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Drug Discovery: Overview01:26

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Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
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Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
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Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
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A drug's physicochemical properties fundamentally influence its metabolism. For instance, a drug's molecular size and shape critically determine its interaction with enzymes and transporters — larger drugs may face difficulty reaching enzyme active sites, altering their metabolic pathways. The pKa of a drug, which establishes its ionization state, can impact its solubility and absorption, thereby influencing metabolism.
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The physicochemical characteristics of drugs play a crucial role in formulating stable and bioavailable drug products. The solubility of a drug, governed by the varying pH along the GI tract and its dissociation constant (pKa), is pivotal in determining its ionization state and absorption rate. Notably, weak acids and bases remain unionized and are absorbed more rapidly.
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The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
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Trends in small molecule drug properties: A developability molecule assessment perspective.

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Molecule physicochemical properties impact drug development. A constant H-bond donor count is key for oral drugs, while other properties influence attrition. Target class also guides formulation strategies.

Keywords:
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Area of Science:

  • Pharmaceutical sciences
  • Medicinal chemistry
  • Drug development

Background:

  • Developability assessment is crucial for biopharmaceutical success, bridging medicinal chemistry discovery and CMC development.
  • Existing literature often focuses on ADMET properties from a medicinal chemistry viewpoint, neglecting CMC development impacts.
  • A systematic analysis is needed to understand physicochemical property trends and their CMC implications.

Purpose of the Study:

  • To analyze trends in physicochemical properties of drug molecules and their impact on Chemistry Manufacturing Controls (CMC) development.
  • To investigate the relationship between molecular properties, pharmaceutical attrition, and drug approval over time.
  • To explore how target class influences formulation and drug delivery strategies.

Main Methods:

  • Comprehensive analysis of physicochemical properties using the drug repurposing hub dataset.
  • Temporal analysis of FDA-approved oral molecules (1900-2020).
  • Attrition analysis correlating properties like cLogP, H-bond acceptors, polar surface area, and fraction of sp3 carbons with compound attrition.

Main Results:

  • A constant H-bond donor count is the sole preserved physicochemical property in FDA-approved oral drugs over a century, crucial for permeability and lattice energy.
  • Partition-distribution coefficient, H-bond acceptors, polar surface area, and fraction of sp3 carbons are linked to compound attrition.
  • Opposing trends in properties like cLogP, cLogD, and Fsp3 were observed in recent pharmaceutical attrition versus historical drug approvals.
  • Target class influences formulation; nuclear hormone receptor ligands benefit from lipid-based delivery, while kinase inhibitors present formulation challenges due to solubility issues.

Conclusions:

  • Understanding the impact of molecular properties on performance attributes accelerates candidate selection and risk assessment in drug development.
  • Physicochemical property trends and their influence on CMC development require careful consideration.
  • Tailoring formulation and drug delivery strategies based on target class is essential for successful drug development.