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

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

BACKGROUND:

There 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.

RESULTS:

In 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.

SIGNIFICANCE:

This 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·JOURNAL OF CONTROLLED RELEASE

Tannic acid‑cerium nanoenzymes serve as broad-spectrum antioxidants to alleviate acute kidney injury by modulating macrophage polarization, mitophagy and endoplasmic reticulum stress

Article

Author: Zhao, Yi ; Wang, Yanhui ; Cao, Zhong ; Fu, Huayu ; Liang, Zonghao ; Wu, Jun ; Li, Yumin ; Huang, Bangqi

Acute kidney injury (AKI) is a critical condition marked by a rapid decline in renal function, primarily driven by oxidative stress, mitochondrial dysfunction, and inflammation. Despite extensive research, effective therapeutic strategies addressing the complex pathophysiology of AKI remain limited. In this study, we prepared a tannic acid‑cerium nanoenzyme (TA-Ce) and explored its potential for treating AKI. TA-Ce, synthesized via a one-pot method, demonstrated strong reactive oxygen species (ROS) scavenging, therapeutic efficacy, and biocompatibility in vitro and in vivo. TA-Ce, approximately 25.6 nm in size, was obtained by optimizing the molar ratios of TA to Ce and pH conditions, resulting in effective accumulation in the injured kidney. In addition, TA-Ce exhibited broad-spectrum antioxidant ability, capable of scavenging various ROS and alleviating oxidative stress. Notably, TA-Ce outperformed the conventional anti-inflammatory drug N-acetylcysteine (NAC) in both rhabdomyolysis-induced AKI (RM-AKI) and cisplatin-induced AKI (CP-AKI) mouse models. Mechanistic studies in RM-AKI revealed that TA-Ce disrupted the vicious cycle of oxidative stress, mitochondrial damage, endoplasmic reticulum stress, apoptosis, and inflammation. The nanoenzyme restored mitochondrial autophagic flux by inhibiting the P62-LC3 signaling pathway and alleviated endoplasmic reticulum stress by suppressing the IRE1-XBP1s pathway. Consequently, this prevented the downstream activation of the Bcl-2-Bax-Cyt-c-Cleaved Casp-3 apoptotic pathway and the NF-κB inflammatory pathway, ultimately ameliorating RM-AKI. This study lays a strong foundation for the development of metal-polyphenol nanomaterials as a therapeutic strategy for clinical AKI.

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))	wgglcwrfqb(xbsqegusbv) = rwmefjcwpk mytvctuwue (zkloikegxs ) View more	Positive	24 May 2024
				TACE (Thermal ablation (TA))	wgglcwrfqb(xbsqegusbv) = zxyreqovze mytvctuwue (zkloikegxs ) View more
ASCO2024	Not Applicable	Unresectable Hepatocellular Carcinoma	-	Dona-TACE	hlhscqydpl(ywsopwgzvd) = rzsvrjctun znprxoabjt (vgcyrgejkx ) View more	Positive	24 May 2024
				Lenva-TACE	hlhscqydpl(ywsopwgzvd) = isnsyrgzla znprxoabjt (vgcyrgejkx ) View more
EASL_LCS2024	Not Applicable	-	-	TKIs (sorafenib)	dwkzyicmqh(fgputpvogs) = pjyqejtgzj cxkynmbfbv (wmjtbgybqh )	-	22 Feb 2024
				TACE (doxorubicin+DC-beads)	dwkzyicmqh(fgputpvogs) = ddvoviufrd cxkynmbfbv (wmjtbgybqh )
ASCO2023	Not Applicable	Advanced Hepatocellular Carcinoma Second line	43	TACE+Regorafenib	bjqdfbviet(udcdnutraj) = 16.28% hrzdilhflz (pomjpgexcb ) View more	Positive	31 May 2023
CSCO2021	Not Applicable	Liver Cancer	107	TACE+MWA联合治疗组	iqhpekhugy(fdfawbnqav) = bvfvvbhtpp teytvytrxv (haiknnbdvh ) View more	-	25 Sep 2021
				单纯TACE组	iqhpekhugy(fdfawbnqav) = fargizetvj teytvytrxv (haiknnbdvh ) View more
CSCO2021	Not Applicable	Liver Cancer	53	TACE联合国产PD-1抑制剂及仑伐替尼	ilptgkrljb(wukisruwnn) = bxyreeneif jlahdlxebz (mcpjiaxhvl ) View more	Positive	25 Sep 2021
CSCO2020	Not Applicable	Hepatocellular Carcinoma	323	TACE (BCLC B期)	ilvkszenmu(cvazhuqidm) = arzcctoneu kdbpzhrpqn (zznckfecwr ) View more	-	19 Sep 2020
				TACE (BCLC C期)	ilvkszenmu(cvazhuqidm) = acdgxmlbki kdbpzhrpqn (zznckfecwr ) View more
NCT03007225 (treatment of HCC, CTgov)	Phase 4	Hepatocellular Carcinoma	50	Doxorubicin hydrochloride (Group 1)	irmhoayece = lnydauyqhs ompfdmwayj (fyxolncxhb, vhsxqizury - ouukkzacke) View more	-	17 Sep 2020
				Urografin+gentamycin+Doxorubicin hydrochloride+Lipiodol (Group 2)	irmhoayece = lrhfybewgy ompfdmwayj (fyxolncxhb, srqwzybfwf - poqgizjmda) View more
EASL2019	Not Applicable	Hepatocellular Carcinoma First line	-	TACE (Treatment-naive HCC (TN-HCC))	uoknzihzax(dfgnqabdpc) = nvubzfjhsw cturmwtasw (rmzldpytrm ) View more	Positive	12 Apr 2019
				TACE (Recurrent HCC after curative resection (R-HCC))	uoknzihzax(dfgnqabdpc) = nfznipacho cturmwtasw (rmzldpytrm ) View more
AACR2016	Not Applicable	Hepatocellular Carcinoma	59	TILA-TACE treatment	dkttujvlzi(xfaexerrck) = sjxxwuegov htarffolml (diiafcpupk ) View more	Positive	15 Jul 2016