LCI699 was efficacious and well tolerated in patients with Cushing's disease enrolled in this proof-of-concept study.

This paper describes the studies of the in vitro biotransformation of two selective androgen receptor modulators (SARMs), namely, RAD140 and S‐23, and the in vivo metabolism of RAD140 in horses using ultra‐high performance liquid chromatography–high resolution mass spectrometry. in vitro metabolic studies of RAD140 and S‐23 were performed using homogenised horse liver. The more prominent in vitro biotransformation pathways for RAD140 included hydrolysis, hydroxylation, glucuronidation and sulfation. Metabolic pathways for S‐23 were similar to those for other arylpropionamide‐based SARMs. The administration study of RAD140 was carried out using three retired thoroughbred geldings. RAD140 and the majority of the identified in vitro metabolites were detected in post‐administration urine samples. For controlling the misuse of RAD140 in horses, RAD140 and its metabolite in sulfate form gave the longest detection time in hydrolysed urine and could be detected for up to 6 days post‐administration. In plasma, RAD140 itself gave the longest detection time of up to 13 days. Apart from RAD140 glucuronide, the metabolites of RAD140 described herein have never been reported before.

Clinicians frequently overlook key radiological features related to POD. Alerting clinicians to relevant radiological features improved the sensitivity and specificity of diagnosis.

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Background: Administration of bisphosphonates, including tiludronic acid, to Thoroughbred racehorses below 3 and a half years of age is prohibited in most racing jurisdictions.Objectives: To determine if evidence of administration of tiludronic acid could be obtained from analysis of blood and urine samples beyond 40 days after administration. Study design: Retrospective cohort.Methods: Horses maintained in a highly controlled environment and treated with Tildren ®a were selected from clinical records. Twenty-four horses were identified, 21 of which were still in race training. Blood and urine samples were collected and analysed for the presence of tiludronic acid using ultra-high-performance liquid chromatography-high-resolution mass spectrometry.Results: Tiludronic acid was detected in samples from every horse, including two that had been given a therapeutic dose of the drug 3 years prior to sample collection.The estimated concentrations of tiludronic acid in the blood collected at least 2 years post-administration were consistently very low (less than 0.3 ng/mL). The estimated concentrations in urine were less consistent and were generally lower than those in blood, although higher levels were inconsistently detected in individual horses (up to about 16 ng/mL almost 1 year post-administration in 1 horse and about 3.7 ng/mL at almost 3 years post-administration in another). Main limitations:The study was performed in horses that are older than the primary target group. A single sample was obtained from most horses and so we cannot comment on elimination profiles. Conclusions:Evidence that a therapeutic dose of tiludronic acid has been administered to a horse can be obtained from detection of the drug in blood and urine samples over 3 years after it was administered.