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Open-label, clinical phase I studies of tasquinimod in patients with castration-resistant prostate cancer.

Bratt, Ola LU ; Häggman, M; Ahlgren, Göran LU ; Nordle, O; Björk, A and Damber, J-E (2009) In British Journal of Cancer 101. p.1233-1240
Abstract
Background:Tasquinimod is a quinoline-3-carboxamide derivative with anti-angiogenic activity. Two open-label phase I clinical trials in patients were conducted to evaluate the safety and tolerability of tasquinimod, with additional pharmacokinetic and efficacy assessments.Methods: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.Results:A total of 32 patients were enrolled; 21 patients were maintained for >/=4 months. The maximum tolerated dose was determined to be 0.5 mg per day; but when using stepwise... (More)
Background:Tasquinimod is a quinoline-3-carboxamide derivative with anti-angiogenic activity. Two open-label phase I clinical trials in patients were conducted to evaluate the safety and tolerability of tasquinimod, with additional pharmacokinetic and efficacy assessments.Methods: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.Results:A total of 32 patients were enrolled; 21 patients were maintained for >/=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 >/=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.British Journal of Cancer advance online publication, 15 September 2009; doi:10.1038/sj.bjc.6605322 www.bjcancer.com. (Less)
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type
Contribution to journal
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published
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in
British Journal of Cancer
volume
101
pages
1233 - 1240
publisher
Nature Publishing Group
external identifiers
  • wos:000270767200002
  • pmid:19755981
  • scopus:70349952393
ISSN
1532-1827
DOI
10.1038/sj.bjc.6605322
language
English
LU publication?
yes
id
b7512391-60f7-45b2-82b4-163fcae5783a (old id 1483445)
alternative location
http://www.ncbi.nlm.nih.gov/pubmed/19755981?dopt=Abstract
date added to LUP
2009-10-07 12:06:03
date last changed
2017-11-12 04:05:45
@article{b7512391-60f7-45b2-82b4-163fcae5783a,
  abstract     = {Background:Tasquinimod is a quinoline-3-carboxamide derivative with anti-angiogenic activity. Two open-label phase I clinical trials in patients were conducted to evaluate the safety and tolerability of tasquinimod, with additional pharmacokinetic and efficacy assessments.Methods: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.Results:A total of 32 patients were enrolled; 21 patients were maintained for >/=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 >/=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.British Journal of Cancer advance online publication, 15 September 2009; doi:10.1038/sj.bjc.6605322 www.bjcancer.com.},
  author       = {Bratt, Ola and Häggman, M and Ahlgren, Göran and Nordle, O and Björk, A and Damber, J-E},
  issn         = {1532-1827},
  language     = {eng},
  pages        = {1233--1240},
  publisher    = {Nature Publishing Group},
  series       = {British Journal of Cancer},
  title        = {Open-label, clinical phase I studies of tasquinimod in patients with castration-resistant prostate cancer.},
  url          = {http://dx.doi.org/10.1038/sj.bjc.6605322},
  volume       = {101},
  year         = {2009},
}