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Tasquinimod

Phase Ib Trial of Cabazitaxel and Tasquinimod in Men With Heavily Pretreated Metastatic Castration Resistant Prostate Cancer (mCRPC): The CATCH Trial. The Prostate 2016, Published online, DOI 10.1002/pros.23277. Armstrong A, Humeniuk M, Healy P, Szmulewitz R, Winters C, Kephart J, Harrison M, Martinez E, Mundy K, Halabi S, George D.

Randomized, Double-Blind, Placebo-Controlled Phase III Study of Tasquinimod in Men With Metastatic Castration-Resistant Prostate Cancer. Sternberg C., Armstrong A., Pili R., Ng S., Huddart R., Agarwal N., Khvorostenko D., Lyulko O.,  Brize A., Vogelzang N., Delva R., Harza M, Thanos A, James N., Werbrouck P., Bögemann M., Hutson T, Milecki P., Chowdhury S., Gallardo E., Schwartsmann G., Pouget J-C., Baton F., Nederman T., Tuvesson H., Carducci M. J. Clin. Oncol Aug 2016 34(22): 2636-43. http://dx.doi.org/10.1200/JCO.2016.66.9697

Tasquinimod in the treatment of castrate-resistant prostate cancer – current status and future prospects. Mehta A.R., Armstrong A.J. Ther Adv Urol 2016, Vol. 8(1), 9-18

Tasquinimod modulates tumor-infiltrating myeloid cells and improves the antitumor immune response to PD-L1 blockade in bladder cancer. Nakhlé J., Pierron V., Bauchet A-L., Plas P., Thiongane A., Meyer-Losic F., Schmidlin F. Oncoimmunol 2016, Vol. 0, No. 0, e1145333 (15 pages). http://dx.doi.org/10.1080/2162402X.2016.1145333

Tasquinimod triggers an early change in the polarization of tumor associated macrophages in the tumor microenvironment. Olsson A., Nakhlé J., Sundstedt A., Plas P., Bauchet A-L., Pierron V., Bruetschy L., Deronic A., Törngren M., Liberg D., Schmidlin F., Leanderson T. J ImmunoTher Cancer (2015) 3:53 DOI 10.1186/s40425-015-0098-5

A novel agent tasquinimod demonstrates a potent anti-tumor activity in pre-clinical models of multiple myeloma. Ramachandran I.R., Lin C., Chase T., Gabrilovich D., Nefedova Y. Blood 2014, 124: 5729

Tasquinimod modulates suppressive myeloid cells and enhances cancer immunotherapies in murine models. Shen L, Sundstedt A, Ciesielski MJ, Miles KM, Celander M, Adelaiye R, Orillion A, Ciamporcero E, Ramakrishnan S, Ellis L, Fenstermaker RA, Abrams SI, Eriksson H, Leanderson T, Olsson A, Pili R. Cancer Immunol Res. 2014 Nov 4. pii: canimm.0036.2014.

Assessment of the bone scan index in a randomized placebo-controlled trial of tasquinimod in men with metastatic castration-resistant prostate cancer (mCRPC). Armstrong AJ,Kaboteh R, Carducci M A, Damber JE, Stadler W M, Hansen M, Edenbrandt L, Forsberg G, Nordle Ö, Pili R, Morris M J. Urol Oncol. 2014 Nov;32(8):1308-16

Long-term Survival and Biomarker Correlates of Tasquinimod Efficacy in a Multicenter Randomized Study of Men with Minimally Symptomatic Metastatic Castration-Resistant Prostate Cancer. Armstrong A.J, Häggman M, Stadler W.M, Gingrich J.R, Assikis V, Polikoff J, Damber J.E, Belkoff L, Nordle Ö, Forsberg G, Carducci M.A, and Pili R. Clin Cancer Res; Published Online November 19, 2013; doi:10.1158/1078-0432.CCR-13-1581.

Mechanisms of action of tasquinimod on the tumour microenvironment.
Raymond E, Dalgleish A, Damber J-E, Smith M, Pili R. Cancer Chemother Pharmacol. Oct 2013. DOI 10.1007/s00280-013-2321-8.

Tasquinimod is an allosteric modulator of HDAC4 survival signaling within the compromised cancer microenvironment. Isaacs J.T, Antony L , Dalrymple S.L, Brennen N.W, Gerber S, Hammers H, Wissing M, Kachhap S, Luo J, Xing L, Björk P, Olsson A, Björk A and Leanderson T. Cancer Res; 73(4) February 15, 2013

Tasquinimod: A Novel Angiogenesis Inhibitor–Development in Prostate Cancer. George S and Pili R. Curr Oncol Rep. Publ online 20 Jan, 2013.

From Bevacizumab to Tasquinimod - Angiogenesis as a Therapeutic Target in Prostate Cancer. Schweizer M.T, MD, and Carducci M.A, MD. The Cancer Journal & Volume 19, Number 1, January/February 2013.

A review of tasquinimod in the treatment of advanced prostate cancer. Williamson S.C, Hartley E.A, Heer R. Drug Design, Development and Therapy 2013:7, 167-174.

S100A9 Interaction with TLR4 Promotes Tumor Growth. Källberg E, Vogl T, Liberg D, Olsson A, Björk P, et al. March 2012, PLoS ONE 7(3): e34207. DOI:10.1371/journal.pone.0034207.

Inhibition of metastasis in a castration resistant prostate cancer model by the quinoline-3-carboxamide tasquinimod (ABR-215050). Jennbacken K, Welén K, Olsson A, Axelsson B, Törngren M, Damber J-E, Leanderson T.
The Prostate 2011; advance online publication October 5, 2011; DOI 10.1002/pros.21495

Phase II Randomized, Double-Blind, Placebo-Controlled Study of Tasquinimod in Men With Minimally Symptomatic Metastatic Castrate-Resistant Prostate Cancer. Pili R, Häggman M, Stadler W.M, Gingrich J.R, Assikis V.J, Björk A, Nordle Ö, Forsberg G, Carducci M.A, Armstrong A.J. J. Clin. Oncol  Oct 20, 2011:4022-4028 (published online on Sep 19, 2011; DOI:10.1200/JCO.2011.35.6295.).

Tasquinimod (ABR-215050), a quinoline-3-carboxamide anti-angiogenic agent, modulates the expression of thrombospondin-1 in human prostate tumors. Olsson A, Björk A, Vallon-Christersson J, isaacs JT, Leanderson T. Molecular Cancer 2010, 9:107, DOI:10.1186/1476-4598-9-107.

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. Isaacs J T. Expert Opin. Investig. Drugs (2010) 19(10):1235-1243.

Open-label, clinical phase I studies of tasquinimod in patients with castration-resistant prostate cancer. O Bratt, M Häggman, G Ahlgren, Ö Nordle, A Björk and J-E Damber
Br J Cancer 2009 101: 1233-1240; advance online publication, September 15, 2009; 10.1038/sj.bjc.6605322

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.
Dalrymple SL, Becker RE, Isaacs JT. Prostate 67, 790-7, May 15, 2007.

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