HANS ROLLEMA Neuropharmacology
EDUCATION · PhD - Medicinal Chemistry, PharmD
EXPERIENCE · 2012-2014 Systamedic - Director Neuropharmacology; 1992-2010 Pfizer - Neuroscience. Involved in the discovery and development of varenicline (Chantix)
EXPERTISE · Microdialysis, Bioanalysis, CNS Pharmacology, Nicotinic Acetylcholine Receptor. Over 90 scientific publications.
BIO
Hans Rollema studied Pharmacy in The Netherlands and received his PhD in Pharmaceutical Chemistry at the University of Groningen, The Netherlands in 1976, where he became an associate professor and conducted research on the mechanisms of action of anti-Parkinson drugs and antipsychotics. He was part of the Groningen group that pioneered the use of in vivo microdialysis for drug research.
In 1992 he was recruited by Pfizer to run a microdialysis lab in the Neuroscience research laboratories in Groton, CT, supporting various Neuroscience discovery projects with data on the effects of novel and reference compounds on neurotransmitter release. He was a member of the nicotinic partial agonist project team (1993-1998) that discovered varenicline (Chantix, Champix) and later became the point of contact for the preclinical pharmacology of varenicline. Since 2005 he has been working with several NY Chantix teams on the submission and safety and regulatory aspects of this smoking cessation aid. After retiring from Pfizer in December 2010, he started a biomedical consulting business and has been consulting for Pfizer and biotechs on the preclinical pharmacology of varenicline and on nAChR ligands for different indications.
In 2012 he joined SystaMedic and in 2014 BioPharmaWorks LLC (Groton, CT) as director of Neuropharmacology. Hans Rollema has published about 100 scientific papers in peer-reviewed journals and given several presentations at international meetings.
CV
Training (University of Groningen, The Netherlands)
1976 Ph.D. Thesis: Medicinal chemistry of phenothiazine antipsychotics
1963-1970 Study Pharmacy (specialization: CNS Medicinal Chemistry, Bioanalysis)
Academic positions (Groningen, The Netherlands; UCSF, USA)
1985-1992 Associate Professor in Medicinal and Pharmaceutical Analytical Chemistry
1987-1988 Visiting Professor at U. California, San Francisco (with Dr. Neal Castagnoli)
1977-1992 Tenured Faculty at University of Groningen, The Netherlands
1970 Lecturer at the Department of Pharmaceutical and Analytical Chemistry
Teaching and research
· Design of novel aminotetralin dopamine agonists as anti-Parkinson agents
· Mechanism of action of antipsychotic drugs
· Mechanism of action of the Parkinsonian neurotoxin MPTP
· In situ bioanalysis of drugs and metabolites
· Microdialysis of neurotransmitters
Pfizer (Groton, USA)
1998 – 2010 Research Fellow
1992 – 1998 Principal Research Investigator
· Head microdialysis lab in Neuroscience: guide and support CNS projects and full development
compounds with in vivo transmitter release data
· Member of varenicline discovery and development teams, preclinical point of contact
Rollema Biomedical Consulting (Mystic, USA)
2011 - present Independent Consultant (sole proprietorship)
· Drug discovery and development
· Microdialysis
· Neuropharmacology
· Nicotinic Acetylcholine Receptors, Nicotine Dependence, Smoking Cessation
BioPharmaWorks LLC (Groton, USA)
2014 - present Consultancy Services, Director Neuropharmacology
Selected peer-reviewed publications (since 2010)
Rollema H, Hurst RS (2018) The contribution of agonist and antagonist activities of α4β2 nAChR ligands to smoking cessation efficacy: a quantitative analysis of literature data. Psychopharmacology 235 (9): 2479–2505
Els C, Rollema H, Chue P (2017) Neuropsychiatric Issues and Pharmacotherapy for smoking cessation in: ‘Disease Interrupted: Tobacco Reduction and Cessation’ 2nd Ed, Chapter 16, p. 251-267. Els C, Kunyk D, Selby P (eds) Center for Addiction and Mental Health, Toronto, Canada
Rollema H (2017) Nicotine in: Disease Interrupted: Tobacco Reduction and Cessation’ 2nd Ed. Chapter 5, p.73-92. Els C, Kunyk D, Selby P (eds) Center for Addiction and Mental Health, Toronto, Canada
Cremers TIFH, Flik G, Folgering JHA, Rollema H, Stratford Jr RE (2016) Development of a rat plasma and brain extracellular fluid pharmacokinetic model for bupropion and hydroxybupropion based on microdialysis sampling, and application to predict human brain concentrations. Drug Metab Dispos 44:624–633
Zaveri N, Rollema H, Swan GE (2015) Nicotine Dependence in: 'The Tobacco Epidemic', Loddenkemper R, Kreuter M (eds) Prog Respir Res. Basel, Karger, 2015, Vol 42:47–57.
Rollema H, Hurst RS, Bertrand D (2014) Nicotinic Agonists and Antagonists. In: Encyclopedia of Psychopharmacology, Eds. I.P. Stolerman & L.H. Price, Springer-Verlag Berlin, Heidelberg. DOI 10.1007/978-3-642-27772-6_304-2 # Springer-Verlag Berlin Heidelberg 2014
Rollema H, Russ C, Lee TC, Hurst RS, Daniel Bertrand D (2014) Functional Interactions of Varenicline and Nicotine With nAChR Subtypes Implicated in Cardiovascular Control. Nic. Tob. Res. 16, (6): 733–742
Kim SY, Choi HS, Rollema H, Schwam EM, McRae T, Dubrava S, Jacobsen J (2014) Phase II Crossover Trial of Varenicline in Mild-to-Moderate Alzheimer’s Disease. Dement Geriatr Cogn Disord 37:232–245
Weber ML, Hofland CM, Shaffer CL, Flik G, Cremers T, Hurst RS, Rollema H (2013) Therapeutic doses of antidepressants are projected not to inhibit human α4β2 nicotinic acetylcholine receptors. Neuropharmacol 72:88-95
Rollema H (2012) Nicotine in: Disease Interrupted: Tobacco Reduction and Cessation, chapter 4. Eds. Els C, Kunyk D, Selby P, Charleston, SC: CreateSpace, 2012
Fossa AA, Wisialowski TA, Cremers T, Vander Hart M, Tseng E, Deng S, Rollema H, Wang EQ (2012) Improved preclinical cardiovascular therapeutic indices with long-term inhibition of norepinephrine reuptake using reboxetine, Toxicol. Appl. Pharmacol http://dx.doi.org/10.1016/j.taap.2012.09.010
Hurst RS, Rollema H, Bertrand D (2012) Nicotinic acetylcholine receptors: from basic science to therapeutics. Pharmacol & Therap 137 (2013) 22–54. DOI:10.1016/j.pharmthera.2012.08.012
Aubin HJ, Hans Rollema H, Svensson TH, Winterer G (2011) Smoking, Quitting, and Psychiatric Disease: A Review. Neurosci Biobehav Rev, 36(1):271-84
Rollema H, Wilson GG, Lee TC, Folgering JHA, Flik G (2011) Effect of co-administration of varenicline and antidepressants on extracellular monoamine concentrations in rat prefrontal cortex. Neurochem Int 58: 78–84.
Mineur YS, Einstein EB, Seymour PA, Coe JW, O'Neill BT, Rollema H, Picciotto MR (2011) a4b2 Nicotinic acetylcholine receptor partial agonists with low intrinsic efficacy have antidepressant-like properties. Behav Pharm doi:10.1097/FBP.0b013e328347546d
Wager T, Pettersen BA, Schmidt AW, Spracklin DK, Mente S, Butler TW, Howard H, Lettiere DJ, Rubitski DM, Wong DF, Nedza FM, Nelson FR, Rollema H, Raggon JW, Aubrecht J, Freeman JK et al (2011) Discovery of Two Clinical Histamine H-3 Receptor Antagonists: trans-N-Ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)-phenyl]cyclobu tanecarboxamide (PF-03654746) and trans-3-Fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylp ropyl)cyclobutanecarboxamide (PF-03654764). J Med Chem 54(21):7602-20
Kleijn J, Folgering JH, van der Hart MC, Rollema H, Cremers TI, Westerink BH (2011) Direct effect of nicotine on mesolimbic dopamine release in rat nucleus accumbens shell. Neurosci Lett. 493:55-8.
Chatterjee S, Steensland P, Simms JA, Holgate J, Coe JW, Hurst RS, Shaffer CL, Low J, Rollema H, Bartlett SE (2011) Partial agonists of the 34* neuronal nicotinic acetylcholine receptor reduce ethanol consumption and seeking in rats. Neuropsychopharmacology. 36(3):603-15
Wager T, Pettersen B, Schmidt AW (….), Rollema H et al (2011) Discovery of Two Clinical Histamine H-3 Receptor Antagonists: trans-N-Ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)-phenyl]cyclobu tanecarboxamide (PF-03654746) and trans-3-Fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylp ropyl)cyclobutanecarboxamide (PF-03654764). J Med Chem 54(21):7602-20
Rollema H, Faessel HM (2010) Pharmacodynamic and pharmacokinetic profile of the α4β2 nicotinic acetylcholine receptor partial agonist varenicline, a smoking cessation aid. J Pediat Biochem 1:1751- 1784
Faessel HM, Obach RS, Rollema H, Ravva P, Burstein AH (2010) A review of the clinical pharmacokinetics and pharmacodynamics of varenicline for smoking cessation. Clin Pharmacokinet 49: 799-816
Rollema H, Bertrand D, Hurst RS (2010) Nicotinic receptor agonists and antagonists (2010) In: Encyclopedia of Psychopharmacology, Ed. I.P. Stolerman, Springer-Verlag Berlin, Heidelberg. 887-899.
Rollema H. Shrikhande A, Ward K, Tingley D, Coe JW, Bertrand D et al (2010) Preclinical properties of varenicline, cytisine and dianicline, a4b2 nAChR partial agonists for nicotine dependence, translate to clinical efficacy. An in vitro and in vivo study. Brit J Pharmacology, 160: 334-345.
Tonstad S, Rollema H. (2010) Varenicline in Smoking Cessation. Expert Rev of Resp Med: Drug Profile. Expert Review of Respiratory Medicine 4: 291-299.
Reperant C, Pons S, Dufour E, Rollema H, Gardier A, Maskos U (2010) Effect of the α4β2* nicotinic acetylcholine receptor partial agonist varenicline on dopamine release in β2-/- mice with selective re-expression of the β2 subunit in the ventral tegmental area. Neuropharmacology 58:346-50.
Rollema H, Faessel HM, Williams KE (2010) Varenicline overdose in a teenager – a clinical pharmacology perspective. Clin. Toxicology 47: 605–606.
Rollema H, Faessel HM (2010), Pharmacodynamic and pharmacokinetic profiles of the 42 nicotinic acetylcholine receptor partial agonist varenicline, a smoking cessation aid. J. Ped. Biochem 1:175–184
Rollema H, Guanowsky V, Mineur YS, Shrikhande A, Coe JW, Seymour PA, Picciotto MR (2010) Varenicline has antidepressant-like activity in the forced swim test and augments sertraline’s effect. Eur J Pharmacol 605:114-116.
O’Connor E, Parker J, Rollema H, Mead A (2010) The α4β2 nicotinic acetylcholine-receptor partial agonist varenicline inhibits both nicotine self-administration following repeated dosing and reinstatement of nicotine seeking in rats. Psychopharmacology, 208: 365-376