隨著現(xiàn)代社會生活節(jié)奏加快、工作壓力加大，無關(guān)老幼也不分男女，脫發(fā)已成為新時代的“流行病”。

此前，國家衛(wèi)健委發(fā)布調(diào)查的數(shù)據(jù)顯示，截至2020年末我國脫發(fā)人群已突破2.52億人，占人口總數(shù)的比例高達18%。在龐大的脫發(fā)人群中，又以雄激素性脫發(fā)患者數(shù)量最多，占比90%以上。換言之，全國有超過2.2億人患有雄激素性脫發(fā)。脫發(fā)在歐美國家人群尤為突出，據(jù)美國脫發(fā)協(xié)會調(diào)查報告，2/3的美國男性在35歲時都會經(jīng)歷脫發(fā)的困擾，到50歲左右的男性脫發(fā)現(xiàn)象可高達80%以上。脫發(fā)治療藥物具有廣闊的市場前景，脫發(fā)也需要更加安全有效的毛發(fā)再生產(chǎn)品。

為解決脫發(fā)人群的困擾，生物醫(yī)藥界也在不斷作出努力，力圖研發(fā)出能從根本上解決雄激素性脫發(fā)的創(chuàng)新型藥物。

皮膚適應癥創(chuàng)新藥物研發(fā)企業(yè)嘉興特科羅生物科技有限公司（以下簡稱 “特科羅” www.tkskin.com）就在近日宣布，臨床機構(gòu)已開始在美國為其外用藥 TDM-105795招募雄激素性脫發(fā) (AGA) 患者進行Phase Ib 臨床試驗。有望為脫發(fā)患者帶來新的治療手段、讓患者受益。

創(chuàng)新原研藥臨床數(shù)據(jù)優(yōu)異

“雄激素性脫發(fā)對有效和安全的治療手段有真正的需求。”據(jù)特科羅的首席醫(yī)療官 Arthur P. Bertolino博士介紹，TDM-105795在首個臨床試驗中展示出良好的安全性和耐受性，臨床前數(shù)據(jù)也顯示其在動物模型上能高效地誘導毛發(fā)生長，“公司對一期臨床的結(jié)果備受鼓舞”。

據(jù)介紹，目前，針對雄激素性脫發(fā)的小分子藥物鮮有人問津。獲得美國FDA批準用于脫發(fā)治療的藥物只有米諾地爾（Minoxidil）和非那雄胺（Finasteride）兩款藥物。

不同于上述兩款藥物的作用機理，TDM-105795與毛囊細胞內(nèi)的靶點蛋白結(jié)合后能夠激活休眠的毛囊干細胞，誘導休眠期毛囊進入生長期、延長生長期、縮短退化期和休眠期，以達到治療脫發(fā)的效果。

據(jù)了解，TDM-105795是一款具有全球知識產(chǎn)權(quán)保護、國際領(lǐng)先、治療雄激素性脫發(fā)的小分子藥物。已進行的動物試驗數(shù)據(jù)顯示，TDM-105795起效快，在用藥后3-5日毛發(fā)增長效果顯著，15-18日即可完成整個毛發(fā)生長周期，外用能夠以劑量依賴的方式強效刺激毛發(fā)生長。另外，臨床前研究也表明TDM-105795 外用后系統(tǒng)暴露很低，血漿清除半衰期短，能夠很好地避免并不需要的全身作用。

此前，該藥物臨床I期研究申請（IND154722）已獲得美國FDA許可并立即在美國進入臨床I期研究。

最新消息則顯示，特科羅已宣布臨床機構(gòu)開始在美國為TDM-105795招募雄激素性脫發(fā) (AGA) 患者進行Phase Ib臨床試驗，這一推進是基于此前成功完成了單劑量遞增Phase Ia臨床試驗 (NCT04913519) 。據(jù)介紹，根據(jù)試驗的不良事件、局部皮膚反應，以及用藥后生命指征、安全指標化驗檢測和心電圖的基線變化等方面的報告，TDM-105795在Ia臨床研究沒有發(fā)現(xiàn)任何需要警惕的安全問題。

據(jù)悉，Phase Ib臨床試驗標題為 “隨機、雙盲、安慰劑對照、平行設(shè)組、多劑量遞增研究以評估 TDM-105795 在健康男性AGA患者中的安全性、耐受性和藥代動力學”，是一項為期 28 天的多劑量遞增研究，旨在評估重復外用 TDM-105795的安全性、耐受性及藥代動力學參數(shù)，從而確定用于驗證療效的Phase II 臨床試驗的最適制劑濃度。

華泰證券此前發(fā)布的研報表示，2020年中國脫發(fā)診療市場近200億元，其中藥物約占7億元規(guī)模，其預計未來十年該市場復合增速將超20%，至2031年國內(nèi)脫發(fā)藥物治療市場規(guī)模有望達到155億元。此外，有歐美脫發(fā)患者的巨大人群和市場潛力，手握治療雄激素性脫發(fā)創(chuàng)新型小分子藥物的特科羅也將迎來一片藍海。

專注皮膚病新藥研發(fā)

“我們對治療雄激素性脫發(fā) (AGA) 的 TDM-105795項目在臨床上取得的進展感到興奮，同時期待其它針對不同皮膚疾病的管線化合物以類似的方式進入臨床，我們希望能為解決該疾病領(lǐng)域的市場需求做出重大貢獻。”特科羅首席執(zhí)行官王增全博士如是稱。

公開信息顯示，特科羅是一家專注皮膚病新藥研發(fā)的小分子藥物研發(fā)型創(chuàng)新企業(yè)。公司致力于成為世界領(lǐng)先的皮膚病新藥研發(fā)平臺，研發(fā)上市針對各主要皮膚相關(guān)疾病的First-in-Class或同類最優(yōu)的全球新藥，為全球患者提供基于全新機理的更高效、更安全、成本更低的新藥產(chǎn)品。

目前，特科羅已在雄激素性脫發(fā)以及自身免疫及炎癥性皮膚疾病方面，構(gòu)建了同類首創(chuàng)或同類最佳的藥物候選管線。TDM-105795正是特科羅首發(fā)生發(fā)項目的產(chǎn)品，也是公司推進度最快的產(chǎn)品線。

而在炎癥性皮膚病方面，公司專注于針對不同皮膚疾病種類選擇具有高度差異化的創(chuàng)新Jak小分子抑制劑藥物推進研發(fā)，目前已經(jīng)擁有強大的知識產(chǎn)權(quán)基礎(chǔ)，多個系列具有明顯差異化和競爭特色的化合物在濕疹，銀屑病和紅斑狼瘡等疾病同步推進開發(fā)。

其中，濕疹項目初步藥效結(jié)果顯示候選藥具有藥效明顯優(yōu)勢，藥效強于已經(jīng)上市的PDE4抑制劑，且與糖皮激素類藥對比有同等藥效而沒有激素對皮膚的不良副作用反應。濕疹項目預期在2022年第二季度申報臨床I期。 公司在銀屑病和紅斑狼瘡的藥物候選新品也將逐漸進入臨床試驗申報階段。

Technoderma Medicines Announces Progression of TDM-105795 Phase 1 Clinical Trials for Treatment of Androgenetic Alopecia

SHANGHAI – January 5, 2022 Technoderma Medicines, Inc. (“the Company”), a clinical stage biopharmaceutical company, is pleased to report the Company has begun recruitment for its second Phase 1 clinical trial of topical TDM-105795 in patients with Androgenetic Alopecia (AGA). This follows successful completion of a single dose escalation study (NCT04913519) in which no material clinical safety issues were demonstrated based on reporting of adverse events, local skin reactions and changes from baseline in vital signs, safety labs, and ECG.

This second clinical trial is a 28-day multiple dose escalation study entitled, “A Randomized, Double-Blind, Vehicle-Controlled, Parallel Group, Multi-Dose Escalation Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of TDM-105795 in Healthy Male Subjects with Androgenetic Alopecia”. Its objectives are to evaluate topical TDM-105795 repeated dose safety and toleration and its pharmacokinetics, in order to define formulation strength(s) appropriate for a proof-of-concept Phase 2 study planned to follow.

“There is a real current need for effective and safe medical options to treat Androgenetic Alopecia,” said Arthur P. Bertolino, MD, PhD, MBA, Chief Medical Officer at Technoderma Medicines. “The Company is encouraged by TDM-105795 safety and toleration demonstrated in its first clinical trial and by preclinical data showing robust induction of hair growth in an animal model.”

Dr. Zengquan Wang, Chief Executive Officer at Technoderma Medicines commented, “We are excited about the progress being made with the TDM-105795 AGA program advancing in the clinic. In addition, we look forward to additional pipeline compounds likewise following into the clinic for treatment of various dermatologic diseases. We hope to contribute significantly to addressing the market need in this therapy area.”

About TDM-105795

TDM105795 is a small molecule drug candidate being developed as a topical drug to promote hair growth. Preclinical assessment of TDM105795 indicates that TDM105795 has poor systemic absorption following topical application and a short elimination half-life, features well-suited to avoid unwanted systemic effects. Moreover, in vivo efficacy studies in C3H mice showed that TDM105795 was able to potently stimulate hair growth in a dose-dependent manner when applied topically. This is likely because TDM105795 is able to activate dormant hair follicle stem cells and induce anagen (growth phase) in telogen (resting phase) hair follicles when binding to hair follicle cell target receptor proteins.

About Androgenetic Alopecia (AGA)

Androgenetic Alopecia (AGA), also called male or female pattern baldness, is the most common hair loss condition affecting both men and women, with a higher incidence in men. While more than half of adult males suffer from AGA, this rate increases to 80% in men at age 50 and above. Male AGA is characterized by receding hairline and baldness on the top and front of the head. Female AGA is usually manifested as hair density thinning on the top and crown of the head. As a degenerative disorder with etiology largely unknown, genetic, psychological and mental, endocrinologic and metabolic factors may play a role. The pathogenesis underlying AGA has been linked to hyperactivation of androgen receptors in hair follicle cells, rendering resting hair follicles unable to re-enter the growth phase and undergoing miniaturization.

About Technoderma Medicines

Technoderma Medicines, Inc. is a privately held clinical stage biopharmaceutical company located in Jiaxing Xiuzhou Biomedicine Guoqian Park, Shanghai. Its current core programs focus on development of innovative therapies for Androgenetic Alopecia, Atopic Dermatitis, Lupus Erythematosus and Psoriasis. Its "first-in-class" small molecule drug candidate TDM-105795 for Androgenetic Alopecia is currently undergoing clinical testing. Technoderma’s JAK1/TYK2 inhibitor for Atopic Dermatitis is completing late-stage preclinical testing and it has a target IND filing date in mid-year 2022. The pipeline targets dermatologic indications.