the farnesyltransferase inhibitor a-176120 shows antitumour activity

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Inpharma 1244 - 1 Jul 2000 The farnesyltransferase inhibitor A-176120 * shows antitumour activity in nude mice bearing human tumour cells, report researchers from the US. In mice inoculated with H-ras NIH3T3 cells, A-176120, compared with vehicle, recipients had suppression of tumour growth and significant prolongation of the time interval for tumours to reach a weight of 1g; similar results were seen with administration of cyclophosphamide (positive control). In mice inoculated with K-ras NIH3T3 cells, mean survival time was significantly longer in A-176120, compared with vehicle, recipients. Administration of A-176120 plus cyclophosphamide resulted in an additive effect. The researchers conclude that their study demonstrates that A-176120 has ‘potential as an anticancer therapeutic agent’. * Abbott Laboratories; preclinical Tahir SK, et al. Inhibition of farnesyltransferase with A-176120, a novel and potent farnesyl pyrophosphate analogue. European Journal of Cancer 36: 1161-1170, Jun 2000 800833058 1 Inpharma 1 Jul 2000 No. 1244 1173-8324/10/1244-0001/$14.95 Adis © 2010 Springer International Publishing AG. All rights reserved

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Page 1: The farnesyltransferase inhibitor A-176120 shows antitumour activity

Inpharma 1244 - 1 Jul 2000

■ The farnesyltransferase inhibitor A-176120* showsantitumour activity in nude mice bearing humantumour cells, report researchers from the US. In miceinoculated with H-ras NIH3T3 cells, A-176120,compared with vehicle, recipients had suppression oftumour growth and significant prolongation of thetime interval for tumours to reach a weight of 1g;similar results were seen with administration ofcyclophosphamide (positive control). In miceinoculated with K-ras NIH3T3 cells, mean survival timewas significantly longer in A-176120, compared withvehicle, recipients. Administration of A-176120 pluscyclophosphamide resulted in an additive effect. Theresearchers conclude that their study demonstratesthat A-176120 has ‘potential as an anticancertherapeutic agent’.* Abbott Laboratories; preclinical

Tahir SK, et al. Inhibition of farnesyltransferase with A-176120, a novel andpotent farnesyl pyrophosphate analogue. European Journal of Cancer 36:1161-1170, Jun 2000 800833058

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Inpharma 1 Jul 2000 No. 12441173-8324/10/1244-0001/$14.95 Adis © 2010 Springer International Publishing AG. All rights reserved