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Deuterated drug development

Development of deuterium-enriched drugs for enhanced metabolism and pharmacokinetics properties

Deuterated drug development

Clearsynth is a Contract Research Organization providing services like Preclinical drug discovery (from conceptualization to pre clinical POC) using different Artificial Intelligence and Machine learning (AI/ML) tools. The R&D team is capable of working on diverse projects starting from identifying key therapeutic areas, Identification of hit, Optimization from Hit to lead and in Vivo POC establish in animal disease model.

Deuterium (2H; D) is a stable and non-radioactive isotope of hydrogen and it plays an important role in various fields of science The uniqueness of deuterium (D) over hydrogen (H) is that C-D bond is shorter and more stable compared to C-H bond. This unique feature makes it difficult to break C-D bond and more stable towards the enzymatic cleavage (CYP450) in in-vivo system.

Recently, approval of the deuterated analogue of tetrabenazine ( Austedo; TEVA) and Deucravacitinib (Sotyktu, Bristol Myers Squibb) opened an entirely new world in the field of drug discovery and various Pharmaceutical companies directed their Research and Development efforts towards the development of deuterated analogue of existing non-deuterated drugs to modify drug pharmacokinetics profile.

Clearsynth has expertise in the development of deuterated analogs of known drug molecule by systematic analysis of compounds from literature and selective deuteration at soft spots to improve the pharmacokinetics (Increase AUC, increase Half Life, reduce Clearance), mitigate toxic effect of metabolites, stabilize active metabolite, reduce booster dose (CYP inhibitors) and improve half-life and bioavailability.

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Compound Screening

Systematic analysis of literature for the selection of potential candidates for deuteration. Algorithm-based analysis for the identification of soft spots for deuteration with expected outcome.

Chemistry Services

Synthesis of proposed deuterated analog ( in mg) with >95% isotopic purity for Proof of concept (POC) and in-vivo assay. Bulk scale for PK and toxicology studies in higher specie.

Biology Services

In-vitro and in-vivo assay (in animal model) for proof of concept. Pharmacokinetic study and preliminary TOX study in animal model.

Development

Bulk scale production (in kg scale) non-GMP and GMP for formulation and clinical stage development.