Deuterated drugs in clinical trials
Phase 3
Molecule Name | Compound Code | Sponsor | Clinical Trail Phase | Therapeutic Indication | Description |
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Donafenib | CM 4307 | Suzhou Zelgen Biopharma | Phase 3 | Colorectal Cancer, Thyroid Cancer | Deuterium derivative of sorafenib, is an oral small molecule multikinase inhibitor of multiple receptor kinases. Donafenib is being developed by Suzhou Zelgen Biopharmaceuticals Co., Ltd. (Zelgen) for the treatment of various cancers, including hepatocellular carcinoma, colorectal cancer and thyroid cancer |
Chemically modified vitamin A | ALK-001 | Alkeus Pharmaceuticals | Phase 3 | Geographic atrophy, Age related maculardegeneration [AMD] | ALK-001 is an oral, once daily, chemically-modified form of vitamin A designed to reduce the production of toxic vitamin A dimers by substituting vitamin A and retaining its natural functions. In preclinical trials, ALK-001 has been shown to slow the formation of vitamin A dimers and prevent the disease in mice. |
Ethyl linoleate [Di-deuterated] | RT-001 | Retrotope | Phase 3 | Friedreich's ataxia Infantile neuroaxonal dystrophy Neuroaxonal dystrophies | It is deuterium labeled Ethyl linoleate that inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators. |
Deucravacitinib | BMS-986165 | Bristol myers squibb | Phase 3 | Psoriasis; Psoriatic arthritis; Systemic lupus erythematosus | Deucravacitinib is an oral medication developed for the treatment of various autoimmune diseases. It is a selective tyrosine kinase 2 (TYK2) inhibitor. TYK2 is part of the Janus kinase (JAK) family, which plays a significant role in the signaling pathways of various cytokines involved in immune responses and inflammation. |
Deuruxolitinib | CTP-543 | Concert Pharmaceuticals | Phase 3 | Alopecia areata | Is an investigational drug currently being studied for the treatment of alopecia areata, an autoimmune condition that causes hair loss. It is a Janus kinase (JAK) inhibitor, specifically targeting the JAK1 and JAK2 enzymes, which play a role in the inflammatory pathways involved in autoimmune diseases. By inhibiting these enzymes, deuruxolitinib aims to reduce the inflammatory response that leads to hair loss in alopecia areata patients. |
Deudextromethorphan | AVP-786 | Avanir Pharmaceuticals | Phase 3 | Alzheimer's Disease, Schizophrenia | Deudextromethorphan/quinidine is a combination of deudextromethorphan (d-DXM; deuterated (d6) dextromethorphan and quinidine for the treatment of a variety of neurological and psychiatric indications. Deuteration of DXM hinders its metabolism by CYP2D6 into DXO, thereby allowing for lower doses of quinidine in the combination. |
Phase 2
Molecule Name | Compound Code | Sponsor | Clinical Trail Phase | Therapeutic Indication | Description |
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D9-Ivacaftor | CTP-656 (VX-561) | Concert Pharmaceuticals | Phase 2 | Cystic fibrosis | Ivacaftor is in a class of medications called cystic fibrosis transmembrane conductance regulator (CFTR) potentiators. It works by improving the function of a protein in the body to decrease the build-up of thick mucus in the lungs and improving other symptoms of cystic fibrosis. |
Deuterated-(R)-Pioglitazone | PXL065 (DRX- 065) | Poxel SA | Phase 2 | Nonalcoholic steatohepatitis | Pioglitazone is an oral antidiabetic medication belonging to the thiazolidinedione class, primarily used to treat type 2 diabetes mellitus. It works by increasing the body's sensitivity to insulin, thereby helping to control blood sugar levels. Pioglitazone acts as an agonist for the peroxisome proliferator-activated receptor gamma (PPARĪ³), which plays a key role in the regulation of glucose and lipid metabolism. |
PCS-499 | CTP-499 | Concert Pharmaceuticals | Phase 2 | Necrobiosis lipoidica | PCS-499 is designed to treat conditions characterized by chronic inflammation and fibrotic processes, such as necrobiosis lipoidica (NL), a rare inflammatory skin disorder. PCS-499 is believed to exert its effects through multiple mechanisms, including anti-inflammatory, antifibrotic, and analgesic pathways. |
Avadomide | CC-122 | Celgene | Phase 2 | Malignant Melanoma | Avadomide (also known as CC-122) is an investigational drug developed by Celgene, now part of Bristol-Myers Squibb. It belongs to a class of drugs known as pleiotropic pathway modulators and has shown potential in treating various cancers and inflammatory conditions. Avadomide has been studied primarily in the context of hematologic malignancies such as non-Hodgkin lymphoma (NHL) and multiple myeloma. |
Chemically-modified vitamin A | ALK-001 | Alkeus Pharmaceuticals | Phase 2 | Stargardt disease | ALK-001 is an oral, once daily, chemically-modified form of vitamin A designed to reduce the production of toxic vitamin A dimers by substituting vitamin A and retaining its natural functions. In preclinical trials, ALK-001 has been shown to slow the formation of vitamin A dimers. |
Ethyl linoleate [Di-deuterated] | RT-001 | Retrotope | Phase 2 | Amyotrophic lateral sclerosis;Progressive supranuclear palsy | Deulinoleate ethyl is recognized by cells as identical to normal linoleic acid. But when taken up, it is converted into 13,13-d2-arachidonic acid, a heavy isotope version of arachidonic acid, that gets incorporated into lipid membranes. The deuterated compound resists the non-enzymatic lipid peroxidation (LPO) through isotope effect |
Deucravacitinib | BMS-986165 | Bristol Myers Squibb | Phase 2 | Ulcerative colitis | Deucravacitinib, sold under the brand name Sotyktu, is a medication used for the treatment of moderate-to-severe plaque psoriasis. It acts as a highly selective allosteric inhibitor of non-receptor tyrosine-protein kinase 2 (TYK2) |
Deudextromethorphan | AVP-786 | Avanir Pharmaceuticals | Phase 2 | Neurobehavioral disinhibition | Deudextromethorphan/quinidine (d-DXM/Q; developmental code names AVP-786, CTP-786) is a combination of deudextromethorphan (d-DXM; deuterated (d6) dextromethorphan (DXM)) and quinidine (Q) which is under development by Avanir Pharmaceuticals for the treatment of a variety of neurological and psychiatric indications. Deuteration of DXM hinders its metabolism by CYP2D6 into DXO, thereby allowing for lower doses of quinidine in the combination. This in turn allows for lower potential for drug interactions and cardiac adverse effects caused by quinidine. |
Phase 1
Molecule Name | Compound Code | Sponsor | Clinical Trail Phase | Therapeutic Indication | Description |
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VX 984 | M 9831 | Merck KGaA | Phase 1 | Solid tumours | VX-984 (M9831) is administered alone and in combination with pegylated liposomal doxorubicin (PLD) to evaluate the safety, tolerability, and to determine the maximum tolerated dose (MTD) and preliminary evidence of efficacy of VX-984 in combination with PLD in participants with advanced solid tumors. VX-984 efficiently inhibits NHEJ, resulting in compensatory increases in alternative repair pathways, increases DSBs, and appears to affect transformed cells preferentially. |
Deuterated sodium oxybate | JZP 386 | Concert Pharmaceuticals Jazz Pharmaceuticals | Phase 1 | Narcolepsy | Sodium oxybate is a medication used to treat narcolepsy, specifically to reduce excessive daytime sleepiness and cataplexy (sudden muscle weakness). Deuterated sodium oxybate is a modified form of sodium oxybate (also known as gamma-hydroxybutyrate or GHB). The deuterated form is being explored to improve the pharmacokinetic properties, such as extending the half-life, which could lead to more consistent therapeutic effects and potentially reduced dosing frequency. |
Osimertinib | Dosimertinib | AstraZeneca | Phase 1 | EGFR mutation-positive non-small-lung cancer | Dosimertinib is a potent and orally active EGFR inhibitor, which decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-shows antiproliferative and anti-tumor activity and has the potential for the research of non-small-cell lung cancer (NSCLC) |
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