Fingolimod (FTY720): discovery and development of an oral drug to treat multiple sclerosis

…, A Billich, T Baumruker, P Heining… - Nature reviews Drug …, 2010 - nature.com
The discovery of fingolimod (FTY720/Gilenya; Novartis), an orally active immunomodulatory
drug, has opened up new approaches to the treatment of multiple sclerosis, the most …

Discovery of BAF312 (Siponimod), a potent and selective S1P receptor modulator

…, K Hinterding, A Gardin, P End, P Heining… - ACS medicinal …, 2013 - ACS Publications
A novel series of alkoxyimino derivatives as S1P 1 agonists were discovered through de
novo design using FTY720 as the chemical starting point. Extensive structure–activity …

Pregnancy outcomes in the clinical development program of fingolimod in multiple sclerosis

G Karlsson, G Francis, G Koren, P Heining, X Zhang… - Neurology, 2014 - AAN Enterprises
Objective: To report outcomes of pregnancies that occurred during the fingolimod clinical
development program. Methods: Pregnancy outcomes from phase II, phase III, and phase IV …

Physiologically based pharmacokinetic modeling of FTY720 (2-amino-2 [2-(-4-octylphenyl) ethyl] propane-1, 3-diol hydrochloride) in rats after oral and intravenous …

…, H Li, S Mis, N Pyszczynski, P Heining… - Drug Metabolism and …, 2006 - ASPET
FTY720 (2-amino-2[2-(-4-octylphenyl)ethyl]propane-1,3-diol hydrochloride) is a new
sphingosine-1-phosphate receptor agonist being developed for multiple sclerosis and prevention of …

Cardiac troponins and creatine kinase content of striated muscle in common laboratory animals

S Fredericks, GK Merton, MJ Lerena, P Heining… - Clinica Chimica …, 2001 - Elsevier
Animal models are important for the investigation of human heart pathology, novel treatments,
and medical or surgical interventions for disease. Serum markers of myocardial damage …

The use of minipigs for preclinical safety assessment by the pharmaceutical industry: results of an IQ DruSafe minipig survey

…, A Chester, DO Clarke, P Heining… - Toxicologic …, 2016 - journals.sagepub.com
The use of minipigs in preclinical safety testing of pharmaceuticals is considered an alternative
to the more traditional dog and nonhuman primate (NHP) nonrodent species. Substantial …

The use of minipig in drug discovery and development: pros and cons of minipig selection and strategies to use as a preferred nonrodent species

P Heining, T Ruysschaert - Toxicologic pathology, 2016 - journals.sagepub.com
The pig was introduced more than 20 years ago in drug development following attempts of
finding a species that shares better homology with human than the dog, based on …

Comparison of clinical pathology parameters with two different blood sampling techniques in rats: retrobulbar plexus versus sublingual vein

A Mahl, P Heining, P Ulrich, J Jakubowski… - Laboratory …, 2000 - journals.sagepub.com
Blood samples were taken from the retrobulbar venous plexus or the sublingual vein of
male HanIbm:Wist rats to compare clinical pathology parameters between the two sampling …

Pharmacokinetics and cell trafficking dynamics of 2-amino-2-[2-(4-octylphenyl) ethyl] propane-1, 3-diol hydrochloride (FTY720) in cynomolgus monkeys after single …

…, GML Meno-Tetang, K Chiba, N Arima, P Heining… - … of Pharmacology and …, 2002 - ASPET
The pharmacokinetics and cell trafficking dynamics of 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol
hydrochloride (FTY720), a novel immunosuppressive agent, were examined in …

Vehicle systems and excipients used in minipig drug development studies

…, T Kissner, C Stark, S Milano, P Heining… - Toxicologic …, 2016 - journals.sagepub.com
Minipigs have been used for dermal drug development studies for decades, and they are
currently more frequently considered as the second nonrodent species for pivotal nonclinical …