating hair follicle formation and cycling in a subject in need thereof.
  15. 15. The pharmaceutical composition according to claims 12 to 14 comprises: UCL- TRO-1938 dissolved in DMSO, cream (Excipial formula lipolotion) and ethanol.

Description

METHODS AND COMPOSITIONS FOR STIMULATING HAIR FOLLICLE FORMATION AND CYCLING FIELD OF THE INVENTION: The invention is in the field of hair growth. More particularly, the invention relates to methods and compositions for stimulating hair follicle formation and cycling. BACKGROUND OF THE INVENTION: Alopecia is a general term for hair loss, and the most common form of this condition is alopecia areata, an autoimmune disease leading to hair loss in patches whom exact trigger remains unknownl. The causes of alopecia are multiples including genetic factors with a male predisposition (called androgenetic alopecia)1. A family history of alopecia increases the likelihood of developing the condition, particularly alopecia areata. Hormonal fluctuations influence hair growth particularly during pregnancy, childbirth, menopause, or thyroid issues. It is also well known that various health conditions can trigger alopecia, including thyroid diseases, autoimmune disorders (e.g., lupus, vitiligo), nutritional deficiencies (e.g., vitamin D, iron) but also significant physical or emotional stress. Finally, skin diseases and certain medications, especially those for cancer, arthritis, depression, and heart conditions, can lead to hair loss as a side effect1. Indeed, alopecia can stem from a complex interplay of genetic predisposition, autoimmune responses, hormonal changes, medical conditions, stress factors, medications, and physical damage to the hair. Understanding these causes is crucial for effective management and treatment strategies for those affected by alopecia. Alopecia treatment is challenging and mainly relies on the treatment of the underlying cause but treatment efficacy is very limitedl. In addition to the original cause of the disease, topical treatment using minoxidil or systemic drug administration such as cystine are frequently usedl. Identification of new treatments are needed. SUMMARY OF THE INVENTION: The invention relates to a method for stimulating hair follicle formation and cycling in a subject in need thereof comprising a step of administering the subject with a therapeutically effective amount of an activator of PIK3CA. In particular, the present invention is defined by the claims. DETAILED DESCRIPTION OF THE INVENTION: Inventors observed that the PIK3CA mutation in stem cells during hair regeneration was able to activate the PIK3CA in cells from the hair follicle leading to an excessive growth of the hair. Inventors decided to test the efficacy of the UCL-TRO-1938 as a topical formulation to improve hair growth in mice. They observed that local application of minoxidil was able to modestly increase the growth of the hair following shaving compared to controls. However, UCL-TRO-1938 application was associated with a significant acceleration of hair growth as assessed by the surface covered by hair following shaving compared to vehicle and minoxidil. The efficacy was dose dependent with a statistically significant increase after 7 days in the concentration 50 pM group. They also observed that UCL-TRO-1938 application was associated with a significantly higher number of hair follicles per mm2 and a higher proliferation rate Consistently, immunofluorescence experiments showed an increased phosphorylation rate for AKT on the residue Ser 473 in the UCL-TRO-1938 treatment group compared to others, as well as an increased proliferation assessed with BRDU and finally more expression of hair follicle cells as assessed with CD34, SOX9 and SOX2. All together these data demonstrate that activating PIK3CA topically with a small molecule favor hair growth and thus can be a new therapeutic strategy to improve alopecia. Method for stimulating hair follicle formation and cycling Accordingly, the present invention relates to a method for stimulating hair follicle formation and cycling in a subject in need thereof comprising a step of administering the subject with a therapeutically effective amount of an activator of PIK3CA. In a particular embodiment, the invention relates to a method for treating hair and follicle loss in a subject in need thereof comprising a step of administering the subject with a therapeutically effective amount of an activator of PIK3CA. As used herein, the term “stimulating” refers to up regulating or activating the growth of hair and follicle. As used herein, the terms “treating” or “treatment” refer to both prophylactic or preventive treatment as well as curative or disease modifying treatment, including treatment of subject at risk of contracting the disease or suspected to have contracted the disease as well as subject who are ill or have been diagnosed as suffering from a disease or medical condition, and includes suppression of clinical relapse. The treatment may be administered to a subject having a medical disorder or who ultimately may acquire the disorder, in order to prevent, cure, delay the onset of, reduce the severity of, or ameliorate one or more symptoms of a disorder or