Levoketoconazole

Generic Name: Levoketoconazole

Brand Names: Recorlev

Drug Type: Small Molecule

Chemical Formula: C_₂₆H_₂₈Cl_₂N_₄O_₄

CAS Number: 142128-57-2

Unique Ingredient Identifier: 2DJ8R0NT7K

Background: Cushing's syndrome (CS) is underpinned by chronic hypercortisolism leading to multisystem morbidity, including effects on the cardiovascular and endocrine systems, metabolic syndrome with accompanying changes in body composition, neuropsychiatric effects, changes in blood pressure and chemistry, and opportunistic infections. Ketoconazole has been used both on- and off-label to treat CS due to its ability to inhibit cortisol production. Still, toxicity has limited its use, notably hepatic toxicity and a tendency to prolong the QT interval. Levoketoconazole is one of two enantiomers present in racemic ketoconazole. It possesses most of the inhibitory effect towards steroidogenic enzymes, making it an attractive candidate for CS treatment with a potentially lower toxicity profile than its racemate.

Levoketoconazole was approved by the FDA on December 30, 2021, and is currently marketed under the registered trademark RECORLEV by Xeris Pharmaceuticals, Inc.

Indication: Levoketoconazole is indicated for the treatment of endogenous hypercortisolemia in adult patients with Cushing’s syndrome for whom surgery is not an option or has not been curative. Levoketoconazole is not indicated for the treatment of fungal infections.

Associated Conditions: Endogenous Cushing's Syndrome

Clinical Trials

Bioavailability of Levoketoconazole and Ketoconazole Tablets

Phase 1

Completed

Conditions: Healthy

Interventions: Drug: Levoketoconazole
Drug: Ketoconazole

First Posted Date: 2019-12-26

Last Posted Date: 2020-01-31

Lead Sponsor: Cortendo AB

Target Recruit Count: 34

Registration Number: NCT04212000

Locations: 🇺🇸
Pharmaceutical Research Associates, Inc., Salt Lake City, Utah, United States

Drug Interaction Study of Levoketoconazole and Metformin

Phase 1

Completed

Conditions: Healthy Subjects

Interventions: Drug: Metformin 500 mg Oral Tablet
Drug: Levoketoconazole 150 - 600 mg (BID)

First Posted Date: 2019-03-19

Last Posted Date: 2019-08-30

Lead Sponsor: Cortendo AB

Target Recruit Count: 32

Registration Number: NCT03880825

Locations: 🇺🇸
Clinical Pharmacology of Miami, LLC, Miami, Florida, United States

Levoketoconazole Food Effect Study in Healthy Subjects

Phase 1

Completed

Conditions: Healthy Subjects

Interventions: Drug: levoketoconazole

First Posted Date: 2018-12-07

Last Posted Date: 2019-02-04

Lead Sponsor: Cortendo AB

Target Recruit Count: 22

Registration Number: NCT03768388

Locations: 🇺🇸
Clinical Pharmacology of Miami, LLC, Miami, Florida, United States

Open-label Treatment in Cushing's Syndrome

Phase 3

Completed

Conditions: Cushing Syndrome
Cushing Disease

Interventions: Drug: Levoketoconazole

First Posted Date: 2018-08-08

Last Posted Date: 2023-05-10

Lead Sponsor: Cortendo AB

Target Recruit Count: 51

Registration Number: NCT03621280

Locations: 🇺🇸
Columbia University Medical Center, New York, New York, United States
🇫🇷
APHM Hôpital de la Conception, Marseille, France
🇺🇸
Memorial Sloan Kettering Cancer Center, New York, New York, United States

and more 27 locations

A Study to Assess the Safety and Efficacy of Levoketoconazole in the Treatment of Endogenous Cushing's Syndrome.

Phase 3

Completed

Conditions: Endogenous Cushing's Syndrome

Interventions: Drug: Placebo
Drug: Levoketoconazole

First Posted Date: 2017-09-11

Last Posted Date: 2022-11-08

Lead Sponsor: Cortendo AB

Target Recruit Count: 84

Registration Number: NCT03277690

Locations: 🇺🇸
University of Michigan, Comprehensive Endocrine Research, Internal Medicine - MEND, Ann Arbor, Michigan, United States
🇵🇱
Wojskowy Instytut Medyczny, Klinika Gastroenterologii, Endokrynologii I Chorob Wewnetrznych, Warsaw, Poland
🇬🇷
Evangelismos Athens General Hospital, Department of Endocrinology, Athens, Greece

and more 42 locations

Treatment for Endogenous Cushing's Syndrome

Phase 3

Completed

Conditions: Endogenous Cushing's Syndrome

Interventions: Drug: Levoketoconazole

First Posted Date: 2013-04-24

Last Posted Date: 2021-04-19

Lead Sponsor: Cortendo AB

Target Recruit Count: 94

Registration Number: NCT01838551

Locations: 🇵🇱
Szpital Kliniczny im. Heliodora Swiecickiego, Poznań, Poland
🇺🇸
UCLA School of Medicine, Los Angeles, California, United States
🇺🇸
University of New Mexico HSC, Albuquerque, New Mexico, United States

and more 39 locations

Open Label Safety & Pharmacodynamic Study 24Wk w/DIO-902 Combo w/Metformin & Atorvastatin in T2DM Patients

Phase 2

Terminated

Conditions: Type 2 Diabetes

Interventions: Drug: DIO-902

First Posted Date: 2008-02-22

Last Posted Date: 2008-05-28

Lead Sponsor: DiObex

Target Recruit Count: 150

Registration Number: NCT00622089

Locations: 🇺🇸
Diabetes Glandular Disease Research Associates, San Antonio, Texas, United States
🇦🇺
ECRU, Box Hill, Melbourne, Victoria, Australia
🇦🇺
Endocrinology Department, St Leonards, Australia

and more 21 locations

A Phase 2b Study of DIO-902 or DIO-902 Placebo in Addition to Metformin and Atorvastatin or Atorvastatin Placebo for Type 2 Diabetes

Phase 2

Terminated

Conditions: Type 2 Diabetes

Interventions: Drug: DIO-902 placebo
Drug: DIO-902

First Posted Date: 2007-07-02

Last Posted Date: 2008-11-13

Lead Sponsor: DiObex

Target Recruit Count: 200

Registration Number: NCT00494663

Locations: 🇺🇸
Research Solutions, Jonesboro, Arkansas, United States
🇦🇺
Keough Institute, Nedands, Western Australia, Australia
🇺🇸
Covance Clinical Research Unit - Dr. Andrew Ahmann, Portland, Oregon, United States

and more 21 locations

Drug Development Updates

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