Remove Drugs Remove Pharmacokinetics Remove Small Molecule
article thumbnail

Analyzing Oxygen Atom Distribution in FDA‐Approved Drugs to Enhance Drug Discovery Strategies

Chemical Biology and Drug Design

Analysis of prevalence of ring, nonring, sp 3 -, and sp 2 -hybridized oxygen in approved drugs. For the first time, analysis of distribution of different types of oxygen from center of mass of a molecule. In approved drugs, majority of oxygen atoms are present within 4 from the COM of the molecule.

article thumbnail

How GPCR agonists, including antibodies, are shaping the future of metabolic care

Drug Target Review

G protein-coupled receptors (GPCRs) represent a cornerstone of modern drug discovery due to their crucial role in regulating human physiology and their involvement in numerous diseases. In the early days, each GPCR target required its own structure-modulating ConfoBody to be identified before starting any drug discovery.

Insiders

Sign Up for our Newsletter

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

article thumbnail

PALAZESTRANT

New Drug Approvals

It is a small molecule with a dual mechanism of action, acting as both a complete estrogen receptor antagonist and a selective estrogen receptor degrader (SERD). Oral Administration: Palazestrant is an orally available drug. PALAZESTRANT CAS 2092925-89-6 OP-1250, VU35KM56Q4 449.6 ribociclib).

article thumbnail

Shifting the ADC focus from antibody to payload

Drug Target Review

As antibody-drug conjugates (ADCs) gain traction across oncology and begin to expand into other therapeutic areas, a persistent challenge remains: the design and optimisation of payloads. The ADC itself is not necessarily a large molecule – it’s a small molecule with aspects of a large molecule, and vice versa.

article thumbnail

Metabolism of 2023 FDA Approved Small Molecules – PART 2

Metabolite Tales Blog

Where data was publicly available, the routes of human metabolism for each of the drugs in this subset is listed in Table 1. Metabolites found in humans are also observed in monkeys, and all metabolites were found to possess <10% of the activity of the parent drug. of the administered radiolabel in the human ADME study.

article thumbnail

The rising impact of biomarkers in early clinical development

Drug Target Review

In a recent survey conducted by ICON, Plc, biomarker selection was identified by 35 percent of respondents as a top challenge among drug developers for phase I trials, second only to navigating regulatory compliance (- 38 percent). To qualify as endpoints, biomarkers used in early phases must be relevant to later stages of drug development.

article thumbnail

Metabolism of 2022 FDA approved small molecule drugs PART 2

Metabolite Tales Blog

Metabolism of 2022 FDA approved small molecule drugs part 2 Mixing it Up By Julia Shanu-Wilson In Part 1 of this topic we looked at metabolism of the small molecule drugs approved by the FDA in 2022 that were mediated by CYP3A4.