Delving into the Latest Updates on Folitixorin Calcium with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

5-10 Methylenetetrahydrofolate, 5-FU biomodulator, CoFactor

+ [3]

Target

TYMS

Mechanism

TYMS inhibitors(Thymidylate synthase inhibitors)

Therapeutic Areas

NeoplasmsDigestive System DisordersSkin and Musculoskeletal Diseases+ [1]

Active Indication-

Inactive Indication

Breast CancerColonic CancerMetastatic Colorectal Carcinoma+ [2]

Originator Organization

Mast Therapeutics, Inc.

Active Organization-

Inactive Organization

Mast Therapeutics, Inc.

Drug Highest PhaseDiscontinuedPhase 3

First Approval Date-

Regulation-

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Structure

Molecular FormulaC20H23N7O6

InChIKeyQYNUQALWYRSVHF-ABLWVSNPSA-N

CAS Registry3432-99-3

View All Structures (2)

This double-blind, randomized, placebo-controlled, investigator-initiated, multi-centre trial aims to establish metabolic improvements in AD and PD subjects by dietary supplementation with cofactors N-acetylcysteine, L-carnitine tartrate, nicotinamide riboside and serine. Concomitant use of pivotal metabolic cofactors via simultaneous dietary supplementation will stimulate to enhance hepatic β-oxidation and this study's hypothesis is that this will result in increased mitochondrial activity in human brain cell-types.

Start Date02 Dec 2019

Sponsor / Collaborator

Istanbul Medipol University

[+2]

ChiCTR-IPR-14005485 / RecruitingPhase 4IIT

Post-marketing Clinical Research on compound Kushen Injection in Treatment of Malignant Neoplasm

Start Date25 Oct 2014

Sponsor / Collaborator

Anhui Provincial Hospital

EUCTR2009-009999-12-SE / Not yet recruitingNot Applicable

An Extended Feasibility Phase I/II Study of Methylenetetrahydrofolate and Pemetrexed Single Agent, givenas Neoadjuvant Treatment in Patients with Resectable Rectal Cancer

Start Date17 May 2010

Sponsor / Collaborator

Isofol Medical AB

100 Clinical Results associated with Folitixorin Calcium

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100 Translational Medicine associated with Folitixorin Calcium

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100 Patents (Medical) associated with Folitixorin Calcium

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41

Literatures (Medical) associated with Folitixorin Calcium

05 May 2023·Frontiers in bioscience (Elite edition)

Determination of Vitamin B₁₂ and Folate Compounds in Commercially Available Edible Seaweed Products.

Article

Author: Katsuura, Kiho ; Bito, Tomohiro ; Koseki, Kyohei ; Yoshimura, Ryusei ; Ido, Koki ; Watanabe, Fumio

BACKGROUNDInformation on the contents of both vitamin B12 and folate in edible seaweeds is limited, of which deficiencies disrupt methionine biosynthesis to accumulate homocysteine as a risk factor of cardiovascular diseases.METHODSBoth vitamins were determined in commercially available edible seaweed products using high-performance liquid chromatography.RESULTSDried purple laver (Neopyropia yezoensis) products contain higher levels of vitamin B12 (approximately 30-60 μg/100 g dry weight) and folate compounds (approximately 880-1300 μg/100 g dry weight) than other seaweed products, such as kombu (Saccharina japonica), hijiki (Sargassum fusiformis), and wakame (Undaria pinnatifida). 5-methyltetrahydrofolate was the major folate compound in purple laver products. 5-formyltetrahydrofolate was found at a moderate level, whereas tetrahydrofolate, 5,10-metenyltetrahydrofolate, 10-formyltetrahydrofolate, and folic acid were found to be minor folate compounds.CONCLUSIONSThese findings suggest that dried purple laver (nori) products are suitable sources of vitamin B12 and folate compounds for humans, especially vegetarians.

31 Aug 2022·BioScience Trends

Association of MTHFR 677C>T polymorphism with pregnancy outcomes in IVF/ICSI-ET recipients with adequate synthetic folic acid supplementation

Article

Author: Qi, Qing ; Du, Yan ; Ye, Feijun ; Zhou, Jing ; Zhang, Siwei ; Wang, Ling

Methylenetetrahydrofolate reductase (MTHFR) genetic polymorphism rs1801133 (677C>T) will decrease the utilization of folate. Folate deficiency and its resulting homocysteine (HCY) accumulation can impair female fertility. Folic acid (FA) supplementation is necessary in pregnant women who are undergoing in-vitro fertilization (IVF)/intracytoplasmic sperm injection (ICSI) - embryo transfer (ET), and especially in women with MTHFR rs1801133 C-to-T mutations. At present, affordable and accessible synthetic FA is mainly used. However, some studies have suggested that 5-methylenetetrahydrofolate (5-MTHF), a type of active FA, may be more suitable for women with the MTHFR 677C>T polymorphism, since it is safer and more effective. This retrospective study aimed to evaluate whether the MTHFR rs1801133 gene polymorphism is related to the pregnancy outcomes of IVF/ICSI-ET recipients after sufficient supplementation with FA instead of 5-MTHF. Data on 692 women undergoing IVF/ICSI-ET and taking adequate FA were collected. Participant characteristics were compared using the Kruskal-Wallis test and Pearson chi-square test. Logistic regressions were used to calculate the odds ratio (OR) and 95% confidence interval (95% CI), after adjusting for age, BMI, method of fertilization, method of embryo transfer and number of embryos transferred. An additive model (T/T vs. C/C), dominant model (C/T + T/T vs. C/C), and recessive model (T/T vs. C/T + C/C) were evaluated. Analysis revealed that MTHFR rs1801133 in IVF/ICSI-ET women with adequate FA supplementation was not associated with the pregnancy rate but with age (OR = 0.91, 95% CI = 0.88, 0.94, P < 0.001) and BMI (OR = 0.95, 95% CI = 0.90, 0.997, P = 0.037). In 349 clinically pregnant women, no association of the MTHFR 677C>T with pregnancy outcomes was found in the additive model, dominant model, or recessive model. Of the 273 women with positive pregnancy outcomes, 34 had a preterm delivery. MTHFR 677C>T was not associated with a preterm delivery after adjusting for age and BMI. The current results indicated that MTHFR polymorphism rs1801133 was not related to the pregnancy rate or pregnancy outcomes of women undergoing IVF/ICSI-ET with adequate synthetic FA supplementation, suggesting that simple supplementation with less expensive and readily available FA, rather than expensive 5-MTHF, appeared to be appropriate.

01 May 2022·In Vitro Cellular & Developmental Biology - Animal

Folate derivatives, 5-methyltetrahydrofolate and 10-formyltetrahydrofolate, protect BEAS-2B cells from high glucose–induced oxidative stress and inflammation

Article

Author: Chauhan, Vikas Singh ; Puthusseri, Bijesh ; Pathikkal, Ajana ; Rudrappa, Sudha ; Divya, Peethambaran

Folate (vitamin B₉) and its biologically active derivatives are well-known antioxidant molecules protecting cells from oxidative degradation. The presence of high glucose, often found in diabetic patients, causes oxidative stress resulting in cellular stress and inflammatory injury. Cells in organs such as the lung are highly prone to inflammation, and various protective mechanisms exist to prevent the progressive disorders arising from inflammation. In the present study, the synthetic form of folate, i.e. folic acid, and active forms of folate, i.e. 5-methyltetrahydrofolate and 10-formyltetrahydrofolate, were evaluated for their antioxidant and antiinflammatory potential against high glucose (50 mM)-mediated oxidative stress and inflammation in BEAS-2B cells, an immortalised bronchial epithelial cell line. High glucose treatment showed a 67% reduction in the viability of BEAS-2B cells, which was restored to the viability levels seen in control cultures by the addition of active folate derivatives to the culture media. The DCFH-DA fluorometric assay was performed for oxidative stress detection. The high glucose-treated cells showed a significantly higher fluorescence intensity (1.81- and 3.8-fold for microplate assay and microscopic observation, respectively), which was normalised to control levels on supplementation with active folate derivatives. The proinflammatory NF-κB p50 protein expression in the active folate derivative-supplemented high glucose-treated cells was significantly lower compared to the folic acid treatment. In support of these findings, in silico microarray GENVESTIGATOR database analysis showed that in bronchiolar small airway epithelial cells exposed to inflammatory condition, folate utilization pathway genes are largely downregulated. However, the folate-binding protein gene, which encodes to the folate receptor 1 (FOLR1), is significantly upregulated, suggesting a high demand for folate by these cells in inflammatory situations. Supplementation of the active folate derivatives 5-methyltetrahydrofolate and 10-formyltetrahydrofolate resulted in significantly higher protection over the folic acid from high glucose-induced oxidative stress and inflammation. Therefore, the biologically active folate derivatives could be a suitable alternative over the folic acid for alleviating inflammatory injury-causing oxidative stress.

100 Deals associated with Folitixorin Calcium

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External Link

KEGG	Wiki	ATC	Drug Bank
D08925	-	-	DB05308

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Colonic Cancer	Phase 3	ME	Mast Therapeutics, Inc.	01 May 2006
Colonic Cancer	Phase 3	US	Mast Therapeutics, Inc.	01 May 2006
Metastatic Colorectal Carcinoma	Phase 3	US	Mast Therapeutics, Inc.	01 May 2006
Metastatic Colorectal Carcinoma	Phase 3	ME	Mast Therapeutics, Inc.	01 May 2006
Rectal Cancer	Phase 3	ME	Mast Therapeutics, Inc.	01 May 2006
Rectal Cancer	Phase 3	US	Mast Therapeutics, Inc.	01 May 2006
Breast Cancer	Phase 3	AR	Mast Therapeutics, Inc.	-
Breast Cancer	Phase 3	ES	Mast Therapeutics, Inc.	-
Breast Cancer	Phase 3	RU	Mast Therapeutics, Inc.	-
Breast Cancer	Phase 1	MX	Mast Therapeutics, Inc.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASCO2018	Not Applicable	Advanced Nasopharyngeal Carcinoma	244	Docetaxel, cisplatin and 5-FU (TPF) followed by concurrent chemoradiotherapy	wmzmyrgxao(uhzttjtfjf) = hearing impairment, chronic infection, ear drum perforation were shown in 27 patients (26.7%) and these were significantly higher in elderly ( > 65 years, p = 0.004), advanced T stage (p = 0.022) fcvuzdirsd (pemwilnras ) View more	Positive	01 Jun 2018
KEYNOTE-048 (ASCO2018)	Not Applicable	Recurrent Squamous Cell Carcinoma of the Head and Neck	39	Pembrolizumab	(basajmvydo) = yqzgsclmse xhnyajighm (gnnatkyjwe ) View more	Positive	01 Jun 2018
KEYNOTE-048 (ASCO2018)	Not Applicable	Recurrent Squamous Cell Carcinoma of the Head and Neck	39	Cetuximab+Pt+5-FU (EXTREME)	(basajmvydo) = hotocriwxh xhnyajighm (gnnatkyjwe ) View more	Positive	01 Jun 2018
ASCO2008	Phase 2	Advanced breast cancer	-	5,10 methylenetetrahydrofolic acid + fluorouracil	(zbpsdottxm) = gksvginefn qlsmzjvzjg (bueawujiwy )	-	20 May 2008
ASCO2006	Phase 2	Metastatic Colorectal Carcinoma First line	50	5,10-methylenetetrahydrofolic acid + 5-fluorouracil	(koyvymomlm) = median survival has not been reached jauwajtpko (flajdvizpv )	-	20 Jun 2006
ASCO2005	Phase 2	Gallbladder Carcinoma	13	5-FU (CVI)	(eouikotlgd) = dfhmfqntqf zcgjelfvvp (xmvykybbdl ) View more	-	01 Jun 2005