A Randomized, Controlled, Double-Blind Clinical Trial on the Efficacy and Safety of Amlodipine Folic Acid Tablets Combined with 5-Methyltetrahydrofolate Tablets in Lowering Homocysteine in Hypertensive Patients with MTHFR 677 TT Genotype

开始日期2025-02-19

申办/合作机构

北京大学第一医院

100 项与左甲柳叶酸钙相关的临床结果

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100 项与左甲柳叶酸钙相关的转化医学

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100 项与左甲柳叶酸钙相关的专利（医药）

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545

项与左甲柳叶酸钙相关的文献（医药）

2026-04-01·MATURITAS

Dietary intake of live microbes is inversely associated with fatigue and modified by serum folate among adults aged 40 years or more

Article

作者: Dennis, Elizabeth A ; Li, Yuanyuan ; Kleckner, Amber S ; Sorkin, John D ; Bigman, Galya ; Ryan, Alice S

OBJECTIVES:

To investigate the independent associations between dietary live-microbe intake, as well as circulating levels of folate metabolites, and fatigue, and to examine their interaction as a potential biological pathway underlying fatigue in aging adults.

STUDY DESIGN:

Cross-sectional analysis of adults aged ≥40 years participating in the National Health and Nutrition Examination Survey 2011-2023.

MAIN OUTCOME MEASURES:

Fatigue was assessed using the Patient Health Questionnaire fatigue item and categorized as none/low versus moderate/severe. Dietary intake of live-microbe foods was derived from two 24-h recalls and classified as low, medium, or high. Total serum concentrations folate and its metabolites, including 5-methyltetrahydrofolate, were quantified. Survey-weighted logistic regression, adjusted for sociodemographic, dietary, and clinical covariates, estimated main effects and interactions between the effects of 5-methyltetrahydrofolate and of live-microbe intake; sensitivity analyses additionally adjusted for depressive symptoms and sleep disturbance.

RESULTS:

Moderate/severe fatigue was reported by 16.3% of 14,376 participants and 15.0% reported no intake of live-microbe foods. High versus low live-microbe intake was associated with lower odds of moderate/severe fatigue (odds ratio [OR] 0.60; 95% confidence interval [CI] 0.46-0.79). Higher serum 5-methyltetrahydrofolate levels were also associated with lower odds of moderate/severe fatigue (OR 0.85; 95% CI 0.73-0.98). In stratified analyses, high live-microbe intake corresponded to 38-65% lower odds of moderate/severe fatigue only among adults with higher levels of 5-methyltetrahydrofolate, with no significant associations among those with lower levels.

CONCLUSIONS:

Intake of microbe-rich foods and higher levels of circulating 5-methyltetrahydrofolate are both associated with lower levels of fatigue in midlife and older adults, and folate sufficiency appears to potentiate the fatigue-reducing benefits of live-microbe foods, supporting a nutrient-microbe pathway relevant to healthy aging.

2026-03-01·JOURNAL OF AOAC INTERNATIONAL

An HPLC-MS-Based Method for Determination of the D- and L- 5-Methyltetrahydrofolate Isomer Ratio in Dietary Supplements

Article

作者: Andrews, Karen W ; Wang, Xiaojuan ; Oh, Laura ; Sun, Jianghao ; Harnly, James M ; Gusev, Pavel ; Vavilala, Suma ; Pandey, Deepesh ; Pehrsson, Pamela

Abstract:

Background:

5-Methyltetrahydrofolate (5-MTHF), a reduced form of folate (vitamin B9) marketed as a potentially more bioavailable alternative to folic acid, is a key ingredient in dietary supplement (DS), particularly prenatal multivitamin/minerals. Its synthesis may produce racemic mixtures of bioactive L-5-MTHF and inactive D-5-MTHF, raising concerns about labeling accuracy, integrity, and health impacts. DS manufacturers consider D-5-MTHF an impurity and do not use racemic mixtures of 5-MTHF in their products.

Objective:

This study aimed to develop and validate an HPLC-MS-based method to separate and quantify the D and L-5-MTHF diastereomers in various DS matrixes and dosage forms.

Methods:

A single-laboratory validated method was developed for determination of 5-MTHF isomers in different dosage forms of DS using targeted selected ion monitoring (targeted SIM) with a ChiralPak HSA column. L-cysteine was selected as an extraction stabilizer, and the mobile phase was composed of 100 mM ammonium acetate and 1% (v/v) acetic acid in acetonitrile (ACN) at a 97:3 ratio.

Results:

The HPLC/MS method was able to separate D- and L-5-MTHF diastereomers by isocratic elution within 20 min. It showed great linearity with the concentration range of 1 to 160 µg/mL of 5-MTHF with R2 >0.99. The method was validated for the limit of detection (LOD), limit of quantitation (LOQ), linear range, specificity, and recovery according to the guidelines described in Q2(R1) Validation of Analytical Procedures: Text and Methodology Guidance for Industry. The method was then applied for the analysis of 101 samples, and two samples were found to exceed the USP limit of ≤1% D-5-MTHF relative to L-5-MTHF (1.39 and 50.28%).

Conclusions:

This performance of HPLC-MS method established effectively determines D- and L-5-MTHF ratios in complex DS, serving as a reliable tool to detect adulteration with racemic mixtures in prenatal and other 5-MTHF-labeled containing DS. It is significantly faster than previously reported methods and possesses great selectivity in separation of the diastereomers in different forms of DS.

Highlights:

Successfully validated an HPLC-MS method for quantifying D- and L-5-MTHF diastereomers in diverse DS dosage forms, aiding enantiomeric purity assessment.

2026-03-01·BIOMEDICINE & PHARMACOTHERAPY

Folate receptor 1 activation suppresses high glucose-induced amyloidogenesis in neurons via STAT3/Nrf2 pathway-dependent mitigation of mitochondrial oxidative stress

Article

作者: Jo, Hyo Youn ; Chae, Chang Woo ; Kim, Dae Hyun ; Lee, Hyun Jik ; Jung, Young Hyun ; Lim, Jae Ryong ; Oh, Yeon Ju ; Han, Ho Jae

Diabetes is a major risk factor for diabetic encephalopathy (DE), which is closely associated with sporadic Alzheimer's disease. Folic acid (FA) receptor signaling can suppress generation of neuropathogenic amyloid-beta (Aβ) induced by high extracellular glucose, suggesting that enhanced activation of this pathway could be a therapeutic strategy against DE-associated dementia, but the precise molecular signaling mechanisms are unclear. We report that high glucose levels increased the expression of amyloid precursor protein (APP) and β-secretase (BACE1) in cultured neurons and concomitantly induced amyloidogenesis, while FA treatment suppressed high glucose-stimulated expression of APP and BACE1, Aβ release, and accumulation of mitochondrial reactive oxygen species. Expression of nuclear factor erythroid 2-related factor 2 (Nrf2) was minimal under high glucose conditions, but was significantly upregulated together with downstream antioxidant enzymes following FA co-treatment. High glucose stimulation also increased folate receptor 1 (FOLR1) mRNA expression, suggesting a compensatory protective response. While treatment with 5-methyltetrahydrofolate (5-MTHF), the activated form of folate, did not significantly alter high glucose-induced upregulation of APP and BACE1, knockdown of FOLR1 mRNA reduced high glucose-stimulated Nrf2 expression and further augmented APP and BACE1 expression under high glucose conditions. Treatment with the STAT3 inhibitor 5'15-DPP also abolished high glucose-stimulated Nrf2 expression and increased APP and BACE1 expression levels. These findings indicate that FA/FOLR1 activation suppresses high glucose-induced amyloidogenesis by mitigating mitochondrial oxidative stress via STAT3/Nrf2 pathway signaling. In conclusion, present study suggests that the FA/FOLR1/STAT3/Nrf2 pathway is an effective therapeutic target for DE.

项与左甲柳叶酸钙相关的新闻（医药）

2026-03-10

·allsci.com

FDA approves GSK’s Wellcovorin for cerebral folate transport deficiency, declines to include autism

The US FDA approved Wellcovorin (leucovorin calcium) tablets on March 10, 2026, for the treatment of cerebral folate deficiency in adult and pediatric patients with a confirmed variant in the FOLR1 gene. The decision makes leucovorin the first therapy cleared by the agency for this rare genetic condition, in which impaired folate transport into the brain leads to developmental delays, movement disorders, seizures, and other neurological complications. GSK holds the New Drug Application for Wellcovorin, and the US FDA collaborated with the company to update the drug’s labeling to include the new indication. The approval covers an expanded use of an established molecule. Leucovorin calcium has been available for decades, used primarily in oncology as a rescue agent after high-dose methotrexate and as a modulator of 5-fluorouracil. The new indication applies specifically to patients with cerebral folate transport deficiency caused by variants in the folate receptor 1 gene, designated CFD-FOLR1. The condition has an estimated prevalence of fewer than 1 in 100,000, placing it in the category of ultra-rare diseases. Prior to this approval, clinicians treated CFD-FOLR1 patients with off-label folinic acid guided by case reports and expert consensus, without a formally sanctioned therapeutic option. The US FDA based its decision on a systematic review of published literature rather than conventional prospective clinical trials. The evidence included published case reports with patient-level information and mechanistic data demonstrating that leucovorin, a reduced folate, can bypass the defective FOLR1-mediated transport pathway and enter the central nervous system through alternative mechanisms such as the reduced folate carrier. Across the published cases, treatment was associated with normalization of cerebrospinal fluid 5-methyltetrahydrofolate levels, reductions in seizure frequency, and improvements in motor and cognitive function. Earlier treatment initiation correlated with better neurological outcomes. The agency noted that this approach to using real-world evidence provides a model for regulatory evaluation in ultra-rare diseases where randomized controlled trials are not feasible. Possible side effects listed in the updated labeling include pruritus, rash, urticaria, dyspnea, rigors, impaired thermoregulation, and anaphylaxis. The approval addresses a condition with no prior regulatory-sanctioned treatment, but unmet needs remain. Published case series indicate that some patients show incomplete neurological recovery on oral leucovorin, and long-term outcome data are limited given the small number of documented cases. The regulatory precedent set by the US FDA’s reliance on literature-based evidence may influence how other candidates for this indication are evaluated. Several investigational approaches are in early-stage development, including intrathecal folinic acid formulations being studied at European academic centers, levoleucovorin in Phase II evaluation, and an AAV9-FOLR1 gene therapy program at the Children’s Hospital of Philadelphia and University of Pennsylvania that aims to restore functional folate receptor expression in the choroid plexus. None of these has advanced beyond early clinical stages, and the development landscape remains dominated by academic and investigator-initiated efforts rather than large pharmaceutical programs, a reflection of the disease’s rarity and the small trial populations involved. Notably, the regulatory review also followed earlier public discussion about broader potential uses of leucovorin in neurodevelopmental disorders. In September 2025, US health officials highlighted the possibility that leucovorin could benefit larger numbers of children with autism, based on small studies suggesting that some patients develop autoantibodies that interfere with folate transport to the brain, including one study that was later retracted. Subsequently, after reviewing the available evidence, the US FDA concluded that the data were sufficient only to support approval for the rare genetic form of cerebral folate deficiency caused by FOLR1 variants, and not for autism spectrum disorder more broadly. Your email address will not be published. Required fields are marked * Comment * Name * Email * Website

上市批准临床2期

2024-08-23

·ETPharma

Govt bans 156 medicines including antibiotics, painkillers, multivitamins: Here is the full list

New Delhi: In a significant move aimed at safeguarding public health, the Indian government has banned 156 fixed-dose combination (FDC) drugs, including a variety of antibiotics, painkillers, multivitamins, and medications for treating fever and hypertension. This decision marks the largest crackdown on FDCs since 2016, when 344 such drugs were prohibited. The Union Ministry of Health and Family Welfare issued a gazette notification on Thursday, officially prohibiting the manufacture, sale, and distribution of the banned FDCs. The ban was based on the recommendations of an expert panel that reviewed a total of 324 FDCs. Impact on Pharmaceutical Industry The banned FDCs include popular combinations such as mefenamic acid and paracetamol injections, commonly used for pain relief and fever, and omeprazole magnesium with dicyclomine HCl, used to treat abdominal pain. The ban is expected to impact major pharmaceutical companies, including Sun Pharmaceuticals, Cipla, Dr. Reddy's Laboratories, Torrent Pharmaceuticals, and Alkem Laboratories. Fixed Dose Combinations Drug Banned List Here is a table listing all 156 banned Fixed Dose Combinations (FDCs) SN Fixed Dose Combination (FDC) 1 Amylase + Protease + Glucoamylase + Pectinase + Alpha Galactosidase + Lactase + Beta-Gluconase + Cellulase + Lipase + Bromelain + Xylanase + Hemicellulase + Malt diastase + Invertase + Papain 2 Antimony Potassium Tartrate + Dried Ferrous Sulphate 3 Benfotiamine + Silymarin + L-Ornithine L-aspartate + Sodium Selenite + Folic acid + Pyridoxine hydrochloride 4 Bismuth Ammonium Citrate + Papain 5 Cyproheptadine HCl + Thiamine HCl + Riboflavine + Pyridoxine HCl + Niacinamide 6 Cyproheptadine Hydrochloride + Tricholine Citrate + Thiamine Hydrochloride + Riboflavine + Pyridoxine Hydrochloride 7 Rabeprazole Sodium (As enteric coated tablet) + Clidinium Bromide + Dicyclomine HCl + Chlordiazepoxide 8 Fungal Diastase + Papain + Nux vomica Tincture + Cardamom Tincture + Casein Hydrolysed + Alcohol 9 Mefenamic Acid + Paracetamol Injection 10 Omeprazole Magnesium + Dicyclomine HCl 11 S-adenosyl methionine + Metadoxine + Ursodeoxycholicacid BP + L-Methylfolate Calcium eq. to L- Methylfolate + Choline bitartratee + Silymarin + L-ornithine Laspartate + Inositol + Taurine 12 Silymarin + Thiamine Mononitrate + Riboflavin + Pyridoxine HCl + Niacinamide + Calcium pantothenate + Vitamin B12 13 Silymarin + Pyridoxine HCl + Cyanocobalamin + Niacinamide + Folic Acid 14 Silymarin + Vitamin B6 + Vitamin B12 + Niacinamide + Folic acid + Tricholine Citrate 15 Sodium Citrate + Citric Acid Monohydrate Flavored with Cardamom Oil, Caraway Oil, Cinnamon Oil, Clove Oil, Ginger Oil + Alcohol 16 Sucralfate + Acelofenac 17 Sucralfate + Domperidone + Dimethicone 18 Sucralfate + Domperidone 19 Tincture Ipecacuanha + Tincture Urgenia + Camphorated Opium Tincture + Aromatic Spirit of Ammonia + Chloroform + Alcohol 20 Ursodeoxycholic Acid + Metformin HCl 21 Weak Ginger tincture + Aromatic Spirit of Ammonia + Peppermint Spirit + Chloroform + Sodium Bicarbonate + Compound Cardamom + Alcohol 22 Sucralfate + Pantoprazole Sodium + Zinc Gluconate + Light Magnesium Carbonate 23 Aloe + Vitamin E Soap 24 Povidone Iodine+ Metronidazole + Aloe 25 Azelaic acid + Tea Tree Oil + Salicylic acid + Allantoin + Zinc oxide + Aloe vera + Jojoba oil + Vitamin E + Soap noodles 26 Azithromycin + Adapalene 27 Calamine + Aloes + Allantoin 28 Calamine + Diphenhydramine Hydrochloride + Aloe + Glycerine + Camphor 29 Chlorphenesin + Zinc oxide + Starch 30 Clindamycin Phosphate + Zinc acetate 31 Gamma Benzene Hexachloride + Benzocaine 32 Glucosamine hydrochloride + Diacerein + Menthol + Camphor + Capsaicin 33 Hydroxyquinone 2.0%w/w + Octyl Methoxycinnamate 5.0% w/w + Oxybenzone 30 % w/w 34 Ketoconazole +Zinc Pyrithione +D-Panthenol +Tea Tree Oil +Aloes 35 Ketoconazole +Aloe vera+ Vitamin A Acetate 36 Ketoconazole +Aloes + ZPTO 37 Kojic Acid +Arbutin +Octinoxate +Vitamin E + Mulberry 38 Lornoxicam +capsaicin +menthol+ camphor 39 Lornoxicam + Thiocolchicoside +Oleum Lini +Menthol + Methyl salicylate 40 Menthol + Aloe vera Topical Spray 41 Menthol +Lignocaine HCl +Aloe vera gel +Clotrimazole +Diphenhydramine 42 Miconazole nitrate + Gentamicin + Fluocinolone Acetonide +Zinc Sulphate 43 Miconazole +Tinidazole 44 Minoxidil +Aminexil+ Alcohol 45 Minoxidil +Azelaic acid + saw palmetto 46 Minoxidil +Aminexil 47 Pine Bark extract+ Kojic acid +Sodium Ascorbyl Phosphate 48 Povidone Iodine +Tinidazole +Zinc sulphate 49 Povidone Iodine + Ornidazole + Dexpanthenol 50 Salicyclic acid +Aloe vera+ Allantoin +D-Panthenol 51 Silver sulphadiazine +Chlorhexidine Gluconate solution +Allantoin + Aloe vera gel +Vitamin E acetate 52 Sodium salicylate + Zinc gluconate + Pyridoxine HCl 53 Tetracycline + Colistin Sulphate 54 Clomiphene +Ubidecarenone 55 Combikit of Clomiphene Citrate + Estradiol Valerate 56 Flavoxate HCl +Ofloxacin 57 Clomiphene Citrate +N-Acetylcysteine 58 Primerose Oil +Cod liver oil 59 Sildenafil Citrate +Papaverine +L-Arginine 60 Tranexamic acid +Mefenamic acid + Vitamin K1 61 Divalproex Sodium +Oxcarbazepine 62 Divalproex Sodium + Levetiracitam 63 Ergotamine tartrate +Caffeine + Paracetamol +Prochlorperazine maleate 64 Piracetam + Ginkgo biloba extracts + Vinpocetin 65 Ginkgo biloba + methylcobalamin 66 Ginkgo biloba + methylcobalamin + Alpha lipoic acid +Pyridoxine HCl 67 Ginseng Extract +Dried extract of Ginkgo Biloba 68 Meclizine HCl+ Paracetamol + Caffeine 69 Nicergoline + Vinpocetine 70 Gamma Linolenic Acid + Methylcobalamin 71 Beclomethasone Dipropionate + Neomycin Sulphate + Clotrimazole + Lignocaine HCl 72 Boric acid+ Phenylephrine HCl + Naphazoline Nitrate + Menthol + Camphor 73 Naphazoline HCl + Chlorpheniramine Maleate + Zinc Sulphate + Hydroxy Propyl Methyl Cellulose 74 Chlorpheniramine Maleate + Naphazoline HCl + Zinc Sulphate + Sodium Chloride + Hydroxy Propyl Methyl Cellulose 75 Chlorpheniramine Maleate + Naphazoline HCl + Hydroxy Propyl Methyl Cellulose 76 Chlorpheniramine Maleate + Sodium Chloride + Boric Acid + Tetrahydrozoline HCl 77 Chlorpheniramine Maleate + Phenylephrine HCl + Antipyrine 78 Ketorolac Tromethamine + Chlorpheniramine Maleate + Phenylephrine HCl + Hydroxy Propyl Methyl Cellulose 79 Ketorolac Tromethamine + Flurometholone 80 Naphazoline HCl + Zinc Sulphate + Boric Acid + Sodium Chloride+ Chlorpheniramine Maleate 81 Naphazoline HCl + Hydroxy Propyl Methyl Cellulose + Boric Acid + Borax + Menthol + Camphor 82 Naphazoline HCl + Hydroxy Propyl Methyl Cellulose + Chlorpheniramine Maleate SN Fixed Dose Combination (FDC) 83 Diphenhydramine Hydrochloride + Phenylephrine Hydrochloride + Menthol + Camphor 84 Diphenhydramine Hydrochloride + Phenylephrine Hydrochloride + Sodium Chloride + Hydroxy Propyl Methyl Cellulose 85 Diphenhydramine Hydrochloride + Phenylephrine Hydrochloride + Sodium Chloride + Methylparaben 86 Methenamine + Sodium Benzoate + Benzyl Alcohol 87 Paracetamol + Phenylephrine Hydrochloride + Chlorpheniramine Maleate 88 Paracetamol + Phenylephrine Hydrochloride + Chlorpheniramine Maleate + Caffeine 89 Propoxyphene + Chlorpheniramine Maleate 90 Propoxyphene + Phenylephrine Hydrochloride + Chlorpheniramine Maleate 91 Propoxyphene + Diphenhydramine Hydrochloride + Phenylephrine Hydrochloride 92 Sodium Benzoate + Sodium Citrate + Citric Acid 93 Vitamin A Palmitate + Vitamin C + Vitamin E + Vitamin B6 + Vitamin B12 94 Vitamin A Palmitate + Vitamin C + Vitamin E + Niacinamide 95 Vitamin B6 + Vitamin B12 + Vitamin C 96 Vitamin B6 + Vitamin B12 + Niacinamide 97 Vitamin B12 + Vitamin B6 + Vitamin C + Folic Acid 98 Vitamin B12 + Vitamin B6 + Niacinamide + Folic Acid 99 Vitamin C + Vitamin E + Vitamin A + Niacinamide 100 Vitamin D + Calcium + Magnesium 101 Vitamin D + Calcium + Magnesium + Zinc 102 Calcium + Vitamin D + Vitamin K 103 Calcium + Vitamin D + Magnesium + Zinc 104 Calcium + Vitamin D + Vitamin K + Magnesium 105 Calcium + Vitamin D + Vitamin K + Magnesium + Zinc 106 Vitamin E + Vitamin A + Vitamin C + Niacinamide 107 Vitamin E + Vitamin A + Vitamin C + Folic Acid 108 Vitamin E + Vitamin A + Vitamin C + Biotin 109 Vitamin E + Vitamin A + Vitamin C + Vitamin B12 110 Vitamin E + Vitamin C + Folic Acid 111 Vitamin E + Vitamin C + Biotin 112 Vitamin E + Vitamin C + Vitamin B12 113 Vitamin E + Vitamin C + Zinc 114 Calcium + Vitamin D + Omega-3 Fatty Acids 115 Calcium + Vitamin D + Omega-3 Fatty Acids + Vitamin K 116 Calcium + Vitamin D + Omega-3 Fatty Acids + Vitamin K + Magnesium 117 Calcium + Vitamin D + Omega-3 Fatty Acids + Vitamin K + Zinc 118 Vitamin A + Vitamin C + Vitamin E + Beta-Carotene 119 Vitamin A + Vitamin C + Vitamin E + Beta-Carotene + Zinc 120 Vitamin C + Vitamin E + Beta-Carotene 121 Vitamin C + Vitamin E + Beta-Carotene + Zinc 122 Vitamin C + Vitamin E + Selenium 123 Vitamin D + Calcium + Vitamin K + Omega-3 Fatty Acids 124 Vitamin D + Calcium + Vitamin K + Omega-3 Fatty Acids + Magnesium 125 Vitamin D + Calcium + Vitamin K + Omega-3 Fatty Acids + Zinc 126 Vitamin D + Calcium + Vitamin K + Omega-3 Fatty Acids + Biotin 127 Vitamin D + Calcium + Omega-3 Fatty Acids + Vitamin K + Selenium 128 Vitamin E + Vitamin A + Vitamin C + Zinc 129 Vitamin E + Vitamin A + Vitamin C + Selenium 130 Vitamin E + Vitamin A + Vitamin C + Biotin 131 Vitamin E + Vitamin A + Vitamin C + Folic Acid + Niacinamide 132 Vitamin E + Vitamin C + Beta-Carotene + Zinc 133 Vitamin C + Vitamin E + Biotin + Folic Acid 134 Vitamin C + Vitamin E + Beta-Carotene + Folic Acid 135 Vitamin C + Vitamin E + Beta-Carotene + Selenium 136 Vitamin E + Vitamin C + Beta-Carotene + Biotin 137 Vitamin D + Calcium + Omega-3 Fatty Acids + Vitamin K + Biotin 138 Vitamin D + Calcium + Omega-3 Fatty Acids + Vitamin K + Selenium 139 Vitamin D + Calcium + Omega-3 Fatty Acids + Vitamin K + Vitamin B12 140 Vitamin D + Calcium + Omega-3 Fatty Acids + Vitamin K + Vitamin B6 141 Vitamin D + Calcium + Omega-3 Fatty Acids + Vitamin K + Folate 142 Calcium + Vitamin D + Magnesium + Vitamin K + Omega-3 Fatty Acids 143 Calcium + Vitamin D + Magnesium + Vitamin K + Biotin 144 Calcium + Vitamin D + Magnesium + Vitamin K + Selenium 145 Calcium + Vitamin D + Magnesium + Vitamin K + Vitamin B12 146 Calcium + Vitamin D + Magnesium + Vitamin K + Folate 147 Calcium + Vitamin D + Vitamin K + Omega-3 Fatty Acids + Vitamin B6 148 Calcium + Vitamin D + Vitamin K + Omega-3 Fatty Acids + Vitamin B12 149 Calcium + Vitamin D + Vitamin K + Omega-3 Fatty Acids + Folic Acid 150 Calcium + Vitamin D + Vitamin K + Omega-3 Fatty Acids + Biotin 151 Calcium + Vitamin D + Vitamin K + Omega-3 Fatty Acids + Selenium 152 Vitamin A + Vitamin C + Vitamin E + Omega-3 Fatty Acids 153 Vitamin A + Vitamin C + Vitamin E + Omega-3 Fatty Acids + Zinc 154 Vitamin A + Vitamin C + Vitamin E + Omega-3 Fatty Acids + Biotin 155 Vitamin A + Vitamin C + Vitamin E + Omega-3 Fatty Acids + Selenium 156 Vitamin A + Vitamin C + Vitamin E + Omega-3 Fatty Acids + Vitamin B12

上市批准

2024-01-02

·SYNAPSE

Exploring MR antagonists: What They Are and How to Keep Up with the Latest Advances

The role of the MR (Mineralocorticoid Receptor) in the human body is crucial for maintaining electrolyte and fluid balance. MR is a type of receptor found in various tissues, including the kidneys, heart, and brain. When activated by the hormone aldosterone, MR regulates the reabsorption of sodium and water in the kidneys, leading to increased blood volume and blood pressure. This receptor also plays a role in regulating potassium levels and maintaining the balance of electrolytes. Dysfunction of the MR can lead to conditions such as hypertension, electrolyte imbalances, and cardiovascular diseases. Understanding the role of MR is essential for developing targeted therapies in the pharmaceutical industry. Based on the analysis of the target MR, it is evident that Bayer AG and Pfizer Inc. are among the companies growing fastest in this field. The R&D progress of these companies, along with oOh!media Group Pty Ltd., Daiichi Sankyo Co., Ltd., CMP Development LLC, Estetra SPRL, and China National Pharmaceutical Group Co., Ltd., is promising. The approved indications cover a wide range of therapeutic areas, indicating the diversity of research in the target MR. Small molecule drugs dominate the development phases, suggesting intense competition in this area. The involvement of various countries/locations, including China, highlights the global nature of the target MR. Overall, the current competitive landscape indicates a promising future for the development of drugs under the target MR. How do they work?MR antagonists, also known as mineralocorticoid receptor antagonists, are a class of drugs that block the action of the mineralocorticoid receptor. The mineralocorticoid receptor is a protein found in various tissues, including the kidney, heart, and brain, and it plays a crucial role in regulating electrolyte balance and blood pressure. From a biomedical perspective, MR antagonists are primarily used in the treatment of conditions such as hypertension (high blood pressure) and heart failure. By blocking the mineralocorticoid receptor, these drugs inhibit the effects of aldosterone, a hormone that promotes sodium and water retention and potassium excretion. This leads to a reduction in fluid volume and blood pressure, helping to manage hypertension and improve symptoms in heart failure patients. Common examples of MR antagonists include spironolactone and eplerenone. These drugs are typically prescribed in combination with other medications to optimize blood pressure control and manage fluid balance in patients with cardiovascular disorders. It's important to note that MR antagonists should be used under medical supervision, as they can have potential side effects and interactions with other medications. Close monitoring of electrolyte levels, particularly potassium, is necessary during treatment with MR antagonists to prevent imbalances. List of MR AntagonistsThe currently marketed MR antagonists include: FinerenoneDrospirenoneEsaxerenoneVistaMRDrospirenone/Ethinyl Estradiol/Levomefolate CalciumDrospirenone/EstetrolDrospirenone/EstradiolEplerenoneDrospirenone/Ethinyl EstradiolFludrocortisone AcetateFor more information, please click on the image below. What are MR antagonists used for?MR antagonists are primarily used in the treatment of conditions such as hypertension (high blood pressure) and heart failure. For more information, please click on the image below to log in and search. How to obtain the latest development progress of MR antagonists?In the Synapse database, you can keep abreast of the latest research and development advances of MR antagonists anywhere and anytime, daily or weekly, through the "Set Alert" function. Click on the image below to embark on a brand new journey of drug discovery!

100 项与左甲柳叶酸钙相关的药物交易

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KEGG	Wiki	ATC	Drug Bank
D09354	左甲柳叶酸钙	B03A	DB11256

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适应症	国家/地区	公司	日期
膳食补充剂	美国	Merck KGaA	2009-11-23

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适应症	最高研发状态	国家/地区	公司	日期
避孕	临床1期	荷兰	Bayer AG	2006-10-01
天使综合征	临床前	美国	Rady Children's Hospital-San Diego	2011-12-01
天使综合征	临床前	美国	National Institutes of Health	2011-12-01
天使综合征	临床前	美国	University of California	2011-12-01

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT01853280 (CTgov)	临床2/3期	注意缺陷障碍伴多动	47	L-methylfolate+OROS-Methylphenidate	構憲夢淵獵願齋構遞獵(顧壓積襯餘憲鬱夢繭餘) = 簾齋衊餘簾簾獵鹽齋鏇鬱鹹醖蓋艱蓋鏇觸繭繭 (鬱願醖蓋鬱蓋鬱膚鏇膚, 10.4) 更多	-	2017-11-14
NCT01570088 (Pubmed \| J Nutr)	N/A	-	45	Wheat rolls fortified with microencapsulated L-5-MTHF	憲鏇蓋夢憲顧餘醖願壓(網淵憲網壓壓艱淵糧壓) = 窪製選觸憲蓋構選觸鏇鹹製糧憲選獵願鹹網範 (艱鏇鹽廠繭製觸鏇網淵 ) 更多	-	2013-06-01
				Wheat rolls fortified with equimolar folic acid	憲鏇蓋夢憲顧餘醖願壓(網淵憲網壓壓艱淵糧壓) = 蓋鏇構艱淵廠壓膚廠醖鹹製糧憲選獵願鹹網範 (艱鏇鹽廠繭製觸鏇網淵 ) 更多
NCT00348933 (CTgov)	N/A	天使综合征	90	B12+Metafolin+Creatine+Betaine (Treatment (Metafolin/Creatine/Betaine/B12))	鬱選餘膚壓壓選窪廠鹽(繭夢蓋獵憲構蓋繭鏇積) = 艱醖鹹範獵壓範選選繭餘網願艱製網遞鹹糧齋 (壓憲簾願廠遞構餘夢鬱, 7.8) 更多	-	2012-09-24
				Metafolin (Treatment (Metafolin/Creatine/Betain/B12))	鬱觸獵製餘構廠膚淵鏇(壓衊壓鏇鏇憲遞簾願觸) = 壓齋網蓋衊積壓襯願範鏇艱築鏇醖醖夢鹽艱顧 (顧窪醖鏇淵鹽壓襯餘製, 224.5) 更多
NCT01253187 (CTgov)	临床1期	避孕	44	EE 0.02 mg/DRSP 3 mg (YAZ, BAY86-5300) (EE 0.02 mg/DRSP 3 mg (YAZ, BAY86-5300))	廠築襯製襯齋憲範鬱壓(鏇顧艱膚窪夢觸鹹憲夢) = 憲顧窪獵壓壓願願壓構願膚襯範襯鹽範鑰艱蓋 (獵積願顧淵糧鏇衊糧窪, 衊衊廠觸襯糧顧觸廠積 ~ 蓋餘鬱選鑰衊構壓選顧) 更多	-	2011-05-09
				EE 0.02 mg/DRSP 3 mg/L-5-MTHF Ca 0.451 mg (EE20/DRSP/L-5-MTHF Ca) (EE 0.02mg/DRSP 3mg/L-5-MTHF Ca 0.451mg (EE20/DRSP/L-5-MTHF Ca))	廠築襯製襯齋憲範鬱壓(鏇顧艱膚窪夢觸鹹憲夢) = 選窪壓積網築憲襯網壓願膚襯範襯鹽範鑰艱蓋 (獵積願顧淵糧鏇衊糧窪, 選憲觸壓襯構襯醖鹽糧 ~ 構艱淵襯鬱鹹鹹衊鏇願) 更多