SR-16234(SR-16234) - 药物靶点：ERα_专利_临床

概要

基本信息

药物类型

小分子化药

别名

+ [1]

靶点

ERα

作用机制

ERα拮抗剂(雌激素受体α拮抗剂)

治疗领域

肿瘤皮肤和肌肉骨骼疾病泌尿生殖系统疾病

在研适应症-

非在研适应症

乳腺癌复发性乳腺癌子宫内膜异位症+ [1]

原研机构

SRI International

在研机构-

非在研机构

SRI International

Taiho Pharmaceutical Co., Ltd.Tottori University Hospital

最高研发阶段终止临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C33H47NO3

InChIKeyOHCPNHFLPCVWRG-MWSJHZLTSA-N

CAS号229634-97-3

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关联

4

项与 SR-16234 相关的临床试验

JPRN-UMIN000019193 / CompletedN/AIIT

Clinical trial of SR-16234 in patients with endometriosis. - Clinical trial of SR-16234 in patients with endometriosis.

开始日期2015-10-01

申办/合作机构

Tottori University Hospital

JPRN-jRCT2080221712 / Unknown status临床2期

A dose-finding phase II study of TAS-108

开始日期2012-02-20

申办/合作机构

Taiho Pharmaceutical Co., Ltd.

NCT00166543 / Completed临床2期

A Phase II, Randomized, Double-Blinded Efficacy and Safety Study of Three Doses of TAS-108 Administered Orally in Postmenopausal Patients With Locally Advanced or Locally Recurrent Inoperable or Progressive Metastatic Breast Cancer Following Standard First-Line Endocrine Therapy

This study is being done to find out how safe TAS-108 is and how well TAS-108 works on recurrent or recurrent inoperable breast cancer.

开始日期2004-05-01

申办/合作机构

SRI International

[+1]

100 项与 SR-16234 相关的临床结果

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100 项与 SR-16234 相关的转化医学

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100 项与 SR-16234 相关的专利（医药）

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15

项与 SR-16234 相关的文献（医药）

2018-11-01·American Journal of Reproductive Immunology3区 · 医学

New insights into the efficacy of SR‐16234, a selective estrogen receptor modulator, on the growth of murine endometriosis‐like lesions

3区 · 医学

Article

作者: Ohbayashi, Tetsuya ; Nakamura, Kazuomi ; Nagira, Kei ; Khine, Yin Mon ; Harada, Tasuku ; Taniguchi, Fuminori ; Osaki, Mitsuhiko

ProblemTo evaluate the effects of SR‐16234 (SR), a selective estrogen receptor modulator (SERM), on murine endometriosis‐like lesions.Method of studyBALB/c mice (n = 53) were used to establish the murine endometriosis model. Ovariectomized, estradiol replaced, 6‐week‐old murine endometriosis model were injected with lipopolysaccharide (LPS) with or without SR (1 mg/kg/d) or vehicle, over a period of 4 weeks. Upon treatment completion, the endometriosis‐like lesions that developed in the abdominal cavity of mice were counted, measured, and collected. Gene expression of inflammatory cytokines and estrogen receptor (ER) in the lesions was assessed by real‐time RT‐PCR. Immunohistochemical analysis was used to evaluate the effect of SR on cell proliferation, angiogenic activity, inflammation, and NF‐κB phosphorylation.ResultsTreatment with SR significantly reduced the total number and size of lesions per mouse without inducing endometrial growth. In addition, SR downregulated LPS‐enhanced Vegf, Il‐6, Ptgs‐2, and Ccl‐2 and ER mRNA expression in endometriosis‐like lesions. Immunohistochemical analysis demonstrated a decrease in percentage of positive cells of Ki67, and intensity and rate of positive cells of ERα, CD3, F4/80, PECAM by SR treatment. SR also decreased the expression of NF‐κB p65 and phospho‐NF‐κB p65.ConclusionSR has a regressive effect on the development of murine endometriosis‐like lesions.

2017-12-01·Yonago acta medica4区 · 医学

SR-16234, a Novel Selective Estrogen Receptor Modulator for Pain Symptoms with Endometriosis: An Open-label Clinical Trial.

4区 · 医学

Article

作者: Noma, Hisashi ; Ohta, Ikuko ; Taniguchi, Fuminori ; Harada, Tasuku ; Sunada, Hiroshi ; Endo, Yusuke

BackgroundSR-16234 is a selective estrogen receptor modulator (SERM) structurally different from approved SERM and has been reported to have estrogen receptor (ER) α antagonistic activity and strong affinity with a weak partial agonistic activity to ERβ receptor. SR-16234 showed strong inhibitory effects on transplanted endometrial cysts in the endometriosis model of rat and mouse. In this clinical trial, efficacy and safety of SR-16234 have been evaluated in endometriosis patients.MethodsThis trial was an open-label single arm clinical trial. Ten patients with dysmenorrhea and pelvic pain associated with endometriosis and adenomyosis were enrolled in this trial, and received 40 mg of SR-16234 once daily for 12 weeks. The primary endpoint was the visual analogue scale (VAS) of pelvic pain. The secondary endpoints included dysmenorrhea score, pelvic pain score, objective observations (stiffness of Douglas' pouch, limitation of uterine movement, size of ovarian chocolate cysts, thickness of endometrium, and serum CA125 concentration) and safety.ResultsAfter oral administration of SR-16234 40 mg for 12 weeks, there were statistically significant decreases in pelvic pain VAS, total pelvic pain score, total dysmenorrhea score, stiffness of Douglas' pouch, limitation of uterine movement compared with the baseline values.ConclusionThe present trial suggested that a selective estrogen receptor modulator could be used for treatment of pain associated with endometriosis for the first time.

2012-09-01·Cancer Science2区 · 医学

Randomized phase II study of three doses of oral TAS‐108 in postmenopausal patients with metastatic breast cancer

2区 · 医学

ArticleOA

作者: Noguchi, Shinzaburo ; Sato, Nobuaki ; Yamamoto, Naohito ; Tabei, Toshio ; Saeki, Toshiaki ; Saito, Tsuyoshi ; Inaji, Hideo ; Tokuda, Yutaka ; Sato, Yasuyuki ; Saji, Shigehira ; Nakayama, Takahiro ; Kuranami, Masaru ; Takatsuka, Yuichi ; Aogi, Kenjiro ; Yamashita, Hiroko ; Iwata, Hiroji ; Yoshida, Masayuki ; Ikeda, Tadashi ; Watanabe, Kenichi ; Kikuchi, Atsushi

This randomized phase II study was intended to identify the optimal dose of TAS‐108, a novel steroidal antiestrogen, for the treatment of breast cancer in postmenopausal Japanese women. The potential clinical effects of TAS‐108 on the uterus, bone, serum lipids, and hormones were also investigated. Postmenopausal women with hormone receptor‐positive metastatic breast cancer who had previously received one or two endocrine therapies were randomly assigned to one of the three possible dose levels of TAS‐108 (40, 80 or 120 mg/day). Oral TAS‐108 was given daily, and the efficacy and safety of the three doses were evaluated. A total of 97 patients (33, 32, and 32 in the 40‐, 80‐, and 120‐mg groups, respectively) were treated with TAS‐108. The clinical benefit rate was 30.3% for the 40‐mg, 25.0% for the 80‐mg, and 25.0% for the 120‐mg group. The 40‐mg group achieved the prespecified target threshold. TAS‐108 at all dose levels was well tolerated and appeared to have no harmful effects in terms of the variables examined in this study. We conclude that the optimal dose of TAS‐108 among the three doses is 40 mg, once daily, for further studies. JAPIC Clinical Trials Information number: Japic CTI – 121754.

100 项与 SR-16234 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	SR-16234	-	DB05966

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
子宫内膜异位症	临床3期	-	Taiho Pharmaceutical Co., Ltd.	-
复发性乳腺癌	临床2期	美国	Taiho Pharmaceutical Co., Ltd.	2004-05-01
局部晚期乳腺癌	临床2期	美国	Taiho Pharmaceutical Co., Ltd.	2004-05-01
局部晚期乳腺癌	临床2期	美国	SRI International	2004-05-01
乳腺癌	临床2期	日本	Taiho Pharmaceutical Co., Ltd.	-
子宫内膜异位症	临床2期	-	SRI International	-
子宫内膜异位症	临床2期	-	Taiho Pharmaceutical Co., Ltd.	-
子宫内膜异位症	临床2期	-	SRI International	-
子宫内膜异位症	临床2期	日本	Tottori University Hospital	-
子宫内膜异位症	药物发现	日本	Tottori University Hospital	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


ASCO2009	临床2期	乳腺癌	-	TAS-108 40 mg/day	(鹽壓鏇構淵鹹壓顧餘觸) = 蓋鬱願構鬱觸糧築顧構鹽襯遞糧憲鏇繭糧觸鹹 (鹹壓網顧衊蓋製淵壓遞 ) 更多	-	2009-05-20
				TAS-108 80 mg/day	(鹽壓鏇構淵鹹壓顧餘觸) = 醖壓衊鑰選壓齋壓觸醖鹽襯遞糧憲鏇繭糧觸鹹 (鹹壓網顧衊蓋製淵壓遞 ) 更多