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-

Action-

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 (China)

Login to view timeline

Structure/Sequence

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

/ RecruitingNot ApplicableIIT

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

Login to view more data

100 Translational Medicine associated with Gimeracil

Login to view more data

100 Patents (Medical) associated with Gimeracil

Login to view more data

920

Literatures (Medical) associated with Gimeracil

01 Feb 2025·Synthesis

A Portal to Highly Valuable Pyridonyl Vinyl Sulfonyl Fluorides and Aliphatic Sulfonyl Fluorides

Author: Qin, Hua-Li ; Zeng, Shi-Qi ; Fayad, Eman ; Abu Ali, Ola A. ; Sun, Bing

AbstractA novel and efficient method for selective Michael addition of 2-pyridones to ethenesulfonyl fluoride (ESF) and 1-bromoethene-1-sulfonyl fluoride (BESF) has been developed for constructing a class of pyridonyl aliphatic sulfonyl fluorides and pyridonyl vinyl sulfonyl fluorides in good to excellent yields. This practical method features easy operation, wide substrate scope, and mild reaction conditions.

01 Feb 2025·European Archives of Oto-Rhino-Laryngology

Maintenance treatment with oral anticancer agents after first-line chemotherapy in patients with recurrent or metastatic nasopharyngeal carcinoma: a systematic review and meta-analysis

Review

Author: Zhang, Ju ; Hu, Longfei ; Huang, Yuxin

OBJECTIVEMaintenance therapy following first-line chemotherapy is of particular significance in patients diagnosed with recurrent or metastatic nasopharyngeal carcinoma (NPC). We conducted a meta-analysis to investigate the impact of maintenance therapy (MT) on the survival prognosis of individuals with recurrent or metastatic NPC.METHODSThe databases Embase, PubMed, and the Cochrane Library were thoroughly searched in a comprehensive manner. Prospective studies of MT for recurrent or metastatic NPC are required. Study endpoints included progression-free survival (PFS) and overall survival (OS).RESULTSTwo randomized controlled clinical trials, with a total of 294 participants, were analyzed. The maintenance therapy group consisted of 140 participants, while the remaining participants were in the non-maintenance therapy (non-MT) group. The MT group showed a notable enhancement in PFS compared to the non-MT group, with a hazard ratio(HR) of 0.44 and a 95% Confidence interval [CI] of 0.34-0.58 (p < 0.0001). Overall survival was also significantly improved (HR0.42, 95% CI 0.30-0.58; p < 0.0001). The incidence of grade 3 or 4 side effects in the MT group was leukopenia (2.9%), thrombocytopenia (0.7%), and anemia (4.3%), hand-foot syndrome (5.8%), and thrombocytopenia (0.7%). oral mucositis (1.5%), and nausea and vomiting (2.2%).CONCLUSIONSMaintenance therapy with S-1 (tegafur/gimeracil/oltiracetam) or capecitabine following first-line chemotherapy significantly enhanced OS and PFS in patients with recurrent or metastatic nasopharyngeal carcinoma, while exhibiting minimal incidence of grade 3-4 side effects.

01 Jan 2025·Journal of Chromatography B

Quantification of gimeracil, tegafur, and 5-FU in human plasma via LC-MS/MS with a simplified pretreatment using flow-through extraction

Article

Author: Kawahara, Masami ; Maeda, Shoko ; Seike, Riko ; Watanabe, Norio ; Gocho, Saori ; Inagaki, Masami ; Ando, Motozumi

Gimeracil, a component in S-1 (an oral anticancer agent comprising tegafur, a prodrug of 5-fluorouracil (5-FU), potassium oxonate, and gimeracil), inhibits metabolic enzymes, thereby impeding 5-FU degradation. Therefore, the blood level of gimeracil is closely associated with the disposition of 5-FU, and quantification of gimeracil can provide important information if a case shows an inappropriate 5-FU blood concentration. Nevertheless, methods for quantifying gimeracil in human plasma are rarely reported. Herein, we aimed to develop a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for quantifying gimeracil, in addition to tegafur and 5-FU, levels in human plasma using a clinically applicable simplified pretreatment process and faster elution time. Hence, an acetamide-functionalized monolith silica disk-packed spin column was used to extract gimeracil and internal standard (IS; nicotinamide), whereas diatomaceous earth-based solid phase for liquid-liquid extraction was used to extract tegafur, 5-FU, and IS (5-chlorouracil) from plasma. Each extract was analyzed within 4 min of elution via LC-MS/MS using a shared LC column and mobile phase. Accuracy and precision analyses indicated lower limits of quantification of 5, 10, and 2 ng/mL for gimeracil, tegafur, and 5-FU, respectively. The calibration curves showed good linearity between 5 and 500 ng/mL for gimeracil, 10 and 5000 ng/mL for tegafur, and 2 and 1000 ng/mL for 5-FU. We confirmed that the levels of all analytes in the plasma of patients with cancer undergoing S-1-inclusive therapy were within the calibration range for each analyte. Thus, this newly developed quantification method is likely to be useful for optimization of S-1 therapy.

100 Deals associated with Gimeracil

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D01846	-	-	DB09257

R&D Status

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NJLCG0804 (Pubmed) Manual	Phase 2	EGFR-mutated non-small Cell Lung Cancer EGFR Mutation	25	Tegafur+Gimeracil+Oteracil+Irinotecan Hydrochloride	(prvxlksbhp) = bsproqymsf rxqmdeapdc (uifqbcclbg, 63.9 - 95.5) View more	Positive	16 Aug 2022
Pubmed Manual	Not Applicable	Locally Advanced Gastric Carcinoma Neoadjuvant	96	Apatinib+Tegafur+Gimeracil+Oteracil+Oxaliplatin	(wzotxmtjbs) = the incidences of adverse events between the two groups were not different qayjuxtcsq (uyelhfeqvg ) 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	(bjkrpzzosj) = okwbgtxufq ejvjdndxly (vdbyngrqca ) View more	Positive	20 May 2014
JPRN-C000000416 (SELECT BC, ASCO2014)	Phase 3	Metastatic breast cancer First line	-	TS-1	(bjkrpzzosj) = miwctcwhgl ejvjdndxly (vdbyngrqca ) View more	Positive	20 May 2014
ASCO2012	Not Applicable	Locally Advanced Unresectable Gastric Adenocarcinoma	1,372	TS-1 monotherapy	(brmhkljgyg) = aagrqcnraf lepocltbzu (qiqgbyvvlg, 10.6 - 17.9) View more	-	20 May 2012
ASCO2012	Not Applicable	Locally Advanced Unresectable Gastric Adenocarcinoma	1,372	TS-1/cisplatin	(brmhkljgyg) = bxizziwjfb lepocltbzu (qiqgbyvvlg, 14.4 - 17.9) View more	-	20 May 2012
ASCO2011	Phase 2	HER2-negative breast cancer Neoadjuvant	48	Doxorubicin/cyclophosphamide (AC) followed by docetaxel and TS-1 (DS)	(neuydywnrv) = fjjgnzqjif uqivfneetw (wzvhcmdhuy ) View more	-	20 May 2011
ASCO2010	Phase 1/2	Advanced Lung Non-Small Cell Carcinoma	23	TS-1 monotherapy	(ldivsauzuc) = pnvmszchjn hjkvdlhink (rswaiiinvs ) View more	Positive	20 May 2010
ASCO2009	Not Applicable	Breast Cancer	40	TS-1	awzhltcdti(lriawgusya) = 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. cznxuvuunb (dvpnmrbrxy )	Positive	20 May 2009
CJLSG0402 (ASCO2008)	Phase 1/2	Advanced Lung Non-Small Cell Carcinoma	-	TS-1 plus carboplatin	(fwbtzzkbly) = txisptggaj bzqdfteijk (jdkqrzzsmv ) View more	-	20 May 2008
ASCO2007	Phase 2	Non-small cell lung cancer stage III	28	TS-1 plus cisplatin	(wsdqfhdeuo) = qqvdzgukhc scbylcvpwg (kmpqelsleq, 79.1 - 98.7)	-	20 Jun 2007
ASCO2007	Not Applicable	Neoplasms	147	Concurrent radiation therapy combined with UFT	izwxopatmd(nappmgcbkw) = ofmbltqirw dohyedeymw (fofsgzhaxw )	Positive	20 Jun 2007
ASCO2007	Not Applicable	Neoplasms	147	Concurrent radiation therapy combined with TS-1	izwxopatmd(nappmgcbkw) = mrxydfwmtj dohyedeymw (fofsgzhaxw )	Positive	20 Jun 2007