Searchable abstracts of presentations at key conferences in endocrinology

ea0037ep804 | Pituitary: clinical | ECE2015

Pharmacokinetic and pharmacodynamic analyses of pasireotide LAR from a randomised, phase III study in patients with inadequately controlled acromegaly

Shen Guoxiang , Darstein Christelle , Resendiz Karina Hermosillo , Hu Ke

Introduction: A 24-week, PhIII, randomised study (PAOLA) demonstrated superior efficacy of pasireotide long-acting release (PAS-LAR; 40 and 60 mg) vs continued treatment with octreotide LAR 30 mg or lanreotide Autogel 120 mg (15.4%, 20.0% vs 0%) at providing biochemical control (GH<2.5 μg/l and normalized IGF-1) in patients with acromegaly inadequately controlled on first-generation somatostatin analogues. Results from PK/PD analyses of PAS-LAR are reported here.<...

ea0063gp162 | Cushing's | ECE2019

Pharmacokinetics of osilodrostat following single and multiple doses of osilodrostat in healthy subjects and patients with Cushing’s disease

Han Kevin , Tauchmanova Libuse , Atkinson Susan , Darstein Christelle , Zhang Xinrui , Combes Francois Pierre , Pedroncelli Alberto M

Introduction: Osilodrostat is a potent oral 11β-hydroxylase inhibitor currently in Phase III clinical development for the treatment of Cushing’s syndrome (CS). The key pharmacokinetic (PK) properties, drug–drug interactions (DDIs), and population PK findings for osilodrostat in humans are summarized.Methods: Osilodrostat PK has been characterized in nine Phase I studies (healthy subjects and subjects with hepatic or renal impairment), two ...

ea0037gp.22.05 | Pituitary–Therapy of Cushing's disease | ECE2015

Effects of osilodrostat (LCI699) on cytochrome P450 enzymes in healthy volunteers indicates a low drug–drug interaction potential

Ting Lillian , Tripathi Anadya Prakash , Darstein Christelle , White Tracy , Sauter Nicholas

Introduction: In vitro assessments of osilodrostat (LCI699), a potent oral inhibitor of 11β-hydroxylase suggested potential drug–drug interactions (DDIs) with cytochrome P450 (CYP) enzyme metabolism. This clinical study evaluated the effect of osilodrostat on the pharmacokinetics (PK) of CYP1A2, CYP2C19, CYP2D6, and CYP3A4 probe substrates, caffeine, omeprazole, dextromethorphan, and midazolam, respectively.Methods: A single-centre, op...

ea0035p918 | Pituitary Clinical (<emphasis role="italic">Generously supported by IPSEN</emphasis>) | ECE2014

Pharmacokinetic (PK) and pharmacodynamic (PD) analyses of pasireotide LAR and octreotide LAR: Randomized, double-blind Phase III study in patients with medically naive acromegaly

Shen George , Darstein Christelle , Resendiz Karina Hermosillo , Wang Yanfeng , Hu Ke

Introduction: A recent 12-month randomized, double-blind study showed that pasireotide LAR was superior to octreotide LAR at providing biochemical control (GH and IGF1) in medically naïve patients with acromegaly. This analysis evaluates the PK/PD of pasireotide and octreotide in these patients.Methods: Patients received pasireotide LAR 40 mg/28 day (n=176) or octreotide LAR 20 mg/28 day (n=182) for 12 m. The relationship between p...

ea0056p856 | Pituitary - Clinical | ECE2018

A first-in-human pharmacokinetic, safety, and tolerability study of pasireotide subcutaneous depot

Tiberg Fredrik , Glantz Susanne , Strandgarden Kerstin , Darstein Christelle , Eisinger Johannes , Tauchmanova Libuse , Breitschaft Astrid

Background: Pasireotide is available in twice-daily subcutaneous (sc) and long-acting intramuscular (im) formulations. Pasireotide sc depot is an investigational extended-release sc formulation designed for improved handling and administration. Results are reported from a Phase I dose-escalating study.Methods: All subjects received a single dose of pasireotide sc (600 μg) and were randomized 12:2:2 to pasireotide sc depot as a single upper-thigh inj...

ea0049gp177 | Pituitary | ECE2017

Octreotide subcutaneous (s.c.) depot, a novel ready-to-use formulation, provides higher exposure and maintains response in patients with acromegaly and functioning neuroendocrine tumours (NETs) previously treated with long-acting octreotide: Results from a phase 2, open-label, multicentre, randomized study

Ferone Diego , Borson-Chazot Francoise , Cailleux Anne , Horsch Dieter , lahner Harald , Pivonello Rosario , Tauchmanova Libuse , Darstein Christelle , Olsson Hakan , Tiberg Fredrik , Pavel Marianne

Background: Octreotide s.c. depot is a novel, ready-to-use formulation administered via a thin needle, which may allow self-administration. In a phase 1 study in healthy volunteers, octreotide s.c. depot provided greater bioavailability with faster onset and greater IGF1 suppression than long-acting octreotide. Here, we present data from a phase 2 study evaluating pharmacokinetics (PK), efficacy, safety, and tolerability of octreotide s.c. depot in patients with acromegaly and...