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Plerixafor

Plerixafor is a bicyclam with hematopoietic stem cell-mobilizing activity. On December 15, 2008, the US Food and Drug Administration approved  this drug.  Plerixafor blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4, resulting in hematopoietic stem cell (HSC) release from bone marrow and HSC movement into the peripheral circulation. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus). 

Current developer:    AnorMed Inc (acquired by Genzyme) and Genzyme Inc.

Plerixafor (rINN and USAN, also known as MOZOBIL, JM 3100 and AMD3100) is a macrocyclic compound and potential fusion inhibitor. It is an antagonist (or perhaps more accurately a partial agonist) of the alpha-chemokine receptor CXCR4 & an allosteric agonist of CXCR7.

According to http://en.wikipedia.org/wiki/Plerixafor, Plerixafor was initially developed for potential use in the treatment of HIV, for its role in the blocking of CXCR4, a chemokine receptor which acts as a co-receptor for certain strains of HIV (along with the virus's main cellular receptor, CD4). The bicyclam derivative plerixafor hydrochloride (AMD-3100, Mozobil) was originally discovered as a potent and selective anti-HIV agent; however, problems with unexpected cardiac disturbances led AnorMED (now part of Genzyme) to discontinue its development. Plerixafor was seen to decrease metastasis in mice in several studies. Besides, Plerixafor has been shown to decrease recurrence of glioblastoma in a mouse model after radiotherapy. In this model, the cancer surviving radiation are critically depended on bone marrow derived cells for vasculogenesis whose recruitment mediated by SDF-1 CXCR4 interaction is blocked by AMD3100 (Plerixafor).  

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2: Quiroga MP, Burger JA. BCR-Mediated Decrease of CXCR4 and CD62L in CLL - Letter. Cancer Res. 2010 May 25. [Epub ahead of print] PubMed PMID: 20501831.

3: Micallef IN, Ho AD, Klein LM, Marulkar S, Gandhi PJ, McSweeney PA. Plerixafor (Mozobil) for stem cell mobilization in patients with multiple myeloma previously treated with lenalidomide. Bone Marrow Transplant. 2010 May 17. [Epub ahead of print] PubMed PMID: 20479709.

4: Pusic I, Dipersio JF. Update on clinical experience with AMD3100, an SDF-1/CXCL12-CXCR4 inhibitor, in mobilization of hematopoietic stem and progenitor cells. Curr Opin Hematol. 2010 May 13. [Epub ahead of print] PubMed PMID: 20473162.

5: Nimmagadda S, Pullambhatla M, Stone K, Green G, Bhujwalla ZM, Pomper MG. Molecular imaging of CXCR4 receptor expression in human cancer xenografts with [64Cu]AMD3100 positron emission tomography. Cancer Res. 2010 May 15;70(10):3935-44. Epub 2010 May 11. PubMed PMID: 20460522; PubMed Central PMCID: PMC2874192.

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7: Kessans MR, Gatesman ML, Kockler DR. Plerixafor: a peripheral blood stem cell mobilizer. Pharmacotherapy. 2010 May;30(5):485-92. PubMed PMID: 20411999.

8: Jantunen E, Penttilä K, Pyörälä M, Mahlamäki E, Kuittinen T, Nousiainen T. Addition of plerixafor to a chemotherapy plus G-CSF mobilization in hard-to-mobilize patients. Bone Marrow Transplant. 2010 Apr 19. [Epub ahead of print] PubMed PMID: 20400986.

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11: Costa LJ, Alexander ET, Hogan KR, Schaub C, Fouts TV, Stuart RK. Development and validation of a decision-making algorithm to guide the use of plerixafor for autologous hematopoietic stem cell mobilization. Bone Marrow Transplant. 2010 Apr 12. [Epub ahead of print] PubMed PMID: 20383210.

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16: Flatt T, Lewing K, Gonzalez C, Anthony K, Ryan R, Jones R, Gamis A, Dalal J. Successful mobilization with AMD3100 and filgrastim with engraftment of autologous peripheral blood stem cells in a heavily pretreated pediatric patient with recurrent Burkitt lymphoma. Pediatr Hematol Oncol. 2010 Mar;27(2):138-49. PubMed PMID: 20201695.

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24: Flomenberg N, Comenzo RL, Badel K, Calandra G. Plerixafor (Mozobil) alone to mobilize hematopoietic stem cells from multiple myeloma patients for autologous transplantation. Biol Blood Marrow Transplant. 2010 May;16(5):695-700. Epub 2010 Jan 11. PubMed PMID: 20067838.

25: Chang TL, Klepper A, Ding J, Garber J, Rapista A, Mosoian A, Hubner W, Gutierrez J, Walewski J, Abergel J, Schiano T, Branch A. Human peritoneal macrophages from ascitic fluid can be infected by a broad range of HIV-1 isolates. J Acquir Immune Defic Syndr. 2010 Mar 1;53(3):292-302. PubMed PMID: 20065862; PubMed Central PMCID: PMC2840202.

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29: Arms L, Girard BM, Vizzard MA. Expression and function of CXCL12/CXCR4 in rat urinary bladder with cyclophosphamide-induced cystitis. Am J Physiol Renal Physiol. 2010 Mar;298(3):F589-600. Epub 2009 Dec 23. PubMed PMID: 20032115; PubMed Central PMCID: PMC2838600.

30: Choi HY, Yong CS, Yoo BK. Plerixafor for stem cell mobilization in patients with non-Hodgkin's lymphoma and multiple myeloma. Ann Pharmacother. 2010 Jan;44(1):117-26. Epub 2009 Dec 15. Review. PubMed PMID: 20009003.

31: Hick AC, van Eyll JM, Cordi S, Forez C, Passante L, Kohara H, Nagasawa T, Vanderhaeghen P, Courtoy PJ, Rousseau GG, Lemaigre FP, Pierreux CE. Mechanism of primitive duct formation in the pancreas and submandibular glands: a role for SDF-1. BMC Dev Biol. 2009 Dec 14;9:66. PubMed PMID: 20003423; PubMed Central PMCID: PMC2801489.

32: Toledano H, Yahel A, Cohen IJ, Yaniv I, Stein J. Successful mobilization, harvest and transplant of peripheral blood stem cells using AMD3100 and G-CSF following high dose craniospinal irradiation for medulloblastoma in a young child. Pediatr Blood Cancer. 2010 Apr;54(4):613-5. PubMed PMID: 19998469.

33: Rosenbeck LL, Srivastava S, Kiel PJ. Peripheral blood stem cell mobilization tactics. Ann Pharmacother. 2010 Jan;44(1):107-16. Epub 2009 Dec 8. Review. PubMed PMID: 19996324.

34: Fesler MJ, Kudva G, Petruska PJ. Plerixafor and pegylated filgrastim: a case of safe and effective hematopoietic stem cell mobilization. Bone Marrow Transplant. 2009 Dec 7. [Epub ahead of print] PubMed PMID: 19966845.

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37: Blum A, Childs RW, Smith A, Patibandla S, Zalos G, Samsel L, McCoy JP, Calandra G, Csako G, Cannon RO 3rd. Targeted antagonism of CXCR4 mobilizes progenitor cells under investigation for cardiovascular disease. Cytotherapy. 2009;11(8):1016-9. PubMed PMID: 19929465.

38: Fruehauf S, Veldwijk MR, Seeger T, Schubert M, Laufs S, Topaly J, Wuchter P, Dillmann F, Eckstein V, Wenz F, Goldschmidt H, Ho AD, Calandra G. A combination of granulocyte-colony-stimulating factor (G-CSF) and plerixafor mobilizes more primitive peripheral blood progenitor cells than G-CSF alone: results of a European phase II study. Cytotherapy. 2009;11(8):992-1001. PubMed PMID: 19929463.

39: Hansen PB, Gaarsdal E. [Stem cell harvesting after plerixafor treatment]. Ugeskr Laeger. 2009 Nov 16;171(47):3452-3. Danish. PubMed PMID: 19925734.

40: Park HC, Yasuda K, Ratliff B, Stoessel A, Sharkovska Y, Yamamoto I, Jasmin JF, Bachmann S, Lisanti MP, Chander P, Goligorsky MS. Postobstructive regeneration of kidney is derailed when surge in renal stem cells during course of unilateral ureteral obstruction is halted. Am J Physiol Renal Physiol. 2010 Feb;298(2):F357-64. Epub 2009 Nov 11. PubMed PMID: 19906947; PubMed Central PMCID: PMC2822512.

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42: Micallef IN, Stiff PJ, DiPersio JF, Maziarz RT, McCarty JM, Bridger G, Calandra G. Successful stem cell remobilization using plerixafor (mozobil) plus granulocyte colony-stimulating factor in patients with non-hodgkin lymphoma: results from the plerixafor NHL phase 3 study rescue protocol. Biol Blood Marrow Transplant. 2009 Dec;15(12):1578-86. Epub 2009 Oct 4. PubMed PMID: 19896082.

43: Hansen PB, Gaarsdal E. [Mobilisation of haematopoietic stem cells with plerixafor--secondary publication]. Ugeskr Laeger. 2009 Nov 2;171(45):3272-5. Review. Danish. PubMed PMID: 19887056.

44: Cashen AF. Plerixafor hydrochloride: a novel agent for the mobilization of peripheral blood stem cells. Drugs Today (Barc). 2009 Jul;45(7):497-505. Review. PubMed PMID: 19834627.

45: Nimmagadda S, Sweiss K, Mahmud N, Park Y, Rondelli D. Plerixafor given before the third leukapheresis to rescue an unsuccessful stem cell mobilization with CY and G-CSF. Bone Marrow Transplant. 2009 Oct 12. [Epub ahead of print] PubMed PMID: 19820726.

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47: Lee Y, Kim SJ, Park HD, Park EH, Huang SM, Jeon SB, Kim JM, Lim DS, Koh SS. PAUF functions in the metastasis of human pancreatic cancer cells and upregulates CXCR4 expression. Oncogene. 2010 Jan 7;29(1):56-67. Epub 2009 Sep 28. PubMed PMID: 19784070.

48: Sohy D, Yano H, de Nadai P, Urizar E, Guillabert A, Javitch JA, Parmentier M, Springael JY. Hetero-oligomerization of CCR2, CCR5, and CXCR4 and the protean effects of "selective" antagonists. J Biol Chem. 2009 Nov 6;284(45):31270-9. Epub 2009 Sep 15. PubMed PMID: 19758998; PubMed Central PMCID: PMC2781525.

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51: MacFarland R, Hard ML, Scarborough R, Badel K, Calandra G. A pharmacokinetic study of plerixafor in subjects with varying degrees of renal impairment. Biol Blood Marrow Transplant. 2010 Jan;16(1):95-101. Epub 2009 Sep 10. PubMed PMID: 19748593.

52: Fruehauf S, Veldwijk MR, Seeger T, Schubert M, Laufs S, Topaly J, Wuchter P, Dillmann F, Eckstein V, Wenz F, Goldschmidt H, Ho AD, Calandra G. A combination of granulocyte-colony-stimulating factor (G-CSF) and plerixafor AMD3100 (plerixafor) mobilizes more primitive peripheral blood progenitor cells than G-CSF alone: results of a European phase II study. Cytotherapy. 2009 Aug 31:1-10. [Epub ahead of print] PubMed PMID: 19722120.

53: DiPersio JF, Micallef IN, Stiff PJ, Bolwell BJ, Maziarz RT, Jacobsen E, Nademanee A, McCarty J, Bridger G, Calandra G; 3101 Investigators. Phase III prospective randomized double-blind placebo-controlled trial of plerixafor plus granulocyte colony-stimulating factor compared with placebo plus granulocyte colony-stimulating factor for autologous stem-cell mobilization and transplantation for patients with non-Hodgkin's lymphoma. J Clin Oncol. 2009 Oct 1;27(28):4767-73. Epub 2009 Aug 31. PubMed PMID: 19720922.

54: Brule S, Friand V, Sutton A, Baleux F, Gattegno L, Charnaux N. Glycosaminoglycans and syndecan-4 are involved in SDF-1/CXCL12-mediated invasion of human epitheloid carcinoma HeLa cells. Biochim Biophys Acta. 2009 Dec;1790(12):1643-50. Epub 2009 Aug 17. PubMed PMID: 19695308.

55: Blum A, Childs RW, Smith A, Patibandla S, Zalos G, Samsel L, McCoy JP, Calandra G, Csako G, Cannon RO 3rd. Targeted antagonism of CXCR4 mobilizes progenitor cells under investigation for cardiovascular disease. Cytotherapy. 2009 Aug 13:1-4. [Epub ahead of print] PubMed PMID: 19680994.

56: Dillmann F, Veldwijk MR, Laufs S, Sperandio M, Calandra G, Wenz F, Zeller J, Fruehauf S. Plerixafor inhibits chemotaxis toward SDF-1 and CXCR4-mediated stroma contact in a dose-dependent manner resulting in increased susceptibility of BCR-ABL+ cell to Imatinib and Nilotinib. Leuk Lymphoma. 2009 Oct;50(10):1676-86. PubMed PMID: 19657955.

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58: Heuser M, Kuchenbauer F, Argiropoulos B, Sekulovic S, Leung M, Stasiak M, Ganser A, Humphries RK. Priming reloaded? Blood. 2009 Jul 23;114(4):925-6; author reply 926-7. PubMed PMID: 19628718.

59: Greinix HT, Worel N. New agents for mobilizing peripheral blood stem cells. Transfus Apher Sci. 2009 Aug;41(1):67-71. Epub 2009 Jul 16. PubMed PMID: 19615944.

60: Vose JM, Ho AD, Coiffier B, Corradini P, Khouri I, Sureda A, Van Besien K, Dipersio J. Advances in mobilization for the optimization of autologous stem cell transplantation. Leuk Lymphoma. 2009 Sep;50(9):1412-21. PubMed PMID: 19603345.

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67: Tricot G, Cottler-Fox MH, Calandra G. Safety and efficacy assessment of plerixafor in patients with multiple myeloma proven or predicted to be poor mobilizers, including assessment of tumor cell mobilization. Bone Marrow Transplant. 2010 Jan;45(1):63-8. Epub 2009 Jun 22. PubMed PMID: 19543330.

68: Albanese P, Caruelle D, Frescaline G, Delbé J, Petit-Cocault L, Huet E, Charnaux N, Uzan G, Papy-Garcia D, Courty J. Glycosaminoglycan mimetics-induced mobilization of hematopoietic progenitors and stem cells into mouse peripheral blood: structure/function insights. Exp Hematol. 2009 Sep;37(9):1072-83. Epub 2009 Jun 17. PubMed PMID: 19539688.

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76: Kosacka J, Gericke M, Nowicki M, Kacza J, Borlak J, Spanel-Borowski K. Apolipoproteins D and E3 exert neurotrophic and synaptogenic effects in dorsal root ganglion cell cultures. Neuroscience. 2009 Aug 18;162(2):282-91. Epub 2009 May 3. PubMed PMID: 19414061.

77: DiPersio JF, Stadtmauer EA, Nademanee A, Micallef IN, Stiff PJ, Kaufman JL, Maziarz RT, Hosing C, Früehauf S, Horwitz M, Cooper D, Bridger G, Calandra G; 3102 Investigators. Plerixafor and G-CSF versus placebo and G-CSF to mobilize hematopoietic stem cells for autologous stem cell transplantation in patients with multiple myeloma. Blood. 2009 Jun 4;113(23):5720-6. Epub 2009 Apr 10. PubMed PMID: 19363221.

78: Affani R, Pélissier F, Aubertin AM, Dugat D. Bis-14-membered ring diketal diamines: synthesis and evaluation of their anti-HIV and anti-tumoral activities. Eur J Med Chem. 2009 Aug;44(8):3138-46. Epub 2009 Mar 24. PubMed PMID: 19356827.

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80: Juarez JG, Thien M, Dela Pena A, Baraz R, Bradstock KF, Bendall LJ. CXCR4 mediates the homing of B cell progenitor acute lymphoblastic leukaemia cells to the bone marrow via activation of p38MAPK. Br J Haematol. 2009 May;145(4):491-9. Epub 2009 Mar 6. PubMed PMID: 19344405.

81: Abe H, Ina K, Kitamura H, Sumiyoshi H, Tatsukawa S, Yoshioka H, Fujikura Y. Role of the CXCL12/CXCR4 axis in milky spots of rats bearing ascitic-type hepatoma. Anat Sci Int. 2009 Sep;84(3):226-36. Epub 2009 Apr 2. PubMed PMID: 19340530.

82: Burger JA, Stewart DJ. CXCR4 chemokine receptor antagonists: perspectives in SCLC. Expert Opin Investig Drugs. 2009 Apr;18(4):481-90. Review. PubMed PMID: 19335276.

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272: Owen SM, Rudolph D, Schols D, Fujii N, Yamamoto N, Lal RB. Susceptibility of diverse primary HIV isolates with varying co-receptor specificity's to CXCR4 antagonistic compounds. J Med Virol. 2002 Oct;68(2):147-55. PubMed PMID: 12210401.

273: Liang X, Parkinson JA, Weishäupl M, Gould RO, Paisey SJ, Park HS, Hunter TM, Blindauer CA, Parsons S, Sadler PJ. Structure and dynamics of metallomacrocycles: recognition of zinc xylyl-bicyclam by an HIV coreceptor. J Am Chem Soc. 2002 Aug 7;124(31):9105-12. PubMed PMID: 12149014.

274: Anti-HIV agents. AMD-3100--chemokine blocker under study. TreatmentUpdate. 2000 May;12(3):2-3. PubMed PMID: 12125612.

275: Lukacs NW, Berlin A, Schols D, Skerlj RT, Bridger GJ. AMD3100, a CxCR4 antagonist, attenuates allergic lung inflammation and airway hyperreactivity. Am J Pathol. 2002 Apr;160(4):1353-60. PubMed PMID: 11943720; PubMed Central PMCID: PMC1867206.

276: Zhang WB, Navenot JM, Haribabu B, Tamamura H, Hiramatu K, Omagari A, Pei G, Manfredi JP, Fujii N, Broach JR, Peiper SC. A point mutation that confers constitutive activity to CXCR4 reveals that T140 is an inverse agonist and that AMD3100 and ALX40-4C are weak partial agonists. J Biol Chem. 2002 Jul 5;277(27):24515-21. Epub 2002 Mar 28. PubMed PMID: 11923301.

277: Vödrös D, Thorstensson R, Biberfeld G, Schols D, De Clercq E, Fenyö EM. Coreceptor usage of sequential isolates from cynomolgus monkeys experimentally Infected with simian immunodeficiency virus (SIVsm). Virology. 2001 Dec 5;291(1):12-21. PubMed PMID: 11878872.

278: Vödrös D, Tscherning-Casper C, Navea L, Schols D, De Clercq E, Fenyö EM. Quantitative evaluation of HIV-1 coreceptor use in the GHOST3 cell assay. Virology. 2001 Dec 5;291(1):1-11. PubMed PMID: 11878871.

279: De Clercq E. Hamao Umezawa Memorial Award Lecture: "An Odyssey in the Viral Chemotherapy Field". Int J Antimicrob Agents. 2001 Oct;18(4):309-28. PubMed PMID: 11691563.

280: Pontow S, Ratner L. Evidence for common structural determinants of human immunodeficiency virus type 1 coreceptor activity provided through functional analysis of CCR5/CXCR4 chimeric coreceptors. J Virol. 2001 Dec;75(23):11503-14. PubMed PMID: 11689632; PubMed Central PMCID: PMC114737.

281: Matthys P, Hatse S, Vermeire K, Wuyts A, Bridger G, Henson GW, De Clercq E, Billiau A, Schols D. AMD3100, a potent and specific antagonist of the stromal cell-derived factor-1 chemokine receptor CXCR4, inhibits autoimmune joint inflammation in IFN-gamma receptor-deficient mice. J Immunol. 2001 Oct 15;167(8):4686-92. PubMed PMID: 11591799.

282: Nakagaki K, Nakagaki K, Takahashi K, Schols D, De Clercq E, Tabira T. CXCR4 is the primary receptor for feline immunodeficiency virus in astrocytes. J Neurovirol. 2001 Oct;7(5):487-92. PubMed PMID: 11582522.

283: Gupta SK, Pillarisetti K, Thomas RA, Aiyar N. Pharmacological evidence for complex and multiple site interaction of CXCR4 with SDF-1alpha: implications for development of selective CXCR4 antagonists. Immunol Lett. 2001 Aug 1;78(1):29-34. PubMed PMID: 11470148.

284: Maeda K, Yoshimura K, Shibayama S, Habashita H, Tada H, Sagawa K, Miyakawa T, Aoki M, Fukushima D, Mitsuya H. Novel low molecular weight spirodiketopiperazine derivatives potently inhibit R5 HIV-1 infection through their antagonistic effects on CCR5. J Biol Chem. 2001 Sep 14;276(37):35194-200. Epub 2001 Jul 13. PubMed PMID: 11454872.

285: Hatse S, Princen K, Gerlach LO, Bridger G, Henson G, De Clercq E, Schwartz TW, Schols D. Mutation of Asp(171) and Asp(262) of the chemokine receptor CXCR4 impairs its coreceptor function for human immunodeficiency virus-1 entry and abrogates the antagonistic activity of AMD3100. Mol Pharmacol. 2001 Jul;60(1):164-73. PubMed PMID: 11408611.

286: Gotoh K, Yoshimori M, Kanbara K, Tamamura H, Kanamoto T, Mochizuki K, Fujii N, Nakashima H. Increase of R5 HIV-1 infection and CCR5 expression in T cells treated with high concentrations of CXCR4 antagonists and SDF-1. J Infect Chemother. 2001 Mar;7(1):28-36. PubMed PMID: 11406754.

287: LaBranche CC, Galasso G, Moore JP, Bolognesi DP, Hirsch MS, Hammer SM. HIV fusion and its inhibition. Antiviral Res. 2001 May;50(2):95-115. Review. PubMed PMID: 11369431.

288: Whitson S. Drug watch. Posit Aware. 1999 Jan-Feb;10(1):18-9. PubMed PMID: 11366516.

289: Spenlehauer C, Gordon CA, Trkola A, Moore JP. A luciferase-reporter gene-expressing T-cell line facilitates neutralization and drug-sensitivity assays that use either R5 or X4 strains of human immunodeficiency virus type 1. Virology. 2001 Feb 15;280(2):292-300. PubMed PMID: 11162843.

290: Ghezzi S, Menzo S, Brambilla A, Bordignon PP, Lorini AL, Clementi M, Poli G, Vicenzi E. Inhibition of R5X4 dualtropic HIV-1 primary isolates by single chemokine co-receptor ligands. Virology. 2001 Feb 15;280(2):253-61. PubMed PMID: 11162839.

291: Gerlach LO, Skerlj RT, Bridger GJ, Schwartz TW. Molecular interactions of cyclam and bicyclam non-peptide antagonists with the CXCR4 chemokine receptor. J Biol Chem. 2001 Apr 27;276(17):14153-60. Epub 2001 Jan 11. PubMed PMID: 11154697.

292: Tremblay CL, Kollmann C, Giguel F, Chou TC, Hirsch MS. Strong in vitro synergy between the fusion inhibitor T-20 and the CXCR4 blocker AMD-3100. J Acquir Immune Defic Syndr. 2000 Oct 1;25(2):99-102. PubMed PMID: 11103038.

293: Zhang Y, Lou B, Lal RB, Gettie A, Marx PA, Moore JP. Use of inhibitors to evaluate coreceptor usage by simian and simian/human immunodeficiency viruses and human immunodeficiency virus type 2 in primary cells. J Virol. 2000 Aug;74(15):6893-910. PubMed PMID: 10888629; PubMed Central PMCID: PMC112207.

294: Hendrix CW, Flexner C, MacFarland RT, Giandomenico C, Fuchs EJ, Redpath E, Bridger G, Henson GW. Pharmacokinetics and safety of AMD-3100, a novel antagonist of the CXCR-4 chemokine receptor, in human volunteers. Antimicrob Agents Chemother. 2000 Jun;44(6):1667-73. PubMed PMID: 10817726; PubMed Central PMCID: PMC89930.

295: Cabrera C, Gutiérrez A, Blanco J, Barretina J, Litovchick A, Lapidot A, Evdokimov AG, Clotet B, Esté JA. Anti-human immunodeficiency virus activity of novel aminoglycoside-arginine conjugates at early stages of infection. AIDS Res Hum Retroviruses. 2000 May 1;16(7):627-34. PubMed PMID: 10791873.

296: De Clercq E. Inhibition of HIV infection by bicyclams, highly potent and specific CXCR4 antagonists. Mol Pharmacol. 2000 May;57(5):833-9. Review. PubMed PMID: 10779364.

297: AMD 3100. JM 3100, SDZ SID 791. Drugs R D. 1999 Nov;2(5):337-9. PubMed PMID: 10728474.

298: Zhang Y, Hatse S, De Clercq E, Schols D. CXC-chemokine receptor 4 is not a coreceptor for human herpesvirus 7 entry into CD4(+) T cells. J Virol. 2000 Feb;74(4):2011-6. PubMed PMID: 10644374; PubMed Central PMCID: PMC111679.

299: Blanco J, Barretina J, Henson G, Bridger G, De Clercq E, Clotet B, Esté JA. The CXCR4 antagonist AMD3100 efficiently inhibits cell-surface-expressed human immunodeficiency virus type 1 envelope-induced apoptosis. Antimicrob Agents Chemother. 2000 Jan;44(1):51-6. PubMed PMID: 10602722; PubMed Central PMCID: PMC89627.

300: Bridger GJ, Skerlj RT, Padmanabhan S, Martellucci SA, Henson GW, Struyf S, Witvrouw M, Schols D, De Clercq E. Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-azamacrocycles that inhibit HIV-1 and HIV-2 replication by antagonism of the chemokine receptor CXCR4. J Med Chem. 1999 Sep 23;42(19):3971-81. PubMed PMID: 10508445.

301: Schols D. Promising anti-HIV therapeutic strategy with a small molecule CXCR4 antagonist. Verh K Acad Geneeskd Belg. 1999;61(4):551-64. PubMed PMID: 10500476.

302: Glushakova S, Yi Y, Grivel JC, Singh A, Schols D, De Clercq E, Collman RG, Margolis L. Preferential coreceptor utilization and cytopathicity by dual-tropic HIV-1 in human lymphoid tissue ex vivo. J Clin Invest. 1999 Sep;104(5):R7-R11. PubMed PMID: 10487781; PubMed Central PMCID: PMC408546.

303: Van Gelder J, Witvrouw M, Pannecouque C, Henson G, Bridger G, Naesens L, De Clercq E, Annaert P, Shafiee M, Van den Mooter G, Kinget R, Augustijns P. Evaluation of the potential of ion pair formation to improve the oral absorption of two potent antiviral compounds, AMD3100 and PMPA. Int J Pharm. 1999 Sep 20;186(2):127-36. PubMed PMID: 10486430.

304: Klasse PJ, Rosenkilde MM, Signoret N, Pelchen-Matthews A, Schwartz TW, Marsh M. CD4-Chemokine receptor hybrids in human immunodeficiency virus type 1 infection. J Virol. 1999 Sep;73(9):7453-66. PubMed PMID: 10438835; PubMed Central PMCID: PMC104272.

305: Yi Y, Isaacs SN, Williams DA, Frank I, Schols D, De Clercq E, Kolson DL, Collman RG. Role of CXCR4 in cell-cell fusion and infection of monocyte-derived macrophages by primary human immunodeficiency virus type 1 (HIV-1) strains: two distinct mechanisms of HIV-1 dual tropism. J Virol. 1999 Sep;73(9):7117-25. PubMed PMID: 10438797; PubMed Central PMCID: PMC104231.

306: Egberink HF, De Clercq E, Van Vliet AL, Balzarini J, Bridger GJ, Henson G, Horzinek MC, Schols D. Bicyclams, selective antagonists of the human chemokine receptor CXCR4, potently inhibit feline immunodeficiency virus replication. J Virol. 1999 Aug;73(8):6346-52. PubMed PMID: 10400726; PubMed Central PMCID: PMC112713.

307: Blanco J, Jacotot E, Cabrera C, Cardona A, Clotet B, De Clercq E, Esté JA. The implication of the chemokine receptor CXCR4 in HIV-1 envelope protein-induced apoptosis is independent of the G protein-mediated signalling. AIDS. 1999 May 28;13(8):909-17. PubMed PMID: 10371171.

308: Esté JA, Cabrera C, Blanco J, Gutierrez A, Bridger G, Henson G, Clotet B, Schols D, De Clercq E. Shift of clinical human immunodeficiency virus type 1 isolates from X4 to R5 and prevention of emergence of the syncytium-inducing phenotype by blockade of CXCR4. J Virol. 1999 Jul;73(7):5577-85. PubMed PMID: 10364306; PubMed Central PMCID: PMC112615.

309: Dessolin J, Galea P, Vlieghe P, Chermann JC, Kraus JL. New bicyclam-AZT conjugates: design, synthesis, anti-HIV evaluation, and their interaction with CXCR-4 coreceptor. J Med Chem. 1999 Jan 28;42(2):229-41. PubMed PMID: 9925728.

310: Tamamura H, Xu Y, Hattori T, Zhang X, Arakaki R, Kanbara K, Omagari A, Otaka A, Ibuka T, Yamamoto N, Nakashima H, Fujii N. A low-molecular-weight inhibitor against the chemokine receptor CXCR4: a strong anti-HIV peptide T140. Biochem Biophys Res Commun. 1998 Dec 30;253(3):877-82. PubMed PMID: 9918823.

311: Arakaki R, Tamamura H, Premanathan M, Kanbara K, Ramanan S, Mochizuki K, Baba M, Fujii N, Nakashima H. T134, a small-molecule CXCR4 inhibitor, has no cross-drug resistance with AMD3100, a CXCR4 antagonist with a different structure. J Virol. 1999 Feb;73(2):1719-23. PubMed PMID: 9882387; PubMed Central PMCID: PMC104006.

312: Schols D, De Clercq E. The simian immunodeficiency virus mnd(GB-1) strain uses CXCR4, not CCR5, as coreceptor for entry in human cells. J Gen Virol. 1998 Sep;79 ( Pt 9):2203-5. PubMed PMID: 9747729.

313: Labrosse B, Brelot A, Heveker N, Sol N, Schols D, De Clercq E, Alizon M. Determinants for sensitivity of human immunodeficiency virus coreceptor CXCR4 to the bicyclam AMD3100. J Virol. 1998 Aug;72(8):6381-8. PubMed PMID: 9658078; PubMed Central PMCID: PMC109787.

314: Murakami T, Yamamoto N. [Development of anti-HIV drugs targeted to the coreceptors]. Tanpakushitsu Kakusan Koso. 1998 Apr;43(5):677-85. Review. Japanese. PubMed PMID: 9564785.

315: Donzella GA, Schols D, Lin SW, Esté JA, Nagashima KA, Maddon PJ, Allaway GP, Sakmar TP, Henson G, De Clercq E, Moore JP. AMD3100, a small molecule inhibitor of HIV-1 entry via the CXCR4 co-receptor. Nat Med. 1998 Jan;4(1):72-7. PubMed PMID: 9427609.

316: Schols D, Struyf S, Van Damme J, Esté JA, Henson G, De Clercq E. Inhibition of T-tropic HIV strains by selective antagonization of the chemokine receptor CXCR4. J Exp Med. 1997 Oct 20;186(8):1383-8. PubMed PMID: 9334378; PubMed Central PMCID: PMC2199084.

317: Schols D, Esté JA, Henson G, De Clercq E. Bicyclams, a class of potent anti-HIV agents, are targeted at the HIV coreceptor fusin/CXCR-4. Antiviral Res. 1997 Aug;35(3):147-56. PubMed PMID: 9298754.

318: Datema R, Rabin L, Hincenbergs M, Moreno MB, Warren S, Linquist V, Rosenwirth B, Seifert J, McCune JM. Antiviral efficacy in vivo of the anti-human immunodeficiency virus bicyclam SDZ SID 791 (JM 3100), an inhibitor of infectious cell entry. Antimicrob Agents Chemother. 1996 Mar;40(3):750-4. PubMed PMID: 8851605; PubMed Central PMCID: PMC163192.

319: Esté JA, De Vreese K, Witvrouw M, Schmit JC, Vandamme AM, Anné J, Desmyter J, Henson GW, Bridger G, De Clercq E. Antiviral activity of the bicyclam derivative JM3100 against drug-resistant strains of human immunodeficiency virus type 1. Antiviral Res. 1996 Mar;29(2-3):297-307. PubMed PMID: 8739608.

320: De Vreese K, Reymen D, Griffin P, Steinkasserer A, Werner G, Bridger GJ, Esté J, James W, Henson GW, Desmyter J, Anné J, De Clercq I. The bicyclams, a new class of potent human immunodeficiency virus inhibitors, block viral entry after binding. Antiviral Res. 1996 Mar;29(2-3):209-19. PubMed PMID: 8739600.

321: de Vreese K, Kofler-Mongold V, Leutgeb C, Weber V, Vermeire K, Schacht S, Anné J, de Clercq E, Datema R, Werner G. The molecular target of bicyclams, potent inhibitors of human immunodeficiency virus replication. J Virol. 1996 Feb;70(2):689-96. PubMed PMID: 8551604; PubMed Central PMCID: PMC189868.

322: Joao HC, De Vreese K, Pauwels R, De Clercq E, Henson GW, Bridger GJ. Quantitative structural activity relationship study of bis-tetraazacyclic compounds. A novel series of HIV-1 and HIV-2 inhibitors. J Med Chem. 1995 Sep 15;38(19):3865-73. PubMed PMID: 7562918.

323: De Clercq E, Yamamoto N, Pauwels R, Balzarini J, Witvrouw M, De Vreese K, Debyser Z, Rosenwirth B, Peichl P, Datema R, et al. Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam derivative JM3100. Antimicrob Agents Chemother. 1994 Apr;38(4):668-74. PubMed PMID: 7913308; PubMed Central PMCID: PMC284523.