Delving into the Latest Updates on Gimeracil with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

5-Chloro-2,4-dihydroxypyridine, 5-Chloro-4-hydroxy-2-pyridone, Gimeracil (JAN/INN)

+ [3]

Target-

Mechanism-

Therapeutic Areas-

Active Indication-

Inactive Indication-

Originator Organization-

Active Organization

Shandong New Time Pharmaceutical Co. Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

RegulationSpecial Review Project (CN)

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Structure

Molecular FormulaC5H4ClNO2

InChIKeyZPLQIPFOCGIIHV-UHFFFAOYSA-N

CAS Registry103766-25-2

A multicenter, randomized, phase III clinical study comparing the combination of radiotherapy with Tegafur, Gimeracil, and Oteracil Potassium (TS-1) and Tislelizumab to the combination of radiotherapy with TS-1 in elderly patients with locally advanced esophageal squamous cell carcinoma. - A multicenter, randomized, phase III clinical study comparing the combination of radiotherapy with Tegafur, Gimeracil, and Oteracil Potassium (TS-1) and Tislelizumab to the combination of radiotherapy with TS-1 in elderly patients with locally advanced esophageal squamous cell carcinoma.

Start Date01 Mar 2024

Sponsor / Collaborator

Henan Cancer Hospital

JPRN-UMIN000043646 / RecruitingIIT

Long term follow-up protocol of Peri-operative chemotherapy with intraperitoneal and intravenous Paclitaxel plus TS-1 for serosa positive gastric cancer patients phase 2 study - Long term follow-up of GAPS study

Start Date01 Sep 2019

Sponsor / Collaborator

Kindai University

JPRN-jRCTs071180083 / CompletedPhase 1IIT

Feasibility study of adjuvant chemotherapy with cisplatin(CDDP) and TS-1 in followed by alternate-day treatment with TS-1 in patients with completely resected pathological II-IIIA non small cell lung cancer - None

Start Date29 Mar 2019

Sponsor / Collaborator-

100 Clinical Results associated with Gimeracil

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100 Translational Medicine associated with Gimeracil

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100 Patents (Medical) associated with Gimeracil

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595

Literatures (Medical) associated with Gimeracil

01 Jul 2024·Gastric Cancer

Adjuvant and post-recurrent treatment patterns in patients with resectable gastric cancer in Japan: a retrospective database cohort study

Article

Author: Hironaka, Shuichi ; Matsuda, Yuko ; Nishiyama, Eiji ; Casaes Teixeira, Bruno ; Kimijima, Yuya ; Tejada, Mariella ; Carroll, Robert ; Yoshikawa, Takaki ; Kikko, Yorifumi ; Makino, Reina

AbstractBackgroundThis study examined temporal shifts in adjuvant therapy patterns in Japanese patients with resectable gastric cancer (GC) and treatment patterns of first-line and subsequent therapy among those with recurrent disease.MethodsThis retrospective analysis of hospital-based administrative claims data (April 1, 2008 to March 31, 2022) included adults (aged ≥ 20 years) with GC who started adjuvant therapy on or after October 1, 2008 (adjuvant cohort) and patients in the adjuvant cohort with disease recurrence (recurrent cohort), further defined by the time to recurrence (≤ 180 or > 180 days after adjuvant therapy).ResultsIn the adjuvant cohort (n = 17,062), the most common regimen during October 2008–May 2016 was tegafur/gimeracil/oteracil potassium (S-1; 95.7%). As new standard adjuvant regimen options were established, adjuvant S-1 use decreased to 65.0% and fluoropyrimidine plus oxaliplatin or docetaxel plus S-1 use increased to 15.0% and 20.0%, respectively, in September 2019–March 2022. In the recurrent cohort with no history of trastuzumab/trastuzumab deruxtecan treatment (n = 1257), the most common first-line regimens were paclitaxel plus ramucirumab (34.0%), capecitabine plus oxaliplatin (CapeOX; 17.0%), and nab-paclitaxel plus ramucirumab (10.1%) in patients with early recurrence, and S-1 plus oxaliplatin (26.3%), S-1 plus cisplatin (15.3%), CapeOX (14.0%), S-1 (13.2%), and paclitaxel plus ramucirumab (10.8%) in those with late recurrence.ConclusionsThis study demonstrated temporal shifts in adjuvant treatment patterns that followed the establishment of novel regimens, and confirmed that post-recurrent treatment patterns were consistent with the Japanese Gastric Cancer Association guideline recommendations.

01 Jul 2024·Breast Cancer Research and Treatment

Treatment patterns and clinical outcomes in patients with metastatic triple-negative breast cancer: a large-scale data analysis using the Japanese claims database

Article

Author: Ntalla, Ioanna ; Saji, Shigehira ; Piao, Yi ; Takami, Tomoko ; Kimura, Takayuki

AbstractPurposeThis study evaluated treatment patterns and clinical outcomes among patients with metastatic triple-negative breast cancer (mTNBC) in real-world clinical settings in Japan.MethodsThe treatment patterns, time to next treatment or death (TTNTD), time to treatment discontinuation, adverse events of interest, and medical costs of treating patients with mTNBC in first-, second-, and third-line settings were investigated using data of patients meeting the inclusion criteria between January 2017 and March 2022 in a Japanese medical claims database. The treatment regimens for mTNBC were defined according to the Japanese Breast Cancer Society Clinical Practice Guidelines.ResultsIn this study, 2236 patients with mTNBC (median age 66.0 years; 99.8% female) were included in the first-line cohort. Of these, 46.6% and 20.8% were included in the second- and third-line cohorts, respectively. The two most frequently used treatments were capecitabine (19.1%) and S-1 (tegafur–gimeracil–oteracil) (14.5%) in the first-line cohort, eribulin (18.3%) and bevacizumab/paclitaxel (14.4%) in the second-line cohort, and eribulin (19.4%) and bevacizumab/paclitaxel (17.5%) in the third-line cohort. The TTNTD shortened as the line of therapy progressed (median 8.0, 6.5, and 5.2 months for the first-, second-, and third-line treatments, respectively). Nausea/vomiting and neutropenia/leukopenia occurred in 62.8% and 18.3% of all patients, respectively. The medical total costs per day were 6.7, 10.2, and 12.9 thousand yen during the first-/second-/third-line treatments, respectively.ConclusionThis study provides insight into current treatment patterns for mTNBC in Japan. The cost–benefit balance worsens with later-line treatment and a high unmet need for mTNBC drug treatment remains.

01 Jul 2024·Gastric Cancer

Molecular features and prognostic factors of locally advanced microsatellite instability-high gastric cancer

Article

Author: Terashima, Masanori ; Bando, Etsuro ; Koseki, Yusuke ; Urakami, Kenichi ; Tanizawa, Yutaka ; Furukawa, Kenichiro ; Hatakeyama, Keiichi ; Yamaguchi, Ken ; Fujiya, Keiichi

BACKGROUNDMicrosatellite instability-high (MSI-H) tumors are distinct molecular subtypes in gastric cancer. However, a few studies have comprehensively reported the molecular features of MSI-H tumors and their prognostic factors in locally advanced gastric cancer. This study aimed to clarify the molecular features and prognostic factors of locally advanced MSI-H gastric cancer.METHODSThis study included 499 patients with locally advanced gastric cancer who underwent radical gastrectomy. We evaluated the MSI status and compared with previously published whole-exome sequencing, panel sequencing, and gene expression profiling data. Clinicopathological characteristics and molecular profiles were compared between patients with MSI-H and microsatellite stable (MSS) gastric cancer. A subgroup analysis of survival was performed in patients with MSI-H gastric cancer.RESULTSMSI-H tumors were detected in 79 of 499 patients (15.8%). MSI-H tumors were associated with an increased tumor mutational burden, MLH1 downregulation, CD274 (PD-L1) upregulation, and enrichment of cell cycle pathways. Among patients with MSI-H gastric cancer, the disease-specific survival (DSS) tended to be better in the surgery plus tegafur, gimeracil, and oteracil potassium (S-1) adjuvant chemotherapy group than in the surgery alone group, especially for stage III patients. Furthermore, DSS was better in the T cell-inflamed gene expression signature-high group, and it tended to be worse in the non-solid type poorly differentiated adenocarcinoma group.CONCLUSIONSThe molecular features and prognostic factors of locally advanced MSI-H gastric cancer were clarified. S-1 adjuvant chemotherapy appears to be beneficial, and the T cell-inflamed gene expression signature and histopathological type are prognostic factors in MSI-H tumors.

100 Deals associated with Gimeracil

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External Link

KEGG	Wiki	ATC	Drug Bank
D01846	-	-	DB09257

R&D Status

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


Pubmed Manual	Not Applicable	Locally Advanced Gastric Carcinoma Neoadjuvant	96	Apatinib+Tegafur+Gimeracil+Oteracil+Oxaliplatin	(bwdipnqscz) = the incidences of adverse events between the two groups were not different lcqchptkgq (acaemxnouq ) View more	Positive	11 Jul 2022
Pubmed Manual	Not Applicable	Locally Advanced Gastric Carcinoma Neoadjuvant	96	Oxaliplatin+Capecitabine		Positive	11 Jul 2022
JPRN-C000000416 (SELECT BC, ASCO2014)	Phase 3	Metastatic breast cancer First line	-	Taxane	(pobjvyuthh) = dzbsriwvzk zxzzcrhsoh (ezlqbmtfbw ) View more	Positive	20 May 2014
JPRN-C000000416 (SELECT BC, ASCO2014)	Phase 3	Metastatic breast cancer First line	-	TS-1	(pobjvyuthh) = iglrxjopgh zxzzcrhsoh (ezlqbmtfbw ) View more	Positive	20 May 2014
ASCO2012	Not Applicable	Locally Advanced Unresectable Gastric Adenocarcinoma	1,372	TS-1 monotherapy	(hneruvdmfy) = jlakxnswum syanzmpdrr (xhlyxdbywe, 10.6 - 17.9) View more	-	20 May 2012
ASCO2012	Not Applicable	Locally Advanced Unresectable Gastric Adenocarcinoma	1,372	TS-1/cisplatin	(hneruvdmfy) = dvgvbzwhed syanzmpdrr (xhlyxdbywe, 14.4 - 17.9) View more	-	20 May 2012
ASCO2011	Phase 2	HER2-negative breast cancer Neoadjuvant	48	Doxorubicin/cyclophosphamide (AC) followed by docetaxelDoxorubicin/cyclophosphamide (AC) followed by docetaxelDoxorubicin/cyclophosphamide (AC) followed by docetaxel and TS-1 (DS)	(bvgybfcvnk) = mauhpwhqvr bkajxgwlzl (vehqasusiq ) View more	-	20 May 2011
ASCO2010	Phase 1/2	Advanced Lung Non-Small Cell Carcinoma	23	TS-1 monotherapy	(uffexuwbur) = mwjwszwulr vclgtwxpep (bwjozrvnod ) View more	Positive	20 May 2010
ASCO2009	Not Applicable	Breast Cancer	40	TS-1	dhfkshkfjo(dzncvzpcda) = 6 of the 40 patients (15.0%) who received TS-1 did hand-foot syndrome (HFS), although 20 of the 40 patients (50.0%) who had received capecitabine, developed HFS. rpihyqigdu (llxwowimcv )	Positive	20 May 2009
CJLSG0402 (ASCO2008)	Phase 1/2	Advanced Lung Non-Small Cell Carcinoma	-	TS-1 plus carboplatinTS-1 plus carboplatin	(kxjzohnoiu) = fwkooouryf ckuxcprmtp (ltledxvqel ) View more	-	20 May 2008
ASCO2007	Phase 2	Non-small cell lung cancer stage III	28	TS-1 plus cisplatin	(kathslkjid) = iijisnnjhn jqekdejlcm (olybnudrmq, 79.1 - 98.7)	-	20 Jun 2007
ASCO2007	Not Applicable	Neoplasms	147	Concurrent radiation therapy combined with UFT	cojcscfcnk(mdscfqmbdq) = gcahpmtupz xinscjbezv (puoxjbcwbf )	Positive	20 Jun 2007
ASCO2007	Not Applicable	Neoplasms	147	Concurrent radiation therapy combined with TS-1	cojcscfcnk(mdscfqmbdq) = glhuvhmvzf xinscjbezv (puoxjbcwbf )	Positive	20 Jun 2007