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Tasquinimod

Tasquinimod is a quinoline-3-carboxamide linomide analogue with antiangiogenic and potential antineoplastic activities. Tasquinimod has been shown to decrease blood vessel density but the exact mechanism of action is not known. This agent has also been shown to augment the antineoplastic effects of docetaxel and androgen ablation in a murine model of prostate cancer involving human prostate cancer xenografts. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

The orally active quinoline-3-carboxamide tasquinimod [ABR-215050; CAS number 254964-60-8), which currently is in a phase II-clinical trial in patients against metastatic prostate cancer, exhibits anti-tumor activity via inhibition of tumor angiogenesis in human and rodent tumors. Tasquinimod-induced up-regulation of TSP1 is part of a mechanism involving down-regulation of HIF1alpha and VEGF, which in turn leads to reduced angiogenesis via inhibition of the "angiogenic switch", that could explain tasquinimods therapeutic potential. see: http://www.ncbi.nlm.nih.gov/pubmed/20470445.

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Highlight of recent study using tasquinimod

Tasquinimod  phase II clinical trial  in men with minimally symptomatic metastatic castrate-resistant prostate cancer. (data published in Oct 2011). A randomized, double-blind, placebo-controlled phase II trial  was conducted in men assigned (at a ratio of two to one) to either oral once-daily tasquinimod (TASQ) 0.25 mg/d escalating to 1.0 mg/d over 4 weeks or placebo. The primary end point was the proportion of patients without disease progression at 6 months, defined by Response Evaluation Criteria in Solid Tumors Group, Prostate Cancer Working Group (PCWG2), or pain criteria, excluding prostate-specific antigen. Two hundred one men (134 assigned to TASQ; 67 to placebo) were evaluable, and baseline characteristics were well balanced. Six-month progression-free proportions for TASQ and placebo groups were 69% and 37%, respectively (P < .001), and median progression-free survival (PFS) was 7.6 versus 3.3 months (P = .0042). TASQ significantly slowed progression and improved PFS in patients with metastatic CRPC with an acceptable AE profile. (source: J Clin Oncol. 2011 Oct 20;29(30):4022-8.)

Tasquinimod phase I clinical trial in patients with castration-resistant prostate cancer (data published in 2009). Patients with castration-resistant prostate cancer with no previous chemotherapy were enrolled in this study. The patients received tasquinimod up to 1 year either at fixed doses of 0.5 or 1.0 mg per day or at an initial dose of 0.25 mg per day that escalated to 1.0 mg per day. A total of 32 patients were enrolled; 21 patients were maintained for >or=4 months. The maximum tolerated dose was determined to be 0.5 mg per day; but when using stepwise intra-patient dose escalation, a dose of 1.0 mg per day was well tolerated. The dose-limiting toxicity was sinus tachycardia and asymptomatic elevation in amylase. Common treatment-emergent adverse events included transient laboratory abnormalities, anaemia, nausea, fatigue, myalgia and pain. A serum prostate-specific antigen (PSA) decline of >or=50% was noted in two patients. The median time to PSA progression (>25%) was 19 weeks. Only 3 out of 15 patients (median time on study: 34 weeks) developed new bone lesions. CONCLUSION: Long-term continuous oral administration of tasquinimod seems to be safe, and the overall efficacy results indicate that tasquinimod might delay disease progression. (source: Br J Cancer. 2009 Oct 20;101(8):1233-40).

1: Hansson GP, Olin M, Svanström C, Svensson LD, Sennbro CJ. Bioanalysis in clinical development of tasquinimod using liquid chromatography/tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2011 Nov 15;879(30):3401-6. Epub 2011 Sep 13. PubMed PMID: 21963277.

2: Pili R, Häggman M, Stadler WM, Gingrich JR, Assikis VJ, Björk A, Nordle O, Forsberg G, Carducci MA, Armstrong AJ. Phase II randomized, double-blind, placebo-controlled study of tasquinimod in men with minimally symptomatic metastatic castrate-resistant prostate cancer. J Clin Oncol. 2011 Oct 20;29(30):4022-8. Epub 2011 Sep 19. PubMed PMID: 21931019.

3: Dalrymple SL, Becker RE, Zhou H, Deweese TL, Isaacs JT. Tasquinimod prevents the angiogenic rebound induced by fractionated radiation resulting in an enhanced therapeutic response of prostate cancer xenografts. Prostate. 2011 Aug 11. doi: 10.1002/pros.21467. [Epub ahead of print] PubMed PMID: 21837778.

4: George D, Moul JW. Emerging treatment options for patients with castration-resistant prostate cancer. Prostate. 2011 Jul 11. doi: 10.1002/pros.21435. [Epub ahead of print] PubMed PMID: 21748753.

5: Isaacs JT. The long and winding road for the development of tasquinimod as an oral second-generation quinoline-3-carboxamide antiangiogenic drug for the treatment of prostate cancer. Expert Opin Investig Drugs. 2010 Oct;19(10):1235-43. Review. PubMed PMID: 20836618.

6: Olsson A, Björk A, Vallon-Christersson J, Isaacs JT, Leanderson T. Tasquinimod (ABR-215050), a quinoline-3-carboxamide anti-angiogenic agent, modulates the expression of thrombospondin-1 in human prostate tumors. Mol Cancer. 2010 May 17;9:107. PubMed PMID: 20470445; PubMed Central PMCID: PMC2885345.

7: Bratt O, Häggman M, Ahlgren G, Nordle O, Björk A, Damber JE. Open-label, clinical phase I studies of tasquinimod in patients with castration-resistant prostate cancer. Br J Cancer. 2009 Oct 20;101(8):1233-40. Epub 2009 Sep 15. PubMed PMID: 19755981; PubMed Central PMCID: PMC2768463.

8: Dalrymple SL, Becker RE, Isaacs JT. The quinoline-3-carboxamide anti-angiogenic agent, tasquinimod, enhances the anti-prostate cancer efficacy of androgen ablation and taxotere without effecting serum PSA directly in human xenografts. Prostate. 2007 May 15;67(7):790-7. PubMed PMID: 17373719.

9: Isaacs JT, Pili R, Qian DZ, Dalrymple SL, Garrison JB, Kyprianou N, Björk A, Olsson A, Leanderson T. Identification of ABR-215050 as lead second generation quinoline-3-carboxamide anti-angiogenic agent for the treatment of prostate cancer. Prostate. 2006 Dec 1;66(16):1768-78. PubMed PMID: 16955399.