Lomeguatrib - CAS 192441-08-0
Catalog number: 192441-08-0
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Lomeguatrib, also known as PaTrin-2,  is a potent Inhibitor of O6-Alkylguanine-DNA-Alkyltransferase. Lomeguatrib is also a nontoxic low-molecular weight pseudosubstrate that has the ability to inactivate MGMT. Lomeguatrib can be used with temozolomide (TMZ) for GBM treatment.
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white solid powder
Patrin. O6-(4-bromothenyl)guanine; 6-(4-Bromothenyloxy)-7H-purin-2-amine.
Current Developer:
KuDOS Pharmaceuticals Ltd. and AstraZeneca
1.Impact of O6-methylguanine-DNA methyltransferase (MGMT) promoter methylation and MGMT expression on dacarbazine resistance of Hodgkin's lymphoma cells.
Kewitz S1, Stiefel M1, Kramm CM2, Staege MS3. Leuk Res. 2014 Jan;38(1):138-43. doi: 10.1016/j.leukres.2013.11.001. Epub 2013 Nov 13.
We analyzed the methylation status of the O6-methylguanine-DNA methyltransferase (MGMT) promoter and mRNA expression in HL cells and assessed the response of these cells to dacarbazine. Expression of MGMT correlated with the presence of non-methylated promoters and cell lines with non-methylated promoters showed increased resistance against dacarbazine. KM-H2 cells expressed fusion transcripts between MGMT and proline-rich coiled-coil 2B (PRRC2B) but no wild type MGMT transcripts. Dacarbazine sensitivity suggested that fusion transcripts are translated into a protein with reduced functionality. MGMT promoter methylation predicts dacarbazine sensitivity of HL cells and it might be interesting to analyze this factor in HL patients.
2.Temozolomide: mechanisms of action, repair and resistance.
Zhang J1, Stevens MF, Bradshaw TD. Curr Mol Pharmacol. 2012 Jan;5(1):102-14.
Glioblastoma multiforme is the most common aggressive adult primary tumour of the central nervous system. Treatment includes surgery, radiotherapy and adjuvant temozolomide (TMZ) chemotherapy. TMZ is an alkylating agent prodrug, delivering a methyl group to purine bases of DNA (O6-guanine; N7-guanine and N3-adenine). The primary cytotoxic lesion, O6-methylguanine (O6-MeG) can be removed by methylguanine methyltransferase (MGMT; direct repair) in tumours expressing this protein, or tolerated in mismatch repair-deficient (MMR-) tumours. Thus MGMT or MMR deficiency confers resistance to TMZ. Inherent- and acquired resistance to TMZ present major obstacles to successful treatment. Strategies devised to thwart resistance and enhance response to TMZ, including inhibition of DNA repair mechanisms which contribute to TMZ resistance, are under clinical evaluation. Depletion of MGMT prior to alkylating agent chemotherapy prevents O6-MeG repair; thus, MGMT pseudosubstrates O6-benzylguanine and lomeguatrib are able to sensitise tumours to TMZ.
3.Tumor O(6)-methylguanine-DNA methyltransferase inactivation by oral lomeguatrib.
Watson AJ1, Sabharwal A, Thorncroft M, McGown G, Kerr R, Bojanic S, Soonawalla Z, King A, Miller A, Waller S, Leung H, Margison GP, Middleton MR. Clin Cancer Res. 2010 Jan 15;16(2):743-9. doi: 10.1158/1078-0432.CCR-09-1389. Epub 2010 Jan 12.
PURPOSE: A major mechanism of resistance to chlorethylnitrosureas and methylating agents involves the DNA repair protein O(6)-methylguanine-DNA methyltransferase (MGMT). We sought to determine the dose of oral 6-(4-bromo-2-thienyl) methoxy purin-2-amine (lomeguatrib), a pseudosubstrate inactivator of MGMT, required to render active protein undetectable 12 hours after dosing in prostate, primary central nervous system (CNS), and colorectal cancer patients.
4.Inhibition of DNA repair with MGMT pseudosubstrates: phase I study of lomeguatrib in combination with dacarbazine in patients with advanced melanoma and other solid tumours.
Tawbi HA1, Villaruz L, Tarhini A, Moschos S, Sulecki M, Viverette F, Shipe-Spotloe J, Radkowski R, Kirkwood JM. Br J Cancer. 2011 Sep 6;105(6):773-7. doi: 10.1038/bjc.2011.285. Epub 2011 Aug 2.
BACKGROUND: The DNA repair protein O6-methylguanine-DNA methyltransferase (MGMT) reverses the O6-methylguanine (O6-meG) lesion induced by dacarbazine. Depletion of MGMT can be achieved using O6-meG pseudosubstrates. Herein, we report the first phase I experience of the novel O6-meG pseudosubstrate lomeguatrib, combined with dacarbazine.
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CAS 192441-08-0 Lomeguatrib

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