Polymorphic CYP2B6: molecular mechanisms and emerging clinical significance

UM Zanger, K Klein, T Saussele, J Blievernicht… - 2007 - Future Medicine
Polymorphisms in drug-metabolizing enzymes and drug transporters contribute to wide and
inheritable variability in drug pharmacokinetics, response and toxicity. One of the less well-…

Genetic variability of CYP2B6 in populations of African and Asian origin: allele frequencies, novel functional variants, and possible implications for anti-HIV therapy …

K Klein, T Lang, T Saussele… - Pharmacogenetics …, 2005 - journals.lww.com
The present study investigated CYP2B6 genetic variability by sequencing genomic DNA
samples of African-American, Ghanaian, Taiwanese, Japanese and Korean subjects …

Aberrant splicing caused by single nucleotide polymorphism c. 516G> T [Q172H], a marker of CYP2B6* 6, is responsible for decreased expression and activity of …

…, JK Blievernicht, K Klein, T Saussele… - Journal of pharmacology …, 2008 - ASPET
CYP2B6 is a polymorphic human drug metabolizing cytochrome P450 with clinical relevance
for several drug substrates including cyclophosphamide, bupropion, and efavirenz. The …

Impact of CYP2B6 polymorphism on hepatic efavirenz metabolism in vitro

Z Desta, T Saussele, B Ward, J Blievernicht, L Li… - 2007 - Future Medicine
Objectives: To determine the influence of cytochrome P450 2B6 (CYP2B6) genotype on the
rate of oxidative efavirenz metabolism in human liver microsomes. Materials & methods: …

Impaired expression of CYP2D6 in intermediate metabolizers carrying the* 41 allele caused by the intronic SNP 2988G> A: evidence for modulation of splicing events

…, J Blievernicht, E Schaeffeler, T Saussele… - Pharmacogenetics …, 2006 - journals.lww.com
We investigated the molecular basis for low expression and activity of CYP2D6 associated
with the CYP2D6* 41 allele in about 10–15% of Caucasians with intermediate metabolizer …

Recombinant Production of Human Microsomal Cytochrome P450 2D6 in the Methylotrophic Yeast Pichia pastoris

…, L Grundmann, K Kurr, L Valinotto, T Saussele… - …, 2005 - Wiley Online Library
Microsomal cytochrome P450 monooxygenases of groups 1–3 are mainly expressed in the
liver and play a crucial role in phase 1 reactions of xenobiotic metabolism. The cDNAs …

A natural variant of the heme-binding signature (R441C) resulting in complete loss of function of CYP2D6

K Klein, S Tatzel, S Raimundo, T Saussele… - Drug metabolism and …, 2007 - ASPET
A new variant allele CYP2D6*62 (g.4044C>T; R441C) of the drug-metabolizing cytochrome
P450 (P450) CYP2D6 was identified in a person with reduced sparteine oxidation …

Lacosamide. A new antiepileptic drug as adjunctive therapy in patients with partial-onset seizures

T Saussele - Medizinische Monatsschrift fur Pharmazeuten, 2008 - europepmc.org
Lacosamide (Vimpat) is an aniepileptic drug with a new, dual mode of action. Lacosamide
enhances slow inactivation of voltage-gated sodium channels and modulates the collapsin …

Supplementation with folic acid before and during pregnancy

T Saussele - Medizinische Monatsschrift fur Pharmazeuten, 2008 - europepmc.org
Since 1995, supplementation of folic acid (400 microg/d) for prevention of neural tube defects
is recommended for women during or before pregnancy by the German Society of Nutrition…

PCSK9 inhibitors. A new approach for treatment of hypercholesterolemia

T Saußele - Medizinische Monatsschrift fur Pharmazeuten, 2015 - europepmc.org
To date HMG-CoA-reductase inhibitors are the most effective drugs for reduction of LDL-cholesterol
levels and for prevention of cardiovascular events. Inhibition of the enzyme PCSK9 (…