KX-826 is a topical androgen receptor (AR) antagonist, the world's first AR antagonist for the treatment of alopecia areata to enter registrational Phase III clinical trials.KX-826 works by competing with dihydrotestosterone (DHT) for binding to the AR, thereby locally blocking androgen-mediated signaling to limit miniaturization of hair follicles and promote growth of terminal hair.KX-826 reaches the circulatory system and is rapidly metabolized to inactivated metabolites, with less effect on the systemic AR signaling pathway and a favorable safety profile.

 

Basic Information

 

Cosmetic Name: Methylpyridinyl Fluoromethoxybenzonitrile Dimethyloxothiooxoimidazolidine

Water solubility: insoluble in water

Appearance: Off-white to light yellow powder

 

Physical and Chemical Properties

 

Appearance: Off-white to light yellow powder

Solubility: insoluble in water

 

Usage

 

Mainly used in the treatment of androgenetic alopecia and acne vulgaris.

 

Mechanism of action

 

It is found that the activity of 5α-reductase in scalp follicle type II is significantly higher in AGA alopecia than in non-alopecia area, and the 5α-reductase in the tissue can convert testosterone to 5α-dihydrotestosterone (DHT).

 

Dihydrotestosterone (DHT) and androgen receptors on the hair follicle cells, causing a series of reactions, making the hair follicle miniaturization, anagen hair gradually thinning, hair growth cycle is shortened, the original coarse black hair gradually become colorful cui hair, and ultimately due to the disappearance of hair follicle shrinkage, the cui hair fall, the formation of baldness. The process is usually accompanied by scalp sebaceous gland hyperplasia, increased oil secretion symptoms.

 

KX-826 is a kind of androgen receptor antagonist, through the competition of dihydrotestosterone (DHT) and the target tissue androgen receptor binding, blocking the androgen-mediated signaling, can effectively reduce the impact of androgen on the hair follicle, so that the hair follicle cells to restore the health of the effect of anti-baldness. Persistent use can regulate the hair growth cycle, extend the growth period of hair follicles, and form a healthy hair cycle.

 

Dosage

 

For external use on the scalp, 1 time per day in the morning and 1 time in the evening, each time in the target area spray 6-8 times, and gently massage with the fingertips for 2 minutes

 

Indications

 

Androgenetic alopecia, oil control, anti-hair loss, hair growth needs of the crowd

 

Precautions

 

1. This product is limited to topical use on the scalp of patients with androgenetic alopecia, and cannot be taken orally or applied to other areas of the body.

2. When using this product, you should pay attention to observe any signs of systemic or local effects that may be caused by this product. In the event of side effects or serious dermatologic reactions suspected to be caused by the use of this product, the patient should suspend use of this product and contact a physician.

3. This product may burn and irritate the eyes. In the event of contact with sensitive surfaces (eyes, abraded areas, mucous membranes), the area should be flushed with plenty of water.

4. This product should not be used with caution in children, pregnant women, nursing mothers, or persons over 65 years of age, and should be used in consultation with a physician or pharmacist.

5. This product should not be overdosed (more than 7 sprays per time, or more than twice a day), if overdose, and serious adverse reactions should be immediately seek medical attention.

6. This product is prohibited for those who are allergic to this product, allergic persons should be cautious.

7. Prohibit the use of this product when the properties of the product have changed.

8. Keep this product out of the reach of children. 9.

9. If you are using other drugs, please consult your physician or pharmacist before using this product.

10. Avoid outdoor exposure to sunlight at the site of application.

 

Adverse reactions

 

Some users may experience itching and contact dermatitis, as well as mild localized skin irritation. During use, close attention should be paid to the health condition, and if there is any abnormality, please seek medical advice.

 

Clinical Trial

 

The Phase II clinical trial, with Professor Zhang Jianzhong, Director of the Department of Dermatology at Peking University People's Hospital, as the principal investigator (Leading PI), was a multicenter, randomized, double-blind, placebo-controlled study to evaluate the efficacy and safety of KX-826 for the treatment of adult female patients with androgenetic alopecia. The primary endpoint of the clinical trial was the mean change from baseline in TAHC compared to placebo at 24 weeks of treatment. The majority of adverse events (TEAE) that occurred during the study were mild and similar to the placebo group. There were no TEAEs or deaths that led to withdrawal from the trial.

 

On May 11, 2023, the Phase II clinical trial of KX-826 for the treatment of androgenetic alopecia in men (alopecia areata or AGA) in the U.S. was successfully completed with statistically and clinically significant results and a favorable safety profile.

 

On November 27, 2023, Pioneering Pharmaceuticals issued an announcement disclosing that the Chinese Phase III clinical trial of KX-826 for the topical treatment of male androgenetic alopecia has read out top-line data: the drug demonstrated excellent safety profile, and after 24 weeks of treatment, the TAHC results in the KX-826 group showed statistically significant promotion of hair growth in the KX-826 group as compared to baseline.

 

This Phase III clinical trial is a multicenter, randomized, double-blind, placebo-controlled study to evaluate the efficacy and safety of topical 0.5% concentration of KX-826 used twice daily for the treatment of Chinese adult male alopecia patients.”

 

Safety Terms

 

S26: In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.

In case of contact with eyes, rinse immediately with plenty of water and seek medical advice

 

Risk terms

 

R22: Harmful if swallowed.

Harmful if swallowed.

 

R36/37/38: Irritating to eyes, respiratory system and skin.

Irritating to eyes, respiratory system and skin