Tasquinimod

Tasquinimod is an orally active small molecule immunomodulator with a novel mode of action, blocking tumor supporting pathways in the bone marrow microenvironment. Tasquinimod is being developed for the treatment of blood cancers, with focus on myelofibrosis.

This is tasquinimod

The tumor microenvironment in the bone marrow is essential for development of blood cancers and a key driver of disease recurrency as well as resistance to treatment.

Tasquinimod targets cells in the microenvironment of the bone marrow, immunosuppressive myeloid cells, endothelial cells, and mesenchymal cells, which play a central role in the development of blood cancers. Tasquinimod affects the function of these cells, leading to reduced tumor growth, reduced fibrosis, and restored hematopoiesis.

Myelofibrosis

Myelofibrosis is a rare form of blood cancer. The sex- and age-adjusted incidence is estimated at approximately 1.5 cases per 100,000 people, with a prevalence of 12 patients per 100,000 people (Slowley et al., 2024). This would translate to a prevalence of more than 100,000 people with myelofibrosis in the EU, US, UK, and Japan.

The underlying cause of myelofibrosis is unknown. Patients with myelofibrosis have an abnormal production of blood-forming cells leading to the replacement of healthy bone marrow with scar tissue (fibrosis).

Due to the lack of normal blood cell production, patients typically show laboratory value abnormalities, such as anemia and changes in white blood cell counts, and blood cell-differentiation. Later symptoms include enlargement of the spleen, an increased risk for infections, night sweats and fever. Myelofibrosis is associated with shortened survival, due to for instance bone marrow failure and transformation into acute leukemia.

Current treatments and market

Myelofibrosis can be treated with bone marrow transplantation for eligible individuals, erythropoietin to manage anemia and JAK2 inhibitors to reduce spleen size. Today the following drugs are approved for these patients as symptom-directed therapy: Hydroxy-urea, ruxolitinib, momelotinib, fedratinib and pacritinib (the latter four are JAK2 inhibitors, JAKi). At present there are no approved treatment options that would reverse bone marrow fibrosis in myelofibrosis, and there are only limited treatment options available for myelofibrosis patients whose disease progress during JAKi treatment or cannot tolerate JAKi.

Sales of drugs for the treatment of myelofibrosis is in the eight major markets (US, 5EU, Japan and China) amounted to USD 2,3 billion in 2021 and is projected to grow to USD 2,9 billion by 2031 (Global Data Report March 2023 – Myelofibrosis – Eight Market Drug Forecast and Market Analysis 2021-2031).

Myelofibrosis: Need for disease-modifying treatment

 

Source: GlobalData March 2023, 8 major markets (US, EU5, Japan and China). Presented data are based on 2031 forecast numbers.

Tasquinimod in myelofibrosis

Preclinical studies have shown that tasquinimod reduces myeloproliferation, splenomegaly (enlarged spleen), and fibrosis in models of myelofibrosis (Leimkühler et al. Cell Stem Cell. 2021). Preclinical experiments using malignant cells from patients have further shown that tasquinimod works synergistically with a JAK- or BET inhibitor to reduce spleen size and prolong survival (Fiskus et al. Blood 2023, Fiskus et al. Blood 2024). These promising results suggest that tasquinimod could be a valuable addition to the treatment options for myelofibrosis patients. In collaboration with research groups at Erasmus MC, the Netherlands and at The University of Texas MD Anderson Cancer Center, US, Active Biotech will explore myelofibrosis as a new high value orphan indication for tasquinimod within blood cancers. In February 2022, a global patent license agreement was signed with Oncode Institute, acting on behalf of Erasmus MC, for tasquinimod in myelofibrosis. Under the agreement, Oncode Institute grants to Active Biotech a global exclusive license to develop and commercialize tasquinimod in myelofibrosis. Proof of-concept studies with tasquinimod in myelofibrosis patients are ongoing in Europe and at MD Anderson Cancer Center, TX.

The study in Europe is conducted by the HOVON (Stichting HematoOncologie voor Volwassenen Nederland) research network at clinics in The Netherlands and Germany. The study is mainly funded by Oncode Institute. Preclinical results from a collaboration with a research group at MD Anderson were presented in December 2023 at an oral session and 2024 as a poster at the annual meeting of the American Society of Hematology (ASH) in San Diego, USA. The results demonstrated tasquinimod’s efficacy as monotherapy and in combination with approved and investigational drugs in models of advanced myelofibrosis. These positive results create a rationale for the ongoing clinical study in patients with myelofibrosis at MD Anderson.

Tasquinimod was granted orphan designation in myelofibrosis by the US Food and Drug Administration (FDA) in May 2022.

Ongoing clinical development in myelofibrosis

Proof-of-concept studies with tasquinimod in myelofibrosis patients are ongoing in US and Europe..

  • The study in US, performed at MD Anderson Cancer Center, TX, is currently ongoing. More information about the study can be found in the box below.
  • The study in Europe, conducted by the HOVON (Stichting Hemato-Oncologie voor Volwassenen Nederland) research network at clinics in The Netherlands and Germany is ongoing. The study is funded by Oncode Institute.

Tasquinimod was granted orphan designation in myelofibrosis by the FDA in May 2022.

More information can be found in the box below and at www.clinicaltrials.gov

Multiple myeloma

Multiple myeloma is an incurable blood cancer where abnormal plasma cells in the bone marrow grow uncontrollably while other blood forming cells, such as white and red blood cells and blood platelets, are suppressed. This leads to anemia, infections, destruction of bone tissue and progressive loss of renal function.

Despite new treatments which have greatly improved survival of multiple myeloma patients, the biological heterogeneity of the disease and the emergence of drug resistance is a major challenge, and the medical need of innovative treatment modalities remains high.

The market for treatment of multiple myeloma

The number of diagnosed prevalent multiple myeloma cases in the eight major markets (US, 5EU, Japan and China) in 2022 amounted to approximately 317,000 and is projected to grow to approximately 352,000 by 2032. In 2022 the US represented 49 percent of the diagnosed cases, the 5 major EU markets 26 percent and Japan and China combined 25 percent. (Global Data Report July 2024, Multiple Myeloma – Eight Market Drug Forecast 2022 – 2032).

The global sales of drugs for the treatment of multiple myeloma in the eight major markets amounted to USD 21.2 billion in 2022 and is projected to reach USD 29.3 billion in 2032. (Global Data Report July 2024, Multiple Myeloma – Eight Market Drug Forecast 2022-2032).

The market for drugs used in the treatment of multiple myeloma experiences strong growth and is expected to continue to grow strongly due to the greater incidence in an elderly population, longer progression-free and overall survival, and thanks to new treatments and combination are made available. Of the projected total market sales 2032, the US market represents around 68 percent, the five major EU markets approximately 20 percent and Japan and China for 4 and 8 percent respectively. (Global Data Report July 2024, Multiple Myeloma – Eight Market Drug Forecast 2022 – 2032).

Multiple myeloma – Market Driven by Novel Treatments

Source: Global Data Report July 2024, Multiple Myeloma – Eight Market Drug Forecast 2022-2032.

Current treatments

Multiple myeloma patients undergo several lines of treatment. In both early and later treatment lines, the goal is to reduce tumor burden, improve symptoms and thereby achieve as long a period of effective disease control as possible. To support deeper and durable responses and overcome treatment resistance patients are as standard treated with combinations of drugs from available product classes. Currently, the market is dominated by drugs that can be divided into the following classes: immunomodulatory imides (IMiDs), proteasome inhibitors (PI), monoclonal antibodies, bispecific antibodies, Chimeric Antigen Receptor T- cells (CAR-T) and alkylating agents.

Disease course of multiple myeloma

Tasquinimod in multiple myeloma

Tasquinimod is being developed as a new product class with a distinct and novel mechanism of action and thus has the potential to overcome the problem of drug resistance. The clinical safety profile of tasquinimod is well known from previous clinical phase I-III trials. Given the good tolerability and the possibility to combine with available product classes, tasquinimod has the potential to expand over time from an initial position as the 3rd line treatment to earlier lines of treatment. There is a significant market opportunity for a novel drug in a new product class in multiple myeloma.

Tasquinimod was granted orphan designation in multiple myeloma by the US Food and Drug Administration (FDA) in 2017.

Ongoing clinical development

Based on preclinical data and the previous clinical experience with tasquinimod, a clinical study was initiated, and the first patient was dosed in August 2020. The study has recruited patients with relapsed refractory multiple myeloma who have undergone at least one treatment for myeloma and has been conducted in two parts:

  • First part (A) studying tasquinimod as a monotherapy
  • Second part (B) studying the combination of tasquinimod and an oral standard anti-myeloma regimen (IRd; ixazomib, lenalidomide, dexamethasone)

The recruitment is completed and the data are being analysed.

More information about the ongoing study can be found in the box below . and at www.clinicaltrials.gov

Previous clinical experience of tasquinimod

Tasquinimod has been in development for the treatment of prostate cancer and has completed a phase I-III clinical development program. While the results from the phase III trial in prostate cancer showed that tasquinimod prolonged progression-free survival (PFS) compared to placebo, tasquinimod did not extend overall survival (OS) in this patient population and the development for prostate cancer was discontinued. Tasquinimod was studied in both healthy subjects and cancer patients.

Clinical effects and a favorable safety profile have been demonstrated in more than 1,500 patients, equivalent to more than 650 patient-years of exposure to tasquinimod. Extensive datasets including a regulatory package of preclinical and clinical safety and full commercial scale CMC documentation has been generated.

Targeting the tumor microenvironment

Phase Ib/IIa in multiple myeloma

Completed

Based on preclinical data and the previous clinical experience with tasquinimod, a clinical study was initiated, and the first patient was dosed in August 2020. The study has recruited patients with relapsed refractory multiple myeloma who have undergone at least one prior anti-myeloma therapy and was conducted in two parts:

  • First part (A) studying tasquinimod as a monotherapy
  • Second part (B) studying the combination of tasquinimod and an oral standard anti-myeloma regimen (IRd; ixazomib, lenalidomide, dexamethasone)

The primary endpoint in both parts was safety and tolerability, and key secondary endpoint is preliminary efficacy by objective response rate.

Important milestones were reached in October 2021, February 2022, and May 2023, September 2023 and July 2024 respectively. In October 2021 ten patients in part A had been treated with increasing doses of tasquinimod and the safety read-out showed that tasquinimod was generally well tolerated. The optimal dosing schedule of tasquinimod, when used as a single agent in patients with multiple myeloma has been established at 1 mg per day after a one-week run in of 0.5 mg daily. This is similar to the treatment schedule used in previous studies of tasquinimod. The patients included in this study phase were heavily pretreated, and 8 of the 10 patients were triple refractory to IMiDs, proteosome inhibitors, and anti-CD-38 monoclonal antibodies.

While none of the patients formally achieved a partial response, 3 patients with documented progressive myeloma at study entry achieved significant periods of stable disease on single agent tasquinimod therapy.

This suggests that tasquinimod has anti-myeloma activity in patients with advanced disease that is resistant to established therapies.

In February 2022, the trial subsequently advanced to the previously planned combination part of the phase Ib/IIa study in which tasquinimod is tested in patients with multiple myeloma together with the orally administered anti-myeloma agents ixazomib, lenalidomide, and dexamethasone (IRd).

In September 2023, Active Biotech announced that the dose optimization of tasquinimod + IRd was completed, and the expansion part of the study was started to further document the biological activity of tasquinimod + IRd in patients with multiple myeloma.

Results from the study were presented in June 2025 at the annual meeting of American Society of Clinical Oncology (ASCO).

A total of 17 patients received tasquinimod in combination with iRd. Patients were heavily pretreated with a median of 7 prior lines of therapy (range 4-19) and all were triple-class refractory with 71% (12 pts) refractory to their most recent Imid/PI combination. In the total combination cohort, there was one partial response and 7 minimal responses which resulted in a 47% Clinical Benefit Rate (CBR). Among the 12 patients’ refractory to their latest Imid/PI combination there was one durable partial response (lasting 19.8 months) and three minimal responses (lasting 1.2, 1.5 and 6.7 months) resulting in a CBR of 33%. These patients were unlike to respond to IRd alone and the result suggests synergistic efficacy of tasquinimod with the IRd combination.

The results highlight the potential for targeting the tumor microenvironment with tasquinimod to augment the efficacy of other myeloma therapies. Tasquinimod was well tolerated in combination with ixazomib, lenalidomide, and dexamethasone and the safety profile was in line with previous experience. The most common treatment emergent adverse events included fatigue, gastrointestinal events, pain and respiratory infections. Mostly of mild to moderate grade.

These results will yield important information also for the new hematological indications with tasquinimod.

The study is carried out in an academic partnership with Abramson Cancer Center in Philadelphia, PA, US, with Dr. Dan Vogl as the principal investigator. More information about the study design is available at clinicaltrials.gov (NCT04405167).

Phase II in myelofibrosis

Ongoing

In July 2024, Active Biotech entered into a clinical trial agreement with MD Anderson Cancer Center, TX, US, to start a clinical phase II trial in patients with myelofibrosis. Thrombocytosis Myelofibrosis (Post-ET MF)”. The study is actively enrolling patients since August 2024.

The title of the study is: “Open Label Phase 2 Study of Tasquinimod in Patients with Primary Myelofibrosis (PMF), Post-Polycythemia Vera Myelofibrosis (Post-PV MF), or Post-Essential The study is composed of two separate cohorts which recruit patients parallelly. Cohort 1 evaluates tasquinimod as a single agent in patients with JAKi refractory disease and in patients who are ineligible for JAKi treatment. Cohort 2 evaluates tasquinimod in combination with the JAKi in patients who have a suboptimal response to JAKi alone. The study will enroll up to 33 patients: 12 in cohort 1 and 21 in cohort 2.

The primary endpoint for both cohorts is efficacy: Objective Response Rate (ORR) according to the International Working Group (IWG-MRT) criteria for treatment response in myelofibrosis. ORR is defined as the proportion of patients with Complete Remission (CR), Partial Response (PR) or Clinical Improvement (CI) after six cycles of treatment. Secondary endpoints include safety and tolerability, time to response, response duration, changes in spleen volume and symptom score as well as bone marrow fibrosis grade.

The study is carried out in an academic partnership with MD Anderson Cancer Center, TX, US with Dr Lucia Masarova as the Principal Investigator. More information about the study available at clinicaltrials.gov (NCT06327100).

Phase Ib/II in myelofibrosis

Ongoing

In July 2023, Active Biotech entered into an agreement between the Oncode Institute, Erasmus MC and Stichting-Haemato-Oncologie Volwassenen Netherlands (HOVON) for a clinical study in myelofibrosis. HOVON is one of the leading European clinical study groups in hematological malignancies and is the legal sponsor of the study. The study has been actively recruiting patients since January 2025 and aims to include up to 20 patients.

The title of the study is “Tasquinimod in Patients with Myelofibrosis Refractory to or Intolerant for JAK2 Inhibition” (HOVON 172 MF), and it evaluates tasquinimod as monotherapy in patients with myelofibrosis who have previously been treated with a JAKi or who are not suitable for treatment with JAKi. In addition to safety and tolerability, the study will examine the effect of tasquinimod on the disease by measuring changes in clinically relevant variables including spleen volume, symptom control and bone marrow fibrosis grade.

For more information about the study, visit clinicaltrials.gov (NCT06605586)

Publications

Clinical Activity of Novel Targeting of S100A9 with Tasquinimod for Relapsed and Refractory Multiple Myeloma (RRMM)
Dan T. Vogl, Yulia Nefedova, E. Paul Wileyto, Sara Whittington , Cynthia Diaczynsky, Chau T. Nguyen, Inna Strakovsky, Eva Bondesson, Helén Tuvesson, Erik Vahtola, Adam D. Cohen, Sandra P. Susanibar-Adaniya, Adam J. Waxman, Shivani Kapur, Alfred L. Garfall, Edward A. Stadtmauer. Postern presenterades vid American Society of Clinical Oncology årliga möte 2025 (ASCO 2025) i Chicago, IL, 30 maj-3 juni 2025. Se postern här

Evaluation of the lethal activity and its mechanism of tasquinimod in advanced myeloproliferative neoplasm (MPN) in blastic phase. Warren Fiskus, Lucia Masarova, Christopher P. Mill, Christine E. Birdwell, Kaberi Das, John A. Davis, Hanxi Hou, Kevin Philip, Alicia Matthews, Taghi Manshouri, Surbhi Sharma, Tapan M. Kadia, Courtney D. DiNardo, Prithviraj Bose, Naveen Pemmaraju, Sanam Loghavi, Marie Törngren, and Kapil N. Bhalla. The poster was presented at the 66:e American Society of Hematology Annual Meeting (ASH 2024) i San Diego, CA, 7-10 December 2024. See the poster here

Preclinical Studies Demonstrating Efficacy of Tasquinimod in Models of Advanced Myeloproliferative Neoplasm (MPN) in Blastic Phase. Warren C. Fiskus, Lucia Masarova, Christopher Peter Mill, Christine Birdwell, Kaberi Das, John Davis, Hanxi Hou, Noor Alhamadani, Kevin Philip, Alicia Matthews, Taghi Manshouri, Tapan M. Kadia, Courtney D. DiNardo, Prithviraj Bose, Naveen Pemmaraju, Sanam Loghavi, Marie Törngren and Kapil N. Bhalla. Oral presentation (slides) presented at the 65th American Society of Hematology Annual Meeting (ASH 2023) in San Diego, CA, December 9-12, 2023. Read the presentation here.

Tasquinimod Improves Erythropoiesis and Mitigates Bone Loss in Myelodysplastic Mice. Manja Wobus, Heike Weidner, Kristin Möbus, Anna-Lena Baumann, Ivonne Habermann, Tolga Danismaz, Ekaterina Balaian, Marie Törngren, Helena Eriksson, Eva Bondesson, Martina Rauner, Martin Bornhaeuser and Katja Sockel. Abstract presented at the 65th American Society of Hematology Annual Meeting (ASH 2023) in San Diego, CA, December 9-12, 2023. Read the abstract here.

S100A8/S100A9 Promote Progression of Multiple Myeloma via Expansion of Megakaryocytes. Lin C, Garcia-Gerique L, Bonner EE, Mastio J, Rosenwasser M, Cruz Z, Lawler M, Bernabei L, Muthumani K, Liu Q, Poncz M, Vogl T, Törngren M, Eriksson H, Vogl DT, Gabrilovich DI, Nefedova Y. Cancer Res Commun. 2023 Mar 13;3(3):420-430. Read the article here.

Tasquinimod suppresses tumor cell growth and bone resorption by targeting immunosuppressive myeloid cells and inhibiting c-MYC expression in multiple myeloma. Fan R, Satilmis H, Vandewalle N, Verheye E, Vlummens P, Maes A, Muylaert C, De Bruyne E, Menu E, Evans H, Chantry A, De Beule N, Hose D, Törngren M, Eriksson H, Vanderkerken K, Maes K, Breckpot K, De Veirman K. J Immunother Cancer.  2023 Jan;11(1):e005319. Read the article here.

Targeting S100A9 in the Inflammatory Myelodysplastic Hematopoietic Niche Reprograms the Functional Properties of CD271+ Mesenchymal Stromal Cells. Manja Wobus, Ekaterina Balaian, Triantafyllos Chavakis, Alexander Funk, Thomas Krüger, Uwe Platzbecker, Marie Törngren, Helena Eriksson, Eva Bondesson, Martin Bornhäuser, Katja Sockel. Presented at the 64rd ASH Annual Meeting 2022. Read the poster here.

Tasquinimod Targets Immunosuppressive Myeloid Cells, Increases Osteogenesis and Has Direct Anti-Myeloma Effects By Inhibiting c-Myc Expression in Vitro and In Vivo. Rong Fan, Hatice Satilmis, Niels Vandewalle, Elke De Bruyne, PhD, Eline Menu, PhD, Andrew D Chantry, PhD, MD, Holly Evans, BSc, Marie Törngren, Helena Eriksson, PhD, Karine Breckpot, PhD, Ken Maes, PhD, Karin Vanderkerken, PhD, Kim De Veirman, PhD. Presented at the 63rd ASH Annual Meeting & Exposition 2021. Read the abstract here and the poster here.

Targeting the Inflammatory Niche in MDS By Tasquinimod Restores Hematopoietic Support and Suppresses Immune-Checkpoint Expression in Vitro. Manja Wobus, PhD, Ekaterina Balaian, Uta Oelschlaege, PhD, Russell Towers, Kristin Möbus, Ivonne Habermann, Rebekka Wehner, Friedrich Stölzel, Triantafyllos Chavakis, Marie Törngren, Helena Eriksson, PhD, Uwe Platzbecker, MD, Christoph Röllig, MD, MSC, Martin Bornhäuser, MD, Katja Sockel. Presented at the 63rd ASH Annual Meeting & Exposition 2021. Read the abstract here and the poster here.

Inhibition of S100A9 with tasquinimod demonstrates potent anti-tumor activity in pre-clinical models of multiple myeloma. Cindy Lin , Aubrey Leso , Matthew Rosenwasser , Marie Torngren , Helena Eriksson , Yulia Nefedova. Presented at the Virtual Edition of the 25th European Hematology Association (EHA) Annual Congress Meeting, 2020. Read the abstract here and the poster here.

A randomized, double blind, placebo controlled phase 2 study of maintenance therapy with tasquinimod in patients with metastatic castration-resistant prostate cancer responsive to or stabilized during first-line docetaxel chemotherapy. Fizazi K, Ulys A, Sengeløv L, Moe M, Ladoire S, Thiery-Vuillemin A, Flechon A, Guida A, Bellmunt J, Climent MA, Chowdhury S, Dumez H, Matouskova M, Penel N, Liutkauskiene S, Stachurski L, Sternberg CN, Baton F, Germann N, Daugaard G. Ann Oncol. 2017; 28: 2741-46

A Phase II Multicentre, Open-Label, Proof-of-Concept Study of Tasquinimod in Hepatocellular, Ovarian, Renal Cell, and Gastric Cancers. Escudier B, Faivre S, Van Cutsem E, Germann N, Pouget J-C, Plummer R, Vergote I, Thistlethwaite F, Bjarnason GA, Jones R, Mackay H, Edeline J, Fartoux L, Hirte H, Oza A. Targ Oncol. 2017; 12: 655–61

Phase Ib Trial of Cabazitaxel and Tasquinimod in Men With Heavily Pretreated Metastatic Castration Resistant Prostate Cancer (mCRPC): The CATCH Trial. Armstrong A, Humeniuk M, Healy P, Szmulewitz R, Winters C, Kephart J, Harrison M, Martinez E, Mundy K, Halabi S, George D. The Prostate. 2017; 77: 385-95

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. 2016; 34(22): 2636-43.

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; 5:6, e1145333

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

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; 3(2): 1-13

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. 2011; 29(30): 4022-4028

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(8): 1233-40

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. 2006; 66: 1768-78