Delving into the Latest Updates on Chlorotrianisene with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Chloortrianisestrol, Chlorestrolo, Chlorotrianisene (INN)

+ [8]

Target

ER

Action

agonists

Mechanism

ERs agonists(Estrogen receptors agonists)

Therapeutic Areas

Endocrinology and Metabolic DiseaseUrogenital Diseases

Active Indication

HypogonadismProstatic HyperplasiaUterine Hemorrhage

Inactive Indication

Hepatocellular Carcinoma

Originator Organization

Suzhou First Pharmaceutical Co., Ltd.

Active Organization

Suzhou First Pharmaceutical Co., Ltd.

Inactive Organization

Shenzhen SiBiono GeneTech Co. Ltd.Sanofi-Aventis, Inc.Banner Pharmacaps BV

License Organization-

Drug Highest PhaseApproved

First Approval Date

China (01 Jan 1984),

HypogonadismProstatic HyperplasiaUterine Hemorrhage

Regulation-

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Structure/Sequence

Molecular FormulaC23H21ClO3

InChIKeyBFPSDSIWYFKGBC-UHFFFAOYSA-N

CAS Registry569-57-3

Despite encouraging clinical benefits have gained by anti-PD-1 and Lenvatinib combination, in-depth characterizations about the mechanisms of action remain poorly characterized. Furthermore, although the combination of systemic anti-PD-1 or Lenvatinib treatment and locoregional transcatheter arterial chemoembolization (TACE) is widely carried out to treat unresectable HCC in clinical, the efficacies of different combination regimens are uncertain due to limited researches.

METHODS:

We firstly generated murine HCC models to validate the enhanced anti-tumor effects of anti-PD-1 and Lenvatinib combination therapy. Then single cell mass cytometry (CyTOF) was employed to phenotypically reveal their mechanisms of action. After that, we further compared the effectiveness of TACE plus Lenvatinib (i.e., TACE-Len) dual therapy with TACE, Lenvatinib plus anti-PD-1 (i.e., TACE-Len-PD-1) triple therapy as conversion therapy for unresectable HCC.

RESULTS:

Lenvatinib and anti-PD-1 combination could generate activated immune profiles not only by increasing systemic CD4⁺, CD8⁺T cells and B cells proportions, but also by weakening the immune-tolerance functions derived from both immunosuppressive cells (i.e., MDSCs) and co-inhibitory mediators (i.e., PD-L1 and LAG-3). Meanwhile, our study also suggested that TACE-Len-PD-1 triple therapy could achieve better clinical responses with powerful immune profiles for unresectable HCC compared to TACE-Len dual therapy.

CONCLUSIONS:

Our study provided a delicate immune landscape of anti-PD-1and Lenvatinib combination, and we also offered scientific evidences that TACE-Len-PD-1 triple therapy could fulfill better clinical benefits than TACE-Len dual therapy, which is anticipated to provide objective and effective evidences for clinical use.

01 Jun 2025·Hepatobiliary & Pancreatic Diseases International

Adjuvant lenvatinib in combination with transarterial chemoembolization for hepatocellular carcinoma patients with high risk of postoperative recurrence: A multicenter prospective cohort study

Article

Author: Yang, Xin ; Huang, Zhi-Yong ; Xu, Xiao ; Long, Xin ; Zhong, Jian-Hong ; Qin, Lun-Xiu ; Jia, Hu-Liang ; Li, Xiang-Cheng ; Xiang, Bang-De ; Zhang, Xiao-Yun ; Lu, Lu ; Li, Chang-Xian ; Wang, Chao-Qun ; Wen, Tian-Fu ; Liu, Zhi-Kun ; Zhang, Ju-Bo ; Zeng, Yong-Yi ; Luo, Liu-Ping ; Lu, Cai-De ; Zhu, Wen-Wei ; Huang, Jing ; Chen, Jin-Hong

BACKGROUND:

The high recurrent rate after surgery hinders the survival of patients with hepatocellular carcinoma (HCC). This prospective cohort study aimed to evaluate the efficacy and safety of lenvatinib plus transarterial chemoembolization (TACE) as an adjuvant therapy in HCC patients with high risk of recurrence.

METHODS:

Patients were enrolled from eight hepatobiliary centers in China. The primary endpoint was disease-free survival (DFS). The secondary endpoints were overall survival (OS) and safety. Additionally, propensity score matching (PSM) and other three propensity score analyses were performed to balance the potential baseline bias to validate the conclusion. The adverse events (AEs) were recorded throughout the study. The study was registered at ClinicalTrials.gov (NCT03838796).

RESULTS:

A total of 297 patients were enrolled, with 147 in the LEN + TACE group and 150 in the TACE group. Before PSM, the LEN + TACE group achieved significantly better DFS than the TACE group (19.0 vs. 10.0 months, P = 0.011). PSM analysis identified 111 matched pairs. After PSM, the LEN + TACE group also showed better DFS (19.0 vs. 9.0 months, P = 0.018). Other three propensity score analyses yielded similar DFS benefit tendency. Furthermore, favorable OS was also obtained in the LEN + TACE group before PSM. Lenvatinib related AEs of grade 3 or 4 occurred in 28.6% of the patients in the LEN + TACE group.

CONCLUSIONS:

Adjuvant lenvatinib plus TACE might be a promising adjuvant approach for HCC patients with high risk of recurrence, which could significantly prolong DFS and potentially OS with a manageable safety profile.

01 May 2025·JOURNAL OF VASCULAR AND INTERVENTIONAL RADIOLOGY

Histopathologic Response and Oncologic Outcomes After Segmental and Subsegmental Transarterial Chemoembolization and Radioembolization for Hepatocellular Carcinoma

Article

Author: Tabrizian, Parissa ; Kim, Edward ; Shilo, Dan ; Fischman, Aaron M ; Todd, Rachel I ; Sher, Alex ; Patel, Rajesh I ; Nowakowski, Francis S ; Garcia-Reyes, Kirema I ; Patel, Rahul S ; Bishay, Vivian L ; Lookstein, Robert A

INTRODUCTION:

Patients with hepatocellular carcinoma (HCC) are bridged or downstaged to transplant with locoregional therapies (LRT) including transarterial chemoembolization and radioembolization (TARE). Our aim was to compare histopathologic outcomes of TACE and TARE and determine predictors of complete pathologic necrosis (CPN).

METHODS:

HCC treated with segmental (two segments or less) or subsegmental TACE or TARE and transplanted between January 2014 and March 2022 at a single center were retrospectively reviewed. Histopathologic and post-transplant outcomes were assessed within two years. Multivariable logistic regression, propensity score matching (PSM), and Kaplan-Meier survival analysis were performed.

RESULTS:

208 tumors in 148 patients were treated with segmental or subsegmental TACE or TARE. In total, 132 (63.5%) tumors achieved CPN and 156 (75%) had >90% necrosis on explant. CPN by tumor in the TACE and TARE cohorts was 29% and 83.3%, respectively (p<0.0001). Target tumor complete radiologic response (mRECIST) after TARE had a higher positive predictive value (PPV) (89%) compared to TACE (42.9%). PSM analysis of TACE and TARE demonstrated independent predictors of CPN were time from last treatment to transplant, subsegmental injection, and TARE. Patients who achieved overall CPN had significantly longer recurrence free survival at two years (p=0.02).

CONCLUSION:

In a cohort of patients who were bridged or downstaged to LT, there was improved recurrence-free survival in those who achieved complete pathologic necrosis. Overall, TARE was superior to TACE in achieving pathologic necrosis.

1

News (Medical) associated with Chlorotrianisene

10 Nov 2023

·www.biospace.com

AstraZeneca’s Imfinzi, Chemo Combo Meets Endpoint in Phase III Liver Cancer

External view of AstraZeneca’s production plant in Sweden iStock, Roland Magnusson The company’s immunotherapy, in combination with chemotherapy Avastin, showed favorable progression-free survival in a late-stage hepatocellular carcinoma study. Pictured: AstraZeneca production plant/iStock, Roland Magnusson AstraZeneca’s cancer immunotherapy treatment Imfinzi (durvalumab) has shown encouraging survival results for hepatocellular carcinoma patients eligible for embolization in combination with Genentech’s Avastin (bevacizumab) and transarterial chemoembolization. On Thursday, AstraZeneca announced that results from the Phase III Emerald-1 trial “demonstrated a statistically significant clinically meaningful improvement” in the primary endpoint of progression-free survival. The trial is ongoing as AstraZeneca continues to follow the secondary endpoint of overall survival. AstraZeneca reported that the safety pro the combination was “consistent with the known pro each medicine,” with no new safety issues identified. “These positive results for Imfinzi-based treatment in Emerald-1 may bring the potential of immunotherapy to patients with earlier stages of liver cancer. We look forward to discussing these data with regulatory authorities and seeing the survival data mature over time, which will be important as we aim to bring this novel treatment option to patients,” Susan Galbraith, AstraZeneca’s executive vice president of oncology R&D, said in a statement. While no detailed data was provided, AstraZeneca said that the complete dataset will be presented at an unspecified medical meeting and the company will share it with regulatory authorities. “These results for durvalumab plus bevacizumab have the potential to reshape the treatment of this complex disease with a poor prognosis by showing for the first time that adding an immunotherapy combination to [transarterial chemoembolization (TACE)] significantly improves progression-free survival,” Riccardo Lencioni, the trial’s principal investigator and director of the cancer imaging program in the Department of Diagnostic and Interventional Radiology of Pisa University Hospital in Italy, said in a statement. Imfinzi is also being investigated in other gastrointestinal cancers, including a combination with bevacizumab in adjuvant hepatocellular carcinoma (HCC) and a combo with Imjudo, Lenvatinib and TACE in embolization-eligible HCC. The drug is one of the main moneymakers for AstraZeneca, bringing in over $1.1 billion in the third quarter and $3.1 billion for the first nine months of 2023. Imfinzi has also been showing its efficacy in other cancers. Last month, Imfinzi, in combination with chemotherapy, showed positive results in a Phase III trial for patients with resectable, early-stage and locally advanced gastric and gastroesophageal junction cancers. In April 2023, a combination of the drug and Lynparza reached its primary endpoint in a Phase III trial for patients with high-grade epithelial ovarian cancer. Tyler Patchen is a staff writer at BioSpace. You can reach him at tyler.patchen@biospace.com. Follow him on LinkedIn .

Clinical ResultPhase 3ImmunotherapyASCO

100 Deals associated with Chlorotrianisene

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External Link

KEGG	Wiki	ATC	Drug Bank
D00269	Chlorotrianisene	G03CA06	DB00269

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Hypogonadism	China	Suzhou First Pharmaceutical Co., Ltd.	01 Jan 1984
Prostatic Hyperplasia	China	Suzhou First Pharmaceutical Co., Ltd.	01 Jan 1984
Uterine Hemorrhage	China	Suzhou First Pharmaceutical Co., Ltd.	01 Jan 1984

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Hepatocellular Carcinoma	Phase 2	China	Shenzhen SiBiono GeneTech Co. Ltd.	01 Jul 2014

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Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASCO2024	Not Applicable	Unresectable Hepatocellular Carcinoma First line	-	TACE (Surgical resection (SR))	pbexlodhvj(hclrrbmden) = iqqulgxitm aysmuhgoqc (rqxdhnyhqz ) View more	Positive	24 May 2024
				TACE (Thermal ablation (TA))	pbexlodhvj(hclrrbmden) = jbjydekebz aysmuhgoqc (rqxdhnyhqz ) View more
ASCO2024	Not Applicable	Unresectable Hepatocellular Carcinoma	-	Dona-TACE	cejusmxmwl(fbiyvfvxdk) = jhnorqusjd qhakbppexw (ihpmwryred ) View more	Positive	24 May 2024
				Lenva-TACE	cejusmxmwl(fbiyvfvxdk) = andgjwccmc qhakbppexw (ihpmwryred ) View more
EASL_LCS2024	Not Applicable	-	-	TKIs (sorafenib)	nyeckdonza(cbqxpzjiqc) = zmydbwvxlk kvineteeqn (tfybwugqgh )	-	22 Feb 2024
				TACE (doxorubicin+DC-beads)	nyeckdonza(cbqxpzjiqc) = bumehycjkf kvineteeqn (tfybwugqgh )
ASCO2023	Not Applicable	Advanced Hepatocellular Carcinoma Second line	43	TACE+Regorafenib	iqxkjwwfyb(muvjdrywyt) = 16.28% rptpavcrxq (pjjcahvghn ) View more	Positive	31 May 2023
CSCO2021	Not Applicable	Liver Cancer	107	TACE+MWA联合治疗组	mktebxjjaw(tnxlmgrefv) = fiyguvjnay hotaaxykto (rjertejuxk ) View more	-	25 Sep 2021
				单纯TACE组	mktebxjjaw(tnxlmgrefv) = zhmcqmebwy hotaaxykto (rjertejuxk ) View more
CSCO2021	Not Applicable	Liver Cancer	53	TACE联合国产PD-1抑制剂及仑伐替尼	nuekwlvxkp(ezijkcmssf) = qjusvijafa mfprdblwwx (kqwvefdqfj ) View more	Positive	25 Sep 2021
CSCO2020	Not Applicable	Hepatocellular Carcinoma	323	TACE (BCLC B期)	nxfycbhjzd(itvcrfgulg) = eixrgdtxvy lrxcaertsf (liwokpjtkk ) View more	-	19 Sep 2020
				TACE (BCLC C期)	nxfycbhjzd(itvcrfgulg) = vhpbomdfzs lrxcaertsf (liwokpjtkk ) View more
EASL2019	Not Applicable	Hepatocellular Carcinoma First line	-	TACE (Treatment-naive HCC (TN-HCC))	hyfjtdbfiv(kqzuzitrok) = cwfqbpwmcw dfayaxxpkj (wvsqdwnivp ) View more	Positive	12 Apr 2019
				TACE (Recurrent HCC after curative resection (R-HCC))	hyfjtdbfiv(kqzuzitrok) = rackhhwkwo dfayaxxpkj (wvsqdwnivp ) View more
AACR2016	Not Applicable	Hepatocellular Carcinoma	59	TILA-TACE treatment	yrflxgygxp(ldylrnsgsi) = gxdmqwsyqr uobzdkogyl (svpqwvrges ) View more	Positive	15 Jul 2016
ASCO_GI2016	Not Applicable	Hepatocellular Carcinoma	96	1-2 TACE treatments	mmjyazvqqu(nzkxmsclpc) = dlcunsgxnt terdtsphyc (afezswratq )	-	01 Feb 2016
				3-4 TACE treatments	mmjyazvqqu(nzkxmsclpc) = inpgyddsnf terdtsphyc (afezswratq )