Remove 2012 Remove Pharmacokinetics Remove Small Molecule
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New molecular insights on medical cannabis

Drug Target Review

2,8-10 However, the number of compounds with satisfying pharmacokinetic parameters (PKD) are limited, with most unable to cross the blood-brain barrier or go sufficiently deep into a malignant tumour. 2012 Feb 1;40(1):31–6. Structure–Activity Relationships of Small Molecule Autotaxin Inhibitors with a Discrete Binding Mode.

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Antibody-drug conjugates payloads: then, now and next

Drug Target Review

Groundbreaking strategies like proteolysis-targeting chimeric molecules (PROTACs) are also being explored. 6 Combining the effect of payloads with different mechanisms of action – an approach that revolutionised small molecule chemotherapy – also holds the promise of enhanced therapeutic activity for ADCs.

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Game-changing pan-TEAD inhibitor for solid tumours

Drug Target Review

The current version of Chemistry42 uses over 40 generative models, including generative autoencoders and generative adversarial networks as well as both structure-based and ligand-based drug design to generate and optimise de novo small molecules.

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ATICAPRANT

New Drug Approvals

14] Pharmacokinetics The oral bioavailability of aticaprant is 25%. [1] “LY2456302 is a novel, potent, orally-bioavailable small molecule kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders” Neuropharmacology. Rankovic Z, Hargreaves R, Bingham M (2012).