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-

Login to view timeline

Structure/Sequence

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

Login to view more data

100 Translational Medicine associated with Folitixorin Calcium

Login to view more data

100 Patents (Medical) associated with Folitixorin Calcium

Login to view more data

43

Literatures (Medical) associated with Folitixorin Calcium

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: Puthusseri, Bijesh ; Chauhan, Vikas Singh ; 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.

01 Feb 2019·The Journal of Alternative and Complementary MedicineQ4 · MEDICINE

The Bioavailability of Various Oral Forms of Folate Supplementation in Healthy Populations and Animal Models: A Systematic Review

Q4 · MEDICINE

Review

Author: Agrawal, Nitish ; Schloss, Janet ; Bayes, Jessica

BACKGROUND AND AIMSFolate is an essential nutrient required for many different functions in the body. It is particularly important for DNA synthesis, immune functions, and during pregnancy. Folate supplements are commonly prescribed by health professionals for a number of different conditions, however, the absorption of the different derivatives remains unclear. The aim of this review was to assess the bioavailability of various forms of folate supplements in healthy populations and animal models.METHODSA systematic literature review was conducted of original research, which assessed the bioavailability of different oral forms of folate in healthy adults or animal models. The following databases were searched: PubMed (U.S. National Library of Medicine), ProQuest Medical Collection (ProQuest) and ScienceDirect (Elsevier) up to March 30, 2017. The inclusion criteria consisted of both animal and human research, no disease state or condition, and assessed levels after an intervention of a folate derivative.RESULTSA total of 23 studies out of 5226 met the full inclusion criteria. Of these, 4 were animal studies and 19 were human studies. There was variation in supplement forms used with the most commonly tested being folic acid followed by 5-methylenetetrahydrofolate (5-MTHF). Dosages ranged from 25 μg up to 200 mg. Only three studies found a statistically significant difference in folate bioavailability when evaluating different supplement forms. These studies found 5-MTHF to be more effective at increasing folate levels in participants.CONCLUSIONSThis review has found a number of methodological limitations and conflicting results. Only three out of the 23 studies assessed found a statistically significant difference between different supplemental forms of folate. Quality absorption studies assessing the bioavailability of oral folate supplements are crucial if clinicians are to make effective evidence-based recommendations. More research is required for greater clarification regarding the bioavailability of these supplements.

100 Deals associated with Folitixorin Calcium

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D08925	-	-	DB05308

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Colonic Cancer	Phase 3	ME	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	MX	Mast Therapeutics, Inc.	-
Breast Cancer	Phase 3	RU	Mast Therapeutics, Inc.	-
Breast Cancer	Phase 2	PE	Mast Therapeutics, Inc.	-
Colonic Cancer	Discovery	US	Mast Therapeutics, Inc.	01 May 2006

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

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	xjvrviumgh(iymdubbfoy) = 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) qabtglkvgl (owzrsvtgwq ) View more	Positive	01 Jun 2018
ASCO2008	Phase 2	Advanced breast cancer	-	5,10 methylenetetrahydrofolic acid + fluorouracil	(hvumawmhsm) = faitorrzpe iidazimkep (lnwdgxtrei )	-	20 May 2008
ASCO2006	Phase 2	Metastatic Colorectal Carcinoma First line	50	5,10-methylenetetrahydrofolic acid + 5-fluorouracil	(wniohbebbi) = median survival has not been reached mvlkmriejw (zepehtechw )	-	20 Jun 2006
ASCO2005	Phase 2	Gallbladder Carcinoma	13	5-FU (CVI)	(hjwcjitzzx) = bpwslkhhoc rbhtkzvgxf (wckerzizac ) View more	-	01 Jun 2005