Chemical Biology and Drug Design

SEPTEMBER 20, 2023

Magnoflorine increased the systemic exposure and metabolic stability and suppressed the transport of luteolin. Abstract Both luteolin and magnoflorine have been reported to regulate the development of breast cancer, which makes them easier to co-administrate.

Pharmacokinetics 100

Pharmacokinetics Metabolic Stability Regulations Research 100

ASPET

OCTOBER 24, 2023

PANK2 is one of three kinases that initiate and regulate coenzyme A biosynthesis from vitamin B5 and the ability of BBP-671, an allosteric activator of pantothenate kinases, to enter the brain and elevate coenzyme A was investigated. Significance Statement The blood brain barrier represents a major hurdle for drugs targeting brain metabolism.

Metabolic Stability 100

Metabolic Stability Pharmacokinetics Regulations Treatment 100

Metabolite Tales Blog

DECEMBER 13, 2023

UGT1A enzymes were shown to be down-regulated in several cancers, and mutations in UGT genes enhance the risk of bladder cancer in smokers [10]. A route to be avoided or a desired route of metabolism? 8(2):3640-3648; [link] [11] Pharmacokinetics of the Multi-kinase Inhibitor Pexidartinib: Mass Balance and Dose Proportionality.

Small Molecule 59

Small Molecule Metabolic Stability Treatment Pharmacokinetics 59

Metabolite Tales Blog

APRIL 4, 2023

Tapinarof is a topical aryl hydrocarbon receptor–modulating agent approved for the treatment of psoriasis by downregulating proinflammatory interleukin-17 and regulating expression of the skin-barrier proteins filaggrin and loricrin. Drug metabolism in drug discovery and development. Dermavant’s tapinarof is one such friend.

Small Molecule 52

Small Molecule FDA Approval FDA Drugs 52