ArticleThe Journal of steroid biochemistry and molecular biology2023
Selectivity of osilodrostat as an inhibitor of human steroidogenic cytochromes P450.
Article in The Journal of steroid biochemistry and molecular biology, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers, 1 of them a synthesis that pooled it.
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Who cites it
14 citing papers in PubMed, 1 synthesis or guideline pooled it, 17 citations in OpenAlex.
- Comparative efficacy and safety of aldosterone synthase inhibitors in hypertension: a Bayesian network meta-analysis of randomised controlled rials.Open heart · 2025Pooled it
- Protracted osilodrostat-induced pan-adrenal steroidogenic suppression and adrenal size reduction in Cushing disease.JCEM case reports · 2026Article
- Baxdrostat versus osilodrostat: steroid biosynthesis in human adrenocortical cells.Endocrine connections · 2026Article
- Aldosterone synthase inhibitors: a new option for antihypertensive, cardio-renal protection.Hypertension research : official journal of the Japanese Society of Hypertension · 2026Review
- Histopathological evidence of osilodrostat-induced regression of a cortisol-producing adrenocortical adenoma.JCEM case reports · 2026Article
- Chronotherapy With Once-Daily Osilodrostat Improves Cortisol Rhythm, Quality of Life, and Sleep in Cushing's Syndrome.The Journal of clinical endocrinology and metabolism · 2025Article
- Osilodrostat Treatment for Adrenal and Ectopic Cushing Syndrome: Integration of Clinical Studies With Case Presentations.Journal of the Endocrine Society · 2025Review
- Exploring P450 superfamily diversity with P450Atlas - Online tool for automated subfamily assignment.Protein science : a publication of the Protein Society · 2025Article
- Medical Treatment of Cushing's Syndrome.Endocrinology and metabolism (Seoul, Korea) · 2025Review
- Prediction of pharmacokinetic/pharmacodynamic properties of aldosterone synthase inhibitors at drug discovery stage using an artificial intelligence-physiologically based pharmacokinetic model.Frontiers in pharmacology · 2025Article
- Steroidogenic cytochrome P450 enzymes as drug target.Toxicological research · 2024Review
- Kinetics of Intermediate Release Enhances P450 11B2-Catalyzed Aldosterone Synthesis.Biochemistry · 2024Article
- Aldosterone Synthase Inhibitors for Cardiorenal Protection: Ready for Prime Time?Kidney & blood pressure research · 2024Review
- Severe Cushing's syndrome from an ectopic adrenocorticotropic hormone-secreting neuroendocrine tumour treated by osilodrostat.Endocrinology, diabetes & metabolism case reports · 2023Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Osilodrostat (LCI699) is a potent inhibitor of the human steroidogenic cytochromes P450 11β-hydroxylase (CYP11B1) and aldosterone synthase (CYP11B2). LCI699 is FDA-approved for the treatment of Cushing disease, which is characterized by chronic overproduction of cortisol. While phase II and III clinical studies have proven the clinical efficacy and tolerability of LCI699 for treating Cushing disease, few studies have attempted to fully assess the effects of LCI699 on adrenal steroidogenesis. To this end, we first comprehensively analyzed LCI699-mediated inhibition of steroid synthesis in the NCI-H295R human adrenocortical cancer cell line. We then studied LCI699 inhibition using HEK-293 or V79 cells stably expressing individual human steroidogenic P450 enzymes. Our studies using intact cells confirm the potent inhibition of CYP11B1 and CYP11B2 with negligible inhibition of 17-hydroxylase/17,20-lyase (CYP17A1) and 21-hydroxylase (CYP21A2). Furthermore, partial inhibition of the cholesterol side-chain cleavage enzyme (CYP11A1) was observed. To calculate the dissociation constant (K
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.