2020-10-20

1: Back HM, Lee JH, Chae JW, Song B, Seo JW, Yun HY, Kwon KI. A novel HPLC-MS/MS 
method for the simultaneous determination of astemizole and its major metabolite 
in dog or monkey plasma and application to pharmacokinetics. J Pharm Biomed Anal. 
2015 Oct 10;114:121-6. doi: 10.1016/j.jpba.2015.04.036. Epub 2015 May 21. PubMed 
PMID: 26037160.

2: de Guadalupe Chávez-López M, Pérez-Carreón JI, Zuñiga-García V, Díaz-Chávez J, 
Herrera LA, Caro-Sánchez CH, Acuña-Macías I, Gariglio P, Hernández-Gallegos E, 
Chiliquinga AJ, Camacho J. Astemizole-based anticancer therapy for hepatocellular 
carcinoma (HCC), and Eag1 channels as potential early-stage markers of HCC. 
Tumour Biol. 2015 Aug;36(8):6149-58. doi: 10.1007/s13277-015-3299-0. Epub 2015 
Mar 18. PubMed PMID: 25783527.

3: Kong X, Chen L, Jiao L, Jiang X, Lian F, Lu J, Zhu K, Du D, Liu J, Ding H, 
Zhang N, Shen J, Zheng M, Chen K, Liu X, Jiang H, Luo C. Astemizole arrests the 
proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb 
repressive complex 2. J Med Chem. 2014 Nov 26;57(22):9512-21. doi: 
10.1021/jm501230c. Epub 2014 Nov 12. PubMed PMID: 25369470.

4: García-Quiroz J, García-Becerra R, Santos-Martínez N, Barrera D, Ordaz-Rosado 
D, Avila E, Halhali A, Villanueva O, Ibarra-Sánchez MJ, Esparza-López J, 
Gamboa-Domínguez A, Camacho J, Larrea F, Díaz L. In vivo dual targeting of the 
oncogenic Ether-à-go-go-1 potassium channel by calcitriol and astemizole results 
in enhanced antineoplastic effects in breast tumors. BMC Cancer. 2014 Oct 
3;14:745. doi: 10.1186/1471-2407-14-745. PubMed PMID: 25280486; PubMed Central 
PMCID: PMC4194404.

5: de Guadalupe Chávez-López M, Hernández-Gallegos E, Vázquez-Sánchez AY, 
Gariglio P, Camacho J. Antiproliferative and proapoptotic effects of astemizole 
on cervical cancer cells. Int J Gynecol Cancer. 2014 Jun;24(5):824-8. doi: 
10.1097/IGC.0000000000000151. PubMed PMID: 24819656.

6: Wagner E, Wittmann HJ, Elz S, Strasser A. Pharmacological profile of 
astemizole-derived compounds at the histamine H1 and H4 receptor--H1/H4 receptor 
selectivity. Naunyn Schmiedebergs Arch Pharmacol. 2014 Mar;387(3):235-50. doi: 
10.1007/s00210-013-0926-4. Epub 2013 Nov 17. PubMed PMID: 24241585.

7: Roman G, Crandall IE, Szarek WA. Synthesis and anti-Plasmodium activity of 
benzimidazole analogues structurally related to astemizole. ChemMedChem. 2013 
Nov;8(11):1795-804. doi: 10.1002/cmdc.201300172. Epub 2013 Sep 10. PubMed PMID: 
24022991.

8: Karapetyan YE, Sferrazza GF, Zhou M, Ottenberg G, Spicer T, Chase P, Fallahi 
M, Hodder P, Weissmann C, Lasmézas CI. Unique drug screening approach for prion 
diseases identifies tacrolimus and astemizole as antiprion agents. Proc Natl Acad 
Sci U S A. 2013 Apr 23;110(17):7044-9. doi: 10.1073/pnas.1303510110. Epub 2013 
Apr 1. PubMed PMID: 23576755; PubMed Central PMCID: PMC3637718.

9: García-Quiroz J, García-Becerra R, Barrera D, Santos N, Avila E, Ordaz-Rosado 
D, Rivas-Suárez M, Halhali A, Rodríguez P, Gamboa-Domínguez A, Medina-Franco H, 
Camacho J, Larrea F, Díaz L. Astemizole synergizes calcitriol antiproliferative 
activity by inhibiting CYP24A1 and upregulating VDR: a novel approach for breast 
cancer therapy. PLoS One. 2012;7(9):e45063. doi: 10.1371/journal.pone.0045063. 
Epub 2012 Sep 12. PubMed PMID: 22984610; PubMed Central PMCID: PMC3440370.

10: García-Quiroz J, Camacho J. Astemizole: an old anti-histamine as a new 
promising anti-cancer drug. Anticancer Agents Med Chem. 2011 Mar;11(3):307-14. 
Review. PubMed PMID: 21443504.

11: Lee EH, Oh JH, Park HJ, Kim DG, Lee JH, Kim CY, Kwon MS, Yoon S. Simultaneous 
gene expression signature of heart and peripheral blood mononuclear cells in 
astemizole-treated rats. Arch Toxicol. 2010 Aug;84(8):609-18. doi: 
10.1007/s00204-010-0529-5. Epub 2010 Mar 11. PubMed PMID: 20221588.

12: Rojo LE, Alzate-Morales J, Saavedra IN, Davies P, Maccioni RB. Selective 
interaction of lansoprazole and astemizole with tau polymers: potential new 
clinical use in diagnosis of Alzheimer's disease. J Alzheimers Dis. 
2010;19(2):573-89. doi: 10.3233/JAD-2010-1262. PubMed PMID: 20110603; PubMed 
Central PMCID: PMC2951486.

13: Vu K, Gelli A. Astemizole and an analogue promote fungicidal activity of 
fluconazole against Cryptococcus neoformans var. grubii and Cryptococcus gattii. 
Med Mycol. 2010 Mar;48(2):255-62. doi: 10.1080/13693780903081968. PubMed PMID: 
19572230.

14: Li F, Hsieh Y, Kang L, Sondey C, Lachowicz J, Korfmacher WA. MALDI-tandem 
mass spectrometry imaging of astemizole and its primary metabolite in rat brain 
sections. Bioanalysis. 2009 May;1(2):299-307. doi: 10.4155/bio.09.27. PubMed 
PMID: 21083169.

15: Musonda CC, Whitlock GA, Witty MJ, Brun R, Kaiser M. Chloroquine-astemizole 
hybrids with potent in vitro and in vivo antiplasmodial activity. Bioorg Med Chem 
Lett. 2009 Jan 15;19(2):481-4. doi: 10.1016/j.bmcl.2008.11.047. Epub 2008 Nov 18. 
PubMed PMID: 19054674.

16: Sastry CS, Naidu PY. Spectrophotometric determination of astemizole. Talanta. 
1998 Mar;45(5):795-9. PubMed PMID: 18967063.

17: Srikanth D, Shenoy RR, Rao CM. The effects of topical (gel) astemizole and 
terfenadine on wound healing. Indian J Pharmacol. 2008 Aug;40(4):170-4. doi: 
10.4103/0253-7613.43164. PubMed PMID: 20040951; PubMed Central PMCID: PMC2792619.

18: Guba W, Green LG, Martin RE, Roche O, Kratochwil N, Mauser H, Bissantz C, 
Christ A, Stahl M. From astemizole to a novel hit series of small-molecule 
somatostatin 5 receptor antagonists via GPCR affinity profiling. J Med Chem. 2007 
Dec 13;50(25):6295-8. Epub 2007 Nov 19. PubMed PMID: 18020391.

19: Gómez-Varela D, Contreras-Jurado C, Furini S, García-Ferreiro R, Stühmer W, 
Pardo LA. Different relevance of inactivation and F468 residue in the mechanisms 
of hEag1 channel blockage by astemizole, imipramine and dofetilide. FEBS Lett. 
2006 Sep 18;580(21):5059-66. Epub 2006 Aug 28. PubMed PMID: 16949586.

20: Chong CR, Chen X, Shi L, Liu JO, Sullivan DJ Jr. A clinical drug library 
screen identifies astemizole as an antimalarial agent. Nat Chem Biol. 2006 
Aug;2(8):415-6. Epub 2006 Jul 2. PubMed PMID: 16816845.