Chemical Biology and Drug Design

OCTOBER 5, 2023

Aromatic aldehydes, which increase the oxygen affinity of human hemoglobin to prevent polymerization of sickle hemoglobin and inhibit red blood cell (RBC) sickling, have been the subject of keen interest for the development of effective treatment against SCD.

Metabolic Stability 100

Metabolic Stability Treatment Disease Research 100

Metabolite Tales Blog

JULY 5, 2023

Current macrocycles in clinical use generally focus on treatment of infectious diseases, cancer and auto-immune disorders. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4].

Metabolic Stability 52

Metabolic Stability Drugs FDA Approval Treatment 52

Metabolite Tales Blog

JULY 5, 2023

Current macrocycles in clinical use generally focus on treatment of infectious diseases, cancer and auto-immune disorders. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4].

Metabolic Stability 52

Metabolic Stability Drugs FDA Approval Treatment 52

Metabolite Tales Blog

MAY 12, 2023

This was surprising given that replacement of a phenyl with a pyrimidine and fluorination of aryl or heteroaryl rings are techniques often used to increase metabolic stability. 2019 Oct 14;58(42):14824-14848, [link] [4] See [link] [5] The Dark Side of Fluorine. 3] The Fluorination of C-H Bonds: Developments and Perspectives.

Drugs 52

Drugs Small Molecule Metabolic Stability FDA Approval 52

Metabolite Tales Blog

MARCH 1, 2023

9 The evidence here is that treatment with P450 inhibitors removed the toxic effects seen in the compounds of interest. 2019, 14, 2, 142–16 [link] 10 Chem. 1990, 1034, 233-237 [link] 13 Metabolism of pyrazole in the Rat [link] 14 Drug Metab. 11 Figure 11 Pyrazoles – more stable to oxidative cleavage? link] 12 Biochim.

Metabolic Stability 52

Metabolic Stability Pharmacokinetics Drugs Science 52

Metabolite Tales Blog

APRIL 4, 2023

3 Metabolism differences at steady state Adagrasib, Mirati’s irreversible KRASG12C inhibitor for treatment of non-small cell lung cancer is mainly metabolised by CYP3A4. Interestingly however, since adagrasib (MRTX849) inhibits CYP3A4 following multiple dosing, its metabolism is subsequently taken over by other CYPs.

Small Molecule 52

Small Molecule FDA Approval FDA Drugs 52