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

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

CN (01 Jan 1984),

HypogonadismProstatic HyperplasiaUterine Hemorrhage

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC23H21ClO3

InChIKeyBFPSDSIWYFKGBC-UHFFFAOYSA-N

CAS Registry569-57-3

INTRODUCTION AND OBJECTIVESWe initiated this study to explore the efficacy of camrelizumab combined with transcatheter arterial chemoembolization (TACE) plus sorafenib or lenvatinib versus TACE plus sorafenib or Lenvatinib for unresectable hepatocellular carcinoma (HCC).MATERIALS AND METHODSFrom June 2019 to November 2022, 127 advanced HCC patients were retrospectively analyzed in this study. This consisted of 44 patients that received camrelizumab plus TACE plus sorafenib or lenvatinib (triple therapy group) and 83 patients that received TACE plus sorafenib or lenvatinib (double treatment group). The overall survival (OS), progression-free survival (PFS), objective response rate (ORR), and disease control rate (DCR) were compared between the two patient groups.RESULTSOur findings demonstrated that patients received the triple therapy exhibited superior median OS (15.8 vs. 10.3 months, P=0.0011) and median PFS (7.2 vs. 5.2 months, P=0.019) compared to the double treatment group. In addition, the triple therapy group exhibited better 6-month (93.5% vs. 66.3%), 12-month (67.2% vs. 36.3%), and 24-month (17.2% vs. 7.6%) survival rates than the double treatment group. However, the ORR (43.2% vs. 28.9%, P = 0.106) and DCR (93.2% vs. 81.9%, P = 0.084) of the two groups were similar. Subgroup analysis showed that compared with the double treatment group, the triple therapy group had a better mOS for HCC with HBV (15.8 vs. 9.6 months, P = 0.0015) and tumor diameter ≥ 5cm (15.3 vs. 9.6 months, P = 0.00055).CONCLUSIONSCamrelizumab plus TACE and sorafenib or lenvatinib may be a promising treatment approach for the clinical management of unresectable HCC patients.

01 Feb 2025·International Immunopharmacology

Immunotherapy improved the efficacy of TACE or TACE plus MTTs in HCC patients: A meta-analysis

Review

Author: Guo, Yusheng ; Gong, Bingxin ; Li, Tianxiang ; Kan, Xuefeng ; Zheng, Chuansheng ; Li, Yi ; Yang, Lian ; Pan, Zhenliang

BACKGROUNDAlthough several studies have compared the efficacy and safety of transarterial chemoembolization (TACE) without immune checkpoint inhibitors (ICIs) and TACE with ICIs, there is still a lack of meta-analysis.METHODSPubMed, Embase, Web of Science, and the Cochrane Library were searched until July 2023 for studies comparing the efficacy and safety of TACE without ICIs (TACE ± molecular targeted therapies [MTTs]) and TACE without ICIs (TACE ± MTTs + ICIs). Outcomes included overall survival (OS), progression-free survival (PFS), objective response rate (ORR), disease control rate (DCR), and adverse events (AEs).RESULTSA total of 20 studies involving 2587 HCC patients were included in the meta-analysis. Eighteen studies including 2116 patients looked at the difference in OS between TACE ± MTTs or TACE ± MTTs + ICIs. Compared with TACE ± MTTs, TACE ± MTTs + ICIs were associated with significantly improved OS (HR, 0.37; 95 % CI, 0.30-0.46). Thirteen studies including 1650 patients investigated the difference in PFS between TACE ± MTTs or TACE ± MTTs + ICIs. The outcome showed that TACE ± MTTs + ICIs were associated with longer PFS (HR, 0.50; 95 % CI, 0.41-0.61, P < 0.001). Eighteen studies including 1971 patients investigated the difference in tumor response (ORR and DCR) between TACE ± MTTs or TACE ± MTTs + ICIs. The outcomes indicated that TACE ± MTTs + ICIs bring higher ORR and DCR compared to TACE ± MTTs (ORR: OR, 2.39; 95 % CI, 1.97-2.89, P < 0.001; DCR: OR, 2.30; 95 % CI, 1.84-2.88). Moreover, to look at the direct impact of ICIs, we investigated the difference in OS, PFS, ORR, DCR, AEs, and severe AEs between TACE + tyrosine kinase inhibitors (TKIs) and TACE + TKIs + ICIs. The results indicated that the addition of ICIs provided longer OS, longer PFS, higher ORR, and higher DCR, but did not bring additional AEs and severe AEs.CONCLUSIONImmune checkpoint inhibitors improved the efficacy of TACE or TACE plus MTTs and prolonged the survival of patients with hepatocellular carcinoma. Meanwhile, the addition of immune checkpoint inhibitors to the TACE + TKIs did not bring additional adverse events.

01 Feb 2025·Annals of Surgical Oncology

Hierarchically Positioning Laparoscopic Microwave Ablation in the Therapeutic Span of Early Hepatocellular Carcinoma: A Real-Life Comparative Analysis

Article

Author: Biselli, Maurizio ; Grassini, Maria Vittoria ; Ponziani, Francesca Romana ; Zappa, Marco Antonio ; Cammà, Calogero ; Malerba, Antonio ; Lazzari, Sara ; Casadei Gardini, Andrea ; Ortenzi, Mariano ; Caregari, Silvia ; Stornello, Caterina ; Foschi, Francesco Giuseppe ; Billato, Ilaria ; Benevento, Francesca ; Brolese, Marco ; Golfieri, Rita ; Conti, Fabio ; Grova, Mauro ; Coratella, Fabio ; Chegai, Fabrizio ; Cossiga, Valentina ; Dambina, Valeria ; Migliano, Maria Teresa ; Celsa, Ciro ; Capasso, Mario ; Marra, Fabio ; Inno, Alessandro ; Campani, Claudia ; Giacchetto, Carmelo Marco ; Coccoli, Pietro ; Sacco, Rodolfo ; Palano, Giorgio ; Pelizzaro, Filippo ; Barabino, Matteo ; Furlanetto, Alessandro ; Piscaglia, Fabio ; Dajti, Elton ; Lani, Lorenzo ; Domenicali, Marco ; Stefanini, Benedetta ; Cappelli, Alberta ; Napoli, Lucia ; Borghi, Alberto ; Pelecca, Giorgio ; Cavoli, Tancredi Li ; Ravaioli, Federico ; Sangiovanni, Angelo ; Missale, Gabriele ; Adotti, Valentina ; Cabibbo, Giuseppe ; Masotto, Alberto ; Bevilacqua, Vittoria ; Vidili, Gianpaolo ; Cela, Ester Marina ; Bertellini, Federica ; Rosi, Martina ; Santambrogio, Roberto ; Penzo, Barbara ; Rabatelli, Paola ; Renzulli, Matteo ; Brunetto, Maurizia Rossana ; Ballo, Mattia ; Giuffrida, Paolo ; Mosconi, Cristina ; Facciorusso, Antonio ; Trevisani, Franco ; Olivani, Andrea ; Iavarone, Massimo ; Marchetti, Fabiana ; Sauchella, Assunta ; de Matthaeis, Nicoletta ; Santi, Valentina ; Allegrini, Gloria ; Morisco, Filomena ; Rancatore, Gabriele ; Granito, Alessandro ; Saitta, Carlo ; Biasini, Elisabetta ; Caraceni, Paolo ; Vitale, Alessandro ; Pinto, Elisa ; Dell’Isola, Serena ; Farinati, Fabio ; Muratori, Luca ; Lauria, Valentina ; Marchini, Andrea ; Cillo, Umberto ; Ghittoni, Giorgia

BACKGROUNDLaparoscopic microwave ablation (LMWA) has yet to gain a specific place in treatment guidelines for early hepatocellular carcinoma (HCC). This study compared the outcomes of LMWA and trans-arterial chemoembolization (TACE) for early non-resectable patients with HCC, taking percutaneous radiofrequency ablation (PRFA) as the reference treatment.METHODSA retrospective multicenter observational study was conducted, enrolling non-transplantable, non-resectable patients who had early HCC treated with LMWA (n = 658) from Padua and Milan centers, and with PRFA (n = 844), and TACE (n = 425) from the ITA.LI.CA multicenter database. The matching-adjusted indirect comparison (MAIC) method was used to obtain weighted LMWA and TACE populations similar to the reference PRFA population.RESULTSLaparoscopic ablation showed an excellent safety profile, and MAIC-weighted early postoperative deaths were comparable among the groups. The MAIC-weighted overall survival was similar between the LMWA (1-, 3-, and 5 year survival of 91.0 %, 67.9 %, 47.0 %, respectively) and PRFA (1-, 3- and 5 year survivals of 90.0 %, 64.7 %, 46.6 %, respectively) groups (p = 0.678) and significantly better for the LMWA group than for the TACE group (1-, 3- and 5 year survivals of 84.7 %, 48.8 %, 33.6 %, respectively) (p < 0.001). Weighted multivariate overall survival analysis and competing risk/subgroup analyses confirmed the non-inferiority of LMWA to PRFA and its superiority to TACE. The LMWA- and PRFA-treated patients had a significantly lower risk of HCC-related death (p = 0.004) than the TACE-treated patients (p = 0.001). Conversely, the groups did not differ significantly in terms of non-HCC-related deaths.CONCLUSIONSThe non-inferiority of LMWA to PRFA, its superiority to TACE, and its applicability to a wide range of presentations with few contraindications support its inclusion among radical therapies for treating early-HCC patients.

2

News (Medical) associated with Chlorotrianisene

29 Jan 2024

·www.drugs.com

Addition of Durvalumab, Bevacizumab to TACE Beneficial in Liver Cancer

MONDAY, Jan. 29, 2024 -- For patients with embolization-eligible unresectable hepatocellular carcinoma (uHCC), the addition of durvalumab (D) and bevacizumab (B) to transarterial chemoembolization (TACE) improves progression-free survival (PFS), according to a study presented at the American Society of Clinical Oncology annual Gastrointestinal Cancers Symposium, held from Jan. 18 to 20 in San Francisco. Riccardo Lencioni, M.D., from the University of Pisa School of Medicine in Italy, and colleagues randomly assigned patients with embolization-eligible uHCC to D + B + TACE, D + TACE, or TACE in a 1:1:1 ratio (204, 207, and 205 patients, respectively). The primary end point was PFS for D + B + TACE versus TACE. The researchers found that PFS was significantly improved for D + B + TACE versus TACE (median, 15.0 versus 8.2 months; hazard ratio, 0.77). Across most prespecified subgroups, the results were consistent. The secondary end point of PFS for D + TACE versus TACE did not reach statistical significance. The objective response rate was 43.6, 41.0, and 29.6 percent, respectively, and median time to progression was 22.0, 11.5, and 10.0 months, respectively, for D + B + TACE, D + TACE, and TACE. Maximum grade 3/4 treatment-related adverse events occurred in 32.5, 15.1, and 13.5 percent, respectively; 0, 1.3, and 2.0 percent, respectively, died due to treatment-related adverse events. "These results of the EMERALD-1 trial have the potential to establish a new standard of care for the treatment of unresectable hepatocellular carcinoma," Cathy Eng, M.D., ASCO expert in gastrointestinal cancers, said in a statement. Several authors disclosed ties to pharmaceutical companies, including AstraZeneca, which manufactures durvalumab and funded the study. Press Release More Information Disclaimer: Statistical data in medical articles provide general trends and do not pertain to individuals. Individual factors can vary greatly. Always seek personalized medical advice for individual healthcare decisions. Posted January 2024 More news resources FDA Medwatch Drug Alerts Daily MedNews News for Health Professionals New Drug Approvals New Drug Applications Drug Shortages Clinical Trial Results Generic Drug Approvals Subscribe to our newsletter Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

Clinical ResultASCOClinical Study

19 Jan 2024

·firstwordpharma.com

EMERALD-1 readout dulls Imfinzi's sheen in first-line liver cancer

AstraZeneca's immunotherapy Imfinzi (durvalumab) produced a mixed bag when used as an add-on to transarterial chemoembolisation (TACE) in patients with hepatocellular carcinoma (HCC). According to detailed results from the Phase III EMERALD-1 trial, unveiled Friday at the American Society of Clinical Oncology Gastrointestinal Cancers Symposium (ASCO GI), the combination significantly improved progression-free survival (PFS), but only when Roche's Avastin (bevacizumab) was part of the mix.PFS benefit of nearly 7 monthsThe three-arm study included 616 patients with embolisation-eligible unresectable HCC who were randomised to receive TACE therapy alone, or Imfinzi plus TACE either with or without Avastin. AstraZeneca said the trio combination reduced the risk of disease progression or death by a statistically significant 23%, compared to placebo plus TACE. Median PFS for the two groups was 15 months and 8.2 months, respectively.However, without Avastin, there was no significant PFS difference between those who received Imfinzi plus TACE and the TACE-only groups. Researchers said objective response rate (ORR) and time to progression (TTP) were also superior in the Imfinzi, Avastin and TACE arm. The ORR for these patients was 43.6% and median TTP was 22 months, whereas it was 29.6% and 10 months for TACE-only.Will it be enough?Susan Galbraith, who heads oncology R&D at AstraZeneca, said "we are discussing these positive EMERALD-1 data with global regulatory authorities while awaiting the final overall survival (OS) results from the trial."At the company's earnings call last November, Galbraith said it would be "important for us to show the potential for contribution of components" in the treatment regimen. She also noted that OS data would be key given the EMERALD-1 study's focus is in the locoregional setting, although "it may well be possible to file on PFS, and then wait for OS to be supplemented during the follow-up period and during the review period."Imfinzi is currently approved in combination with Imjudo (tremelimumab) for unresectable HCC in the US, Europe, Japan, China and other countries based on the Phase III TOPAZ-1 and HIMALAYA Phase III trials. The PD-L1 inhibitor is also approved for other indications including non-small-cell lung cancer, extensive-stage small cell lung cancer and advanced biliary tract cancer.

Clinical ResultPhase 3ASCODrug ApprovalImmunotherapy

100 Deals associated with Chlorotrianisene

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D00269	Chlorotrianisene	G03CA06	DB00269

R&D Status

Approved

10 top approved records.

Login

to view more data

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

Developing

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Hepatocellular Carcinoma	Phase 1	CN	Shenzhen SiBiono GeneTech Co. Ltd.	01 Jul 2014

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ESMO_IO2023	Not Applicable	Advanced Hepatocellular Carcinoma	73	Tislelizumab plus TKIs	(hfvodxcian) = tqrafigxki wpukwlolfd (emkeeherfi ) View more	-	07 Dec 2023
				Tislelizumab plus TKIs plus TACE	(dqjetihrit) = rofjmuxfjl douasspprd (cegcxovchs ) View more
113/INT/2021 (ESMO_GI2023)	Not Applicable	Second line	1,381	Lenvatinib	(jryjtbzsub) = mpjjcezpay tthzchjqdm (bgooubnsiq ) View more	Positive	01 Jul 2023
				Atezolizumab plus bevacizumab	(jryjtbzsub) = qmrfnztfkv tthzchjqdm (bgooubnsiq )
ASCO2023	Not Applicable	Unresectable Hepatocellular Carcinoma First line \| Second line	34	Donafenib+TACE+anti-PD1 antibody	(ntktlhazzf) = 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. rrlivrcigk (vgyyorgzvj )	Positive	31 May 2023
ASCO2023	Not Applicable	Advanced Hepatocellular Carcinoma Second line	43	TACE+Regorafenib	smrvffzwmp(pumakmsqqr) = 16.28% anrwsbbfzz (dxzwndrsjz ) View more	Positive	31 May 2023
ASCO 12023 \| ASCO 22023 Manual	Not Applicable	Advanced Hepatocellular Carcinoma Second line	94	Regorafenib	(vhzpfrtrxv) = qvswlfgddq dvpsulwfug (rbrplogsfd, 0.45 - 7.95)	Positive	26 May 2023
				PD-1 inhibitors+TACE+Regorafenib	(vhzpfrtrxv) = qenigatxsg dvpsulwfug (rbrplogsfd, 7.09 - 10.32)
ChiCTR1800018621 (ESMO_ASIA2022) Manual	Phase 4	Hepatocellular Carcinoma	178	apatinib+TACE	(ocoksgwwpd) = diwasukmjd nnyqogpwgc (ukeyzovtjq, 4.53 - 10.15) View more	Positive	03 Dec 2022
				TACE	(ocoksgwwpd) = zyggrmrtda nnyqogpwgc (ukeyzovtjq, 2.83 - 4.90) View more
Pubmed Manual	Not Applicable	Hepatocellular Carcinoma First line \| Neoadjuvant	51	TACE+Lenvatinib+Toripalimab	kyblwvcugb(yifpweemkq) = fqcbcblbey pxyaxslgls (yfbcdxcrzt ) View more	Positive	02 Sep 2022
				TACE+Lenvatinib	kyblwvcugb(yifpweemkq) = mzhurmvrae pxyaxslgls (yfbcdxcrzt ) View more
Pubmed \| Front Oncol Manual	Not Applicable	Unresectable Hepatocellular Carcinoma	110	TACE+PD-1 Inhibitors+Lenvatinib	(ueaquplpfc) = dzmhsuukup xpubfeaogy (rdaeluhmqr ) View more	Positive	21 Apr 2022
				TACE	(ueaquplpfc) = komamdokna xpubfeaogy (rdaeluhmqr ) View more
EASL_LCS2022	Not Applicable	Unresectable Intrahepatic Cholangiocarcinoma hepatitis B/C	32	TACE and lenvatinib	(onovjdicuv) = 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%]) pjsjzjjbcb (iuvbylqxoi )	Positive	03 Feb 2022
				TACE and lenvatinib plus PD-1 inhibitor
CSCO2021	Not Applicable	Liver Cancer	107	TACE+MWA联合治疗组	fwmoktaeti(qpfoynnqmy) = fzytckjjfo caikfffjvh (lcrlkvwvpo ) View more	-	25 Sep 2021
				单纯TACE组	fwmoktaeti(qpfoynnqmy) = eijgawnvse caikfffjvh (lcrlkvwvpo ) View more