Delving into the Latest Updates on Carboxyamidotriazole with Synapse

To compare the efficacy and safety of 100 mg CAI capsules in combination with vinorelbine + cisplatin and placebo in combination with vinorelbine + cisplatin as first-line treatment in patients with stage IV non-small cell lung cancer (NSCLC). Primary efficacy indicator: progression-free survival (PFS). Secondary efficacy indicators: objective response rate (CR+PR), disease control rate (CR+PR+SD), overall survival (OS), and quality of life.

Start Date11 Sep 2011

Sponsor / Collaborator

Guangdong Yinzhu Group Co., Ltd.

[+1]

NCT00006486 / CompletedPhase 2IIT

A Phase II Randomized Discontinuation Trial Of Carboxyaminoimidazole (CAI, NSC 609974) In Metastatic Renal Carcinoma

Randomized phase II trial to study the effectiveness of carboxyamidotriazole in treating patients who have metastatic kidney cancer. Carboxyamidotriazole may stop the growth of kidney cancer by stopping blood flow to the tumor

Start Date01 Oct 2000

Sponsor / Collaborator

National Cancer Institute

NCT00004146 / CompletedPhase 2IIT

Phase II Clinical and Pharmacologic Study of Radiation Therapy and CAI (Carboxy-Amido Triazole) in Adults With Newly Diagnosed Glioblastoma Multiforme

Drugs used in chemotherapy use different ways to stop tumor cells from dividing so they stop growing or die. Radiation therapy uses high-energy x-rays to damage tumor cells. Combining radiation therapy with chemotherapy may kill more tumor cells. Phase II trial to study the effectiveness of carboxyamidotriazole plus radiation therapy in treating patients who have newly diagnosed supratentorial glioblastoma multiforme.

Start Date01 Mar 2000

Sponsor / Collaborator

National Cancer Institute

100 Clinical Results associated with Carboxyamidotriazole

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100 Translational Medicine associated with Carboxyamidotriazole

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100 Patents (Medical) associated with Carboxyamidotriazole

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282

Literatures (Medical) associated with Carboxyamidotriazole

01 Oct 2024·Toxicology and Applied Pharmacology

Identification of autophagy-related signatures in doxorubicin-induced cardiotoxicity

Article

Author: Chen, Haoqiang ; Wang, Qian ; Wu, Haiyan ; Ding, Xiaoxue ; Liu, Suijuan ; Kuang, Xiaohui ; Zhang, Hong ; Pang, Mingjie ; Zhang, Yan ; Li, Kunzhi

PURPOSEDoxorubicin is an antibiotic drug used clinically to treat infectious diseases and tumors. Unfortunately, it is cardiotoxic. Autophagy is a cellular self-decomposition process that is essential for maintaining homeostasis in the internal environment. Accordingly, the present study was proposed to characterize the autophagy-related signatures of doxorubicin-induced cardiotoxicity.METHODSDatasets related to doxorubicin-induced cardiotoxicity were retrieved by searching the GEO database and differentially expressed genes (DEGs) were identified. DEGs were taken to intersect with autophagy-related genes to obtain autophagy-related signatures, and Gene Ontology (GO)/Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analysis and protein-protein interaction (PPI) network were performed on them. Further, construction of miRNA-hub gene networks and identification of target drugs to reveal potential molecular mechanisms and therapeutic strategies. Animal models of doxorubicin-induced cardiotoxicity were constructed to validate differences in gene expression for autophagy-related signatures.RESULTSPBMC and heart samples from the GSE37260 dataset were selected for analysis. There were 995 and 2357 DEGs in PBMC and heart samples, respectively, and they had 23 intersecting genes with autophagy-related genes. RT-qPCR confirmed the differential expression of 23 intersecting genes in doxorubicin-induced cardiotoxicity animal models in general agreement with the bioinformatics results. An autophagy-related signatures consisting of 23 intersecting genes is involved in mediating processes and pathways such as autophagy, oxidative stress, apoptosis, protein ubiquitination and phosphorylation. Moreover, Akt1, Hif1a and Mapk3 are hub genes in autophagy-associated signatures and their upstream miRNAs are mainly rno-miR-1188-5p, rno-miR-150-3p and rno-miR-326-3p, and their drugs are mainly CHEMBL55802, Carboxyamidotriazole and 3-methyladenine.CONCLUSIONThis study identifies for the first-time autophagy-related signatures in doxorubicin's cardiotoxicity, which could provide potential molecular mechanisms and therapeutic strategies for doxorubicin-induced cardiotoxicity.

01 Aug 2024·Biomedical Chromatography

An effective LC–MS method for the simultaneous determination of a potential anti‐rheumatoid arthritis drug, carboxyamidotriazole, and its major metabolite in rat plasma

Article

Author: Lang, Xuli ; Xing, Chengfeng ; Tang, Jia ; Wang, Baolian ; Kou, Yuhui ; Mu, Hongfei ; Wang, Yanan

AbstractCarboxyamidotriazole (CAI) was previously recognized as a well‐tolerated anticancer drug. It has also demonstrated significant anti‐inflammatory effects in various cell and animal model experiments, prompting its investigation as a potential treatment for rheumatoid arthritis. In this study, the potential biotransformation metabolites of CAI were identified both in vitro and in vivo. A sensitive, specific, and accurate LC–MS method was developed for the quantitative analysis of CAI and its major metabolite, CAI‐OH, in rat plasma. CAI, CAI‐OH, and telmisartan (used as an internal standard) were separated using a Zorbax SB C18 column. The mobile phase consisted of water (phase A, containing 0.1% formic acid) and acetonitrile (phase B, containing 0.1% formic acid) at a flow rate of 0.2 mL/min. The analytes were examined using a high‐resolution mass spectrometer, with detected mass‐to‐charge ratios of m/z 424.01293 for CAI, m/z 440.00785 for CAI‐OH, and m/z 515.24415 for telmisartan. Good linearity was observed within the range of 10–5000 ng/mL. Both inter‐ and intra‐batch precision (relative standard deviation, %) were below 6%, and the accuracy ranged from 94.9% to 106.1%. The analytes remained stable throughout the entire experimental period. This method was successfully applied in a pharmacokinetic study of CAI following oral administration in rats.

01 Jun 2024·Ophthalmology Retina

Efficacy of Carbonic Anhydrase Inhibitors on Cystoid Fluid Collections and Visual Acuity in Patients with X-Linked Retinoschisis

Article

Author: Florijn, Ralph J ; Boon, Camiel J F ; Hahn, Leo C ; Hensman, Jonathan ; Bergen, Arthur A ; Heutinck, Pam ; de Zaeytijd, Julie ; van Schooneveld, Mary J ; Diederen, Roselie M H ; Leroy, Bart P ; Thiadens, Alberta A ; van Genderen, Maria M ; Hoyng, Carel B ; van den Born, L Ingeborgh ; Strubbe, Ine ; Ten Brink, Jacoline B

PURPOSETo date, there is no standard treatment regimen for carbonic anhydrase inhibitors (CAIs) in X-linked retinoschisis (XLRS) patients. This retrospective study aims to evaluate the efficacy of CAIs on visual acuity and cystoid fluid collections (CFC) in XRLS patients in Dutch and Belgian tertiary referral centers.DESIGNRetrospective cohort study.PARTICIPANTSForty-two patients with XLRS.METHODSIn total, 42 patients were enrolled. To be included, patients had to have previous treatment with an oral CAI (acetazolamide), a topical CAI (brinzolamide/dorzolamide), or a combination of an oral and a topical CAI for at least 4 consecutive weeks. We evaluated the effect of the CAI on best-corrected visual acuity (BCVA) and central foveal thickness (CFT) on OCT.MAIN OUTCOME MEASURESCentral foveal thickness and BCVA.RESULTSThe median age at the baseline visit of the patients in this cohort study was 14.7 (range, 43.6) years, with a median (interquartile range [IQR]) follow-up period of 4.0 (2.2-5.2) years. During the follow-up period, 25 patients were treated once with an oral CAI (60%), 24 patients were treated once with a topical CAI (57%), and 11 patients were treated once with a combination of both topical and oral CAI (26%). We observed a significant reduction of CFT for oral CAI by 14.37 μm per 100 mg per day (P < 0.001; 95% confidence interval [CI], -19.62 to -9.10 μm) and for topical CAI by 7.52 μm per drop per day (P = 0.017; 95% CI, -13.67 to -1.32 μm). The visual acuity changed significantly while on treatment with oral CAI by -0.0059 logMAR per 100 mg (P = 0.008; 95% CI, -0.010 to -0.0013 logMAR). Seven patients (17%) had side effects leading to treatment discontinuation.CONCLUSIONSOur data indicate that treatment with (oral) CAI may be beneficial for short-term management of CFC in patients with XLRS. Despite a significant reduction in CFT, the change in visual acuity was modest and not of clinical significance. Nonetheless, the anatomic improvement of the central retina in these patients may be of value to create an optimal retinal condition for future potential treatment options such as gene therapy.FINANCIAL DISCLOSURE(S)The authors have no proprietary or commercial interest in any materials discussed in this article.

100 Deals associated with Carboxyamidotriazole

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External Link

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-	Carboxyamidotriazole	-	DB11960

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Non-Small Cell Lung Cancer	Discovery	CN	Guangdong Yinzhu Pharmaceutical Technology Co., Ltd.	08 Jul 2021
Glioblastoma Multiforme	Discovery	US	National Cancer Institute	01 Mar 2000
Gliosarcoma	Discovery	US	National Cancer Institute	01 Mar 2000
metastatic non-small cell lung cancer	Discovery	US	National Cancer Institute	01 Apr 1999
Non-small cell lung cancer stage IIIA	Discovery	US	National Cancer Institute	01 Apr 1999
Non-small cell lung cancer stage IIIB	Discovery	US	National Cancer Institute	01 Apr 1999
Fallopian Tube Carcinoma	Discovery	US	National Cancer Institute	01 Apr 1998
Ovarian Epithelial Carcinoma	Discovery	US	National Cancer Institute	01 Apr 1998
Platinum-Resistant Primary Peritoneal Carcinoma	Discovery	US	National Cancer Institute	01 Apr 1998
Refractory Primary Peritoneal Serous Adenocarcinoma	Discovery	US	National Cancer Institute	01 Apr 1998

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Clinical Result

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


EHA2017	Phase 2	Acute Myeloid Leukemia	20	CAI	wmntlzodpi(aubbntupxx) = saovawfgrj knwhkwfkde (dtabnqasik ) View more	Positive	18 May 2017
NCT00004146 (CTgov)	Phase 2	Glioblastoma Multiforme \| Gliosarcoma	55	CAI (CAI With RT - Arm 1)	(jkmubtlbet) = uweumpevzf vsiebdtbph (rvidsgtmid, nnnnqgctyd - kdmxxynung) View more	-	08 May 2015
				CAI (CAI With RT + Enzyme Inducing Anticonvulsants)	eezxkjdwzn(vngnexbbky) = pdxqikzifh qytukduvwg (jgcbazoihz, rjenkuxmtd - ientueesmr)
NCT00003869 (CTgov)	Phase 3	Non-small cell lung cancer stage IIIA \| Non-small cell lung cancer stage IIIB \| metastatic non-small cell lung cancer	186	Carboxyamidotriazole (Carboxyamidotriazole)	(guogxvgrma) = uaivmmzvqv xozgrxrxja (eracrvntct, ncewmkppjl - jsucidmlsk) View more	-	22 Dec 2010
				placebo (Placebo)	(guogxvgrma) = kugjvycopi xozgrxrxja (eracrvntct, yquonjzdaj - xgknuholfz) View more
NCT00005045 (E4896, Pubmed \| Cancer)	Phase 2	Advanced Renal Cell Carcinoma	-	Carboxyamidotriazole	(rheqeclytl) = lewwkrypmk acseghfltg (uemgpdpaez ) View more	-	01 Dec 2005
NCCTG (ASCO2005)	Phase 3	Non-Small Cell Lung Cancer Maintenance	186	Carboxyaminoimidazole (CAI)	(sojqebfeqf) = niivfhdqbz pulessbmgi (ibwuhhxzoh ) View more	Negative	01 Jun 2005
				Placebo	(sojqebfeqf) = sswsazqovp pulessbmgi (ibwuhhxzoh ) View more