Contribution of SPECT measurements of D2 and 5-HT2A occupancy to the clinical development of the antipsychotic SB-773812

Journal of Nuclear Medicine

Volumn 52, Issue 4, 2011, Pages 526-534

  Catafau, Ana M ^a   Bullich, Santiago ^b   Nucci, Gianluca ^c,d   Burgess, Clare ^e   Gray, Frank ^e   Merlo Pich, Emilio ^c  

^a GLAXOSMITHKLINE   (Spain)

^b Barcelona Biomedical Research Park   (Spain)

^c GSK   (Italy)

^d PFIZER INC   (United States)

^e GLAXOSMITHKLINE   (United Kingdom)

Author keywords

Antipsychotic; Receptor occupancy; SB 773812; Schizophrenia; Single photon emission computed tomography

Indexed keywords

4 AMINO N [1 [3(4 FLUOROPHENOXY)PROPYL]4 METHYL 4 PIPERIDINYL] 5 IODO 2 METHOXYBENZAMIDE I 123; DOPAMINE RECEPTOR; IODOBENZAMIDE I 123; R 91150; RADIOPHARMACEUTICAL AGENT; RISPERIDONE; SB 773812; SEROTONIN 2A RECEPTOR; UNCLASSIFIED DRUG;

ADULT; ARTICLE; CLINICAL ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG DOSE REGIMEN; DRUG PENETRATION; DRUG RECEPTOR BINDING; DRUG TARGETING; HUMAN; MALE; MONOTHERAPY; PHASE 2 CLINICAL TRIAL (TOPIC); PRIORITY JOURNAL; RADIATION EXPOSURE; RECEPTOR OCCUPANCY; SCHIZOPHRENIA; SINGLE DRUG DOSE; SINGLE PHOTON EMISSION COMPUTER TOMOGRAPHY; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADULT; ALGORITHMS; ANTIPSYCHOTIC AGENTS; BRAIN; COHORT STUDIES; DIAGNOSTIC AND STATISTICAL MANUAL OF MENTAL DISORDERS; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; IMAGE PROCESSING, COMPUTER-ASSISTED; IODOBENZENES; MALE; PIPERIDINES; RADIOPHARMACEUTICALS; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTORS, DOPAMINE D2; RISPERIDONE; SCHIZOPHRENIA; TOMOGRAPHY, EMISSION-COMPUTED, SINGLE-PHOTON; YOUNG ADULT;

EID: 79954617020     PISSN: 01615505     EISSN: None     Source Type: Journal    
DOI: 10.2967/jnumed.110.081885     Document Type: Article

References (33)

1. Gray JA, Roth BL. The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007;12:904-922. (Pubitemid 47482704)
2. Josephs D, Spicer J, O'Doherty M. Molecular imaging in clinical trials. Target Oncol. 2009;4:151-168.
3. Catafau AM, Merlo-Pich E, Bye A. Functional brain imaging in drug development. In: Nuclear Medicine in Psychiatry. Otte A, Audenert K, Peremans K, Dierckx R, Heeringen K, eds. Heidelberg, Germany: Springer Verlag; 2004:95-107.
4. Catafau AM, Danus M, Bullich S, et al. Characterization of the SPECT 5-HT2A receptor ligand 123I-R91150 in healthy volunteers: Part 1-pseudoequilibrium interval and quantification methods. J Nucl Med. 2006;47: 919-928. (Pubitemid 46939943)
5. Catafau AM, Danus M, Bullich S, et al. Characterization of the SPECT 5-HT2A receptor ligand 123I-R91150 in healthy volunteers: Part 2-ketanserin displacement. J Nucl Med. 2006;47:929-937. (Pubitemid 46939944)
6. Catafau AM, Bullich S, Danüs M, et al. Test-retest variability and reliability of 123I-IBZM SPECT measurement of striatal dopamine D2 receptor availability in healthy volunteers and influence of iterative reconstruction algorithms. Synapse. 2008;62:62-69. (Pubitemid 350156144)
7. Catafau AM, Penengo MM, Nucci G, et al. Pharmacokinetics and time-course of D2 receptor occupancy induced by atypical antipsychotics in stabilized schizophrenic patients. J Psychopharmacol. 2008;22:882-894.
8. American Psychiatric Association. Diagnostic and Statistical Manual of Mental Disorders: DSM-IV. 4th ed. Washington, DC: American Psychiatric Association; 1994
9. International Commission on Radiological Protection. Radiological Protection in Biomedical Research. ICRP Publication 62. Oxford, U.K.: Pergamon; 1993.
10. Catafau AM, Suarez M, Bullich S, et al.Within-subject comparison of striatal D2 receptor occupancy measurements using [123I]IBZM SPECT and [11C]raclopride PET. Neuroimage. 2009;46:447-458.
11. Bullich S, Ros D, Pavía J, Cot A, López N, Catafau AM. Neurotransmission SPECT and MR registration combining mutual and gradient information. Med Phys. 2009;36:4903-4910.
12. Nyberg S, Eriksson B, Oxenstierna G, Halldin C, Farde L. Suggested minimal effective dose of risperidone based on PET-measured D2 and 5-HT2A receptor occupancy in schizophrenic patients. Am J Psychiatry. 1999;156: 869-875. (Pubitemid 29260341)
13. Nyberg S, Nordström A-L, Halldin C, Farde L. Positron emission tomography studies on D2 dopamine receptor occupancy and plasma antipsychotic drug levels in man. Int Clin Psychopharmacol. 1995;10(suppl 3):81-85. (Pubitemid 26056453)
14. Kapur S, Zipursky RB, Remington G, et al. 5-HT2 and D2 receptor occupancy of olanzapine in schizophrenia: A PET investigation. Am J Psychiatry. 1998;155: 921-928. (Pubitemid 28307604)
15. Kapur S, Zipursky RB, Remington G. Clinical and theoretical implications of 5-HT2 and D2 receptor occupancy of clozapine, risperidone, and olanzapine in schizophrenia. Am J Psychiatry. 1999;156:286-293. (Pubitemid 29077120)
16. Kapur S, Zipursky R, Jones C, Shammi CS, Remington G, Seeman P. A positron emission tomography study of quetiapine in schizophrenia: A preliminary finding of an antipsychotic effect with only transiently high dopamine D2 receptor occupancy. Arch Gen Psychiatry. 2000;57:553-559. (Pubitemid 30349435)
17. Remington G, Kapur S, Zipursky R. The relationship between risperidone plasma levels and dopamine D2 occupancy: A positron emission tomographic study. J Clin Psychopharmacol. 1998;18:82-83. (Pubitemid 28045640)
18. Knable MB, Heinz A, Raedler T, Weinberger DR. Extrapyramidal side effects with risperidone and haloperidol at comparable D2 receptor occupancy levels. Psychiatry Res. 1997;75:91-101. (Pubitemid 27435975)
19. Lavalaye J, Linszen DH, Booij J, Reneman L, Gersons BP, van Royen EA. Dopamine D2 receptor occupancy by olanzapine or risperidone in young patients with schizophrenia. Psychiatry Res. 1999;92:33-44. (Pubitemid 29512391)
20. Schmitt GJ, Meisenzahl EM, Dresel S, et al. Striatal dopamine D2 receptor binding of risperidone in schizophrenic patients as assessed by 123I-iodobenzamide SPECT: A comparative study with olanzapine. J Psychopharmacol. 2002; 16:200-206. (Pubitemid 34983073)
21. Tauscher J, Kufferle B, Asenbaum S, et al. In vivo 123I-IBZM SPECT imaging of striatal dopamine-2 receptor occupancy in schizophrenic patients treated with olanzapine in comparison to clozapine and haloperidol. Psychopharmacology (Berl). 1999;141:175-181. (Pubitemid 29200169)
22. Meisenzahl EM, Dresel S, Frodl T, et al. D2 receptor occupancy under recommended and high doses of olanzapine: An iodine-123-iodobenzamide SPECT study. J Psychopharmacol. 2000;14:364-370. (Pubitemid 32059781)
23. Scherer J, Tatsch K, Schwarz J, Oertel W, Kirsch MC, Albus M. Striatal D2- dopamine receptor occupancy during treatment with typical and atypical neuroleptics. Biol Psychiatry. 1994;36:627-629.
24. Jones C, Kapur S, Remington G, Zipursky RB. Transient D2 dopamine receptor occupancy in low EPS incidence drugs: PET evidence [abstract]. Biol Psychiatry. 2000;47(suppl 1):S112.
25. Gefvert O, Bergstrom M, Langstrom B, Lundberg T, Lindstrom L, Yates R. Time course of central nervous dopamine-D2 and 5-HT2 receptor blockade and plasma drug concentrations after discontinuation of quetiapine (Seroquel) in patients with schizophrenia. Psychopharmacology (Berl). 1998; 135:119-126. (Pubitemid 28055494)
26. Gefvert O, Lundberg T, Wieselgren IM, et al. D2 and 5HT2A receptor occupancy of different doses of quetiapine in schizophrenia: A PET study. Eur Neuropsychopharmacol. 2001;11:105-110. (Pubitemid 32335553)
27. Kapur S, Remington G. Dopamine D2 receptors and their role in atypical antipsychotic action: Still necessary and may even be sufficient. Biol Psychiatry. 2001;50:873-883. (Pubitemid 34020700)
28. Bullich S, Cot A, Gallego J, et al. Impact of scatter correction on receptor occupancy measurements using 123I-IBZM SPECT: Comparison to 11C-raclopride PET. Neuroimage. 2010;50:1511-1518.
29. Frankle WG, Gil R, Hackett E, et al. Occupancy of dopamine D2 receptors by the atypical antipsychotic drugs risperidone and olanzapine: Theoretical implications. Psychopharmacology (Berl). 2004;175:473-480. (Pubitemid 39362046)
30. Laruelle M. Imaging dopamine transmission in schizophrenia: A review and metaanalysis. Q J Nucl Med. 1998;42:211-221. (Pubitemid 28529874)
31. 18F] Setoperone in neuroleptic naive patients and normal subjects. Am J Psychiatry. 1999;156:72-79.
32. Rinne JO, Hietala J, Ruotsalainen U, et al. Decrease in human striatal dopamine D2 receptor density with age: A PET study with [11C]raclopride. J Cereb Blood Flow Metab. 1993;13:310-314. (Pubitemid 23067467)
33. Huang ML, Van Peer A, Woestenborghs R, et al. Pharmacokinetics of the novel antipsychotic agent risperidone and the prolactin response in healthy subjects. Clin Pharmacol Ther. 1993;54:257-268. (Pubitemid 23294526)