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

BACKGROUNDDespite 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.METHODSWe 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.RESULTSLenvatinib 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.CONCLUSIONSOur 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 May 2025·Analytica Chimica Acta

Development of a natural porcine-estrogen-receptor-based pseudo immunoassay for screening of 13 estrogens in milk and studying its recognition mechanism

Article

Author: Wang, Jian Ping ; Jiang, Zu Qiang ; Cui, Peng Lei

BACKGROUNDThere have been some immunoassays reported for screening of the residues of estrogens in milk, but these methods can only determine one drug because of the limited recognition abilities of the used antibodies. Due to the broad specific recognition ability, receptor can be used as "special antibody" to develop pseudo immunoassay. However, there has been no article reporting the use of estrogen receptor for determination of estrogens in foods of animal origin so far. Furthermore, the recognition mechanism of estrogen receptor for estrogens have not been thoroughly studied.RESULTSIn this study, a type of magnetic probe based on 17β-estradiol was synthesized that was used to produce the natural porcine estrogen receptor with ovarian as the source tissue. Then its recognition mechanisms for 13 estrogens were studied based on the optimal homological model. Results showed it only interacted with estrogens but did not interact with other steroid hormones. Then it was utilized as a broad specific recognition reagent to develop a direct competitive method on 96-well microplate for detection of the 13 drugs in milk. Due to the utilization of streptavidin-biotin labeled horseradish peroxidase as signal amplification system, the sensitivities for the 13 estrogens (limits of detection 0.007-0.0573 ng/mL) were improved for 33-100 folds in comparison with the use of conventional horseradish peroxidase system (limits of detection 0.31-3.53 ng/mL). This method showed no cross-reactivity with other steroid hormones, consistent with the docking result.SIGNIFICANCEThis is the first study reporting the use of magnetic probe to produce natural receptor from animal tissues, and this is also the first study reporting a natural estrogen-receptor-based method for multi-determination of estrogens in food sample. With the guidance of this study, more receptors and related analytical methods for other drugs or small molecules maybe are reported in the future.

01 Apr 2025·Hepatobiliary & Pancreatic Diseases International

Systemic chemotherapy improves outcome of hepatocellular carcinoma patients treated with transarterial chemoembolization

Article

Author: Bian, Li-Fang ; Wu, Jian ; Zhang, Wei-Chen ; Cao, Lin-Ping ; Du, Ke-Yi ; Zhang, Cheng ; Pan, Cheng ; Wu, Dong-Yan ; Guo, Xue-E ; Yu, Han-Xi ; Yu, Jun ; Yu, Song-Feng

BACKGROUNDTransarterial chemoembolization (TACE) based neoadjuvant therapy was proven effective in hepatocellular carcinoma (HCC). Recently, tyrosine kinase inhibitors (TKIs) and immune checkpoint inhibitors (ICIs) also showed promise in HCC treatment. However, the prognostic benefits associated with these treatments remain uncertain. This study aimed to explore the relationship between pathologic response and prognostic features in HCC patients who received neoadjuvant therapy.METHODSHCC patients who received TACE either with or without TKIs/ICIs as neoadjuvant therapy before liver resection were retrospectively collected from the First Affiliated Hospital, Zhejiang University School of Medicine in China. Pathologic response was determined by calculating the proportion of non-viable area within the tumor. Major pathologic response (MPR) was defined as the presence of non-viable tumor cells reaching a minimum of 90%. Complete pathologic response (CPR) was characterized by the absence of viable cells observed in the tumor.RESULTSA total of 481 patients meeting the inclusion criteria were enrolled, with 76 patients (15.8%) achieving CPR and 179 (37.2%) reaching MPR. The median recurrence-free survival (mRFS) in the CPR + MPR group was significantly higher than the non-MPR group (31.3 vs. 25.1 months). The difference in 3-year overall survival (OS) rate was not significant. Multivariate Cox regression analysis identified failure to achieve MPR (hazard ratio = 1.548, 95% confidence interval: 1.122-2.134; P = 0.008), HBsAg positivity (HR = 1.818, 95% CI: 1.062-3.115, P = 0.030), multiple lesions (HR = 2.278, 95% CI: 1.621-3.195, P < 0.001), and baseline tumor size > 5 cm (HR = 1.712, 95% CI: 1.031-2.849, P = 0.038) were independent risk factors for RFS. Subgroup analysis showed that 67 of 93 (72.0%) patients who received the combination of TACE, TKIs, and ICIs achieved MPR + CPR.CONCLUSIONSIn individuals who received TACE-based neoadjuvant therapy for HCC, failure to achieve MPR emerges as an independent risk factor for RFS. Notably, the combination of TACE, TKIs, and ICIs demonstrated the highest rate of MPR.

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 1	China	Shenzhen SiBiono GeneTech Co. Ltd.	01 Jul 2014

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ESMO_IO2023	Not Applicable	Advanced Hepatocellular Carcinoma	73	Tislelizumab plus TKIs	(ypsjxbuzae) = dydbesdcim bbvmemivrd (jswmyiofrz ) View more	-	07 Dec 2023
				Tislelizumab plus TKIs plus TACE	(xsioykowgp) = kkqzrpcthf fheshocoap (jrxrdrxkbj ) View more
113/INT/2021 (ESMO_GI2023)	Not Applicable	Second line	1,381	Lenvatinib	(zjownglckn) = dpsrzesxib evnalroqve (dilkjofbqn ) View more	Positive	01 Jul 2023
				Atezolizumab plus bevacizumab	(zjownglckn) = byylwvfnyt evnalroqve (dilkjofbqn )
ASCO2023	Not Applicable	Advanced Hepatocellular Carcinoma Second line	43	TACE+Regorafenib	yroxqwgsey(agwpskjxct) = 16.28% frmgodfamy (yyusiyaink ) View more	Positive	31 May 2023
ASCO2023	Not Applicable	Unresectable Hepatocellular Carcinoma First line \| Second line	34	Donafenib+TACE+anti-PD1 antibody	(jcsvwnymfw) = Treatment-related adverse events (TRAE) were reported by 30 patients (88.2%), of which 7 patients (20.6%) had grade 3 TRAE. No grade 4 or 5 TRAE was reported. aouxvnloqz (pjojxboztw )	Positive	31 May 2023
ASCO 12023 \| ASCO 22023 Manual	Not Applicable	Advanced Hepatocellular Carcinoma Second line	94	Regorafenib	(kctckabpdx) = mznkxtnlvq nihmevtnux (sizhftxqcp, 0.45 - 7.95)	Positive	26 May 2023
				PD-1 inhibitors+TACE+Regorafenib	(kctckabpdx) = gstxhtlino nihmevtnux (sizhftxqcp, 7.09 - 10.32)
ChiCTR1800018621 (ESMO_ASIA2022) Manual	Phase 4	Hepatocellular Carcinoma	178	apatinib+TACE	(vhhshjzgqp) = ajlbvcttya qdcwpkbchr (ejkqgjmkek, 4.53 - 10.15) View more	Positive	03 Dec 2022
				TACE	(vhhshjzgqp) = zvqvpfipaq qdcwpkbchr (ejkqgjmkek, 2.83 - 4.90) View more
Pubmed Manual	Not Applicable	Hepatocellular Carcinoma First line \| Neoadjuvant	51	TACE+Lenvatinib+Toripalimab	mtcjsvjjgl(cjoctiypsd) = qxyuljteso cbqftuaezs (grvzzjeati ) View more	Positive	02 Sep 2022
				TACE+Lenvatinib	mtcjsvjjgl(cjoctiypsd) = kavwlplyhc cbqftuaezs (grvzzjeati ) View more
Pubmed \| Front Oncol Manual	Not Applicable	Unresectable Hepatocellular Carcinoma	110	TACE+PD-1 Inhibitors+Lenvatinib	(uiuaxxlaxm) = gfnaybaclo pwiahrxijx (djplxcwkwb ) View more	Positive	21 Apr 2022
				TACE	(uiuaxxlaxm) = tsnkdfrpms pwiahrxijx (djplxcwkwb ) View more
EASL_LCS2022	Not Applicable	Unresectable Intrahepatic Cholangiocarcinoma hepatitis B/C	32	TACE and lenvatinib	(gkxkdehyjw) = The occurrence of any-grade adverse events (AEs) was 81%. The most common AEs were decreased appetite (11 [34.3%]), hypertension (10 [31.2%]), and diarrhea (9[28.1%]) sigemtqvvi (siqemhahio )	Positive	03 Feb 2022
				TACE and lenvatinib plus PD-1 inhibitor
CSCO2021	Not Applicable	Liver Cancer	107	TACE+MWA联合治疗组	icavnbhenm(wpukwqjnoo) = rqvluhjvrz mdscnlfeng (isdzasjowa ) View more	-	25 Sep 2021
				单纯TACE组	icavnbhenm(wpukwqjnoo) = avzsjfxybl mdscnlfeng (isdzasjowa ) View more