Delving into the Latest Updates on Tasquinimod with Synapse

The goal of this clinical trial is to learn if therapy can be improved in patients with myelofibrosis (MF) who have primary resistance or who have progressed after treatment with a Janus kinase (JAK) inhibitor or are intolerant for this category of drugs.
The main questions it aims to answer are:
* To evaluate the feasibility and safety of once daily dose of tasquinimod for 24 weeks (6 cycles)
* To determine the optimal dose
Patients will be treated once daily with tasquinimod for a maximum period of 24 weeks (6 cycles).
During the study most (diagnostic) procedures are part of the standard of care. Different from standard of care:
* Participation may lead to extra visits to the outpatient clinic
* Additional blood will be drawn when blood is already taken per standard of care
* Bone marrow sampling at entry and at the end of the trial
* MRI scans (or CT-scans) have to be performed
* Quality-of-life questionnaires have to be filled out

Start Date20 Feb 2025

Sponsor / Collaborator

Hemato-Oncologie voor Volwassenen Nederland

NCT06327100

/ RecruitingPhase 1/2IIT

Open Label Phase 1/2 Study of Tasquinimod in Patients With Primary Myelofibrosis (PMF), Post-Polycythemia Vera Myelofibrosis (Post-PV MF), or Post-Essential Thrombocytosis Myelofibrosis (Post-ET MF)

To learn if tasquinimod either alone or in combination with ruxolitinib can help to control PMF, post-PV MF, or post-ET MF.

Start Date01 Aug 2024

Sponsor / Collaborator

The University of Texas MD Anderson Cancer Center

[+1]

ACTRN12621000016831

/ Not yet recruitingPhase 2

A randomized, double-blind, placebo-controlled phase II trial to evaluate the efficacy of tasquinimod in reducing the time taken for a 2-point decrease in admission status.in adults with COVID-19

Start Date15 Dec 2022

Sponsor / Collaborator

Hunter Medical Research Institute

100 Clinical Results associated with Tasquinimod

Login to view more data

100 Translational Medicine associated with Tasquinimod

Login to view more data

100 Patents (Medical) associated with Tasquinimod

Login to view more data

84

Literatures (Medical) associated with Tasquinimod

01 Feb 2026·INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES

Macrophage-derived S100A9 drives liver fibrosis in Echinococcus multilocularis infection by up-regulating secreted protein acidic and rich in cysteine (SPARC) in hepatic stellate cells

Article

Author: Zhang, Xue ; Lü, Guodong ; Bi, Xiaojuan ; Li, Liang ; Lin, Renyong ; Yang, Ning ; Shi, Bowen ; Zhang, Hongbin ; Chu, Jin ; Xue, Junlong

Alveolar echinococcosis (AE), caused by Echinococcus multilocularis(E. multilocularis) infection, is a severe parasitic disease characterized by progressive liver fibrosis. Although the damage-associated molecular pattern molecule S100A9 has been implicated in some inflammatory and fibrotic diseases, its role in AE induced liver fibrosis remains unclear. This study aimed to elucidate the function and mechanism of S100A9 in E. multilocularis induced liver fibrogenesis. Using proteomic analysis, we identified significant up-regulation of S100A9 in the livers of infected mice. In a stem cell-based fibrosis regression model, S100A9 expression correlated closely with the extent of fibrosis. Cellular localization and macrophage depletion experiments revealed macrophages as the primary source of S100A9. In vitro, recombinant S100A9 directly activated human hepatic stellate cells (HSCs) LX-2, up-regulating fibrotic markers in a time-dependent manner. Proteomic and molecular analyses further identified SPARC as a critical downstream mediator, and SPARC knockdown attenuated S100A9 induced HSCs activation and TGF-β/SMAD signaling. In vivo, pharmacological inhibition of S100A9 with tasquinimod significantly ameliorated liver fibrosis, down-regulated SPARC expression, and suppressed SMAD2/3 phosphorylation. Critically, histopathological analysis of liver tissues from AE patients confirmed that S100A9 expression was predominantly localized to fibrotic areas and positively correlated with fibrosis severity. Collectively, these results demonstrate that macrophage-derived S100A9 promotes HSCs activation and liver fibrosis via SPARC dependent way, mechanism, and its clinical relevance in human AE substantiates the S100A9-SPARC axis as a potential therapeutic target in AE.

01 Jan 2026·JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Comparative Investigation of Cytotoxic Effects of Structurally Diverse Small Molecules and In Silico Analysis of 1‐Acetyl‐4‐(4‐Hydroxyphenyl)piperazine

Article

Author: Emrah Tümer ; Mustafa Güzel ; Azmi Yerlikaya

ABSTRACT:

This study assessed the anticancer activity of boron‐containing and structurally diverse small molecules in 4T1 breast cancer and Caco‐2 colon adenocarcinoma cells. Initial screening showed that five boronic acids lacked significant cytotoxicity, underscoring the structural specificity required for boron‐mediated bioactivity. Similarly, reference compounds, including fumaric acid, caffeic acid, ferulic acid, dimethyl malonate and N‐(tert‐butoxycarbonyl)‐L‐alanine, showed no cytotoxic effect under identical conditions. Among the tested agents, 1‐acetyl‐4‐(4‐hydroxyphenyl)piperazine (1A4HP) displayed the most potent cytotoxicity, with IC 50 values of 149.7 μM in 4T1 and 825 μM in Caco‐2 cells. For comparison, the clinically investigated antimetastatic agent tasquinimod showed moderate activity in 4T1 cells (IC 50 = 180.7 μM), serving as a pharmacological benchmark. Mechanistic assays revealed that 1A4HP induced apoptosis and significantly impaired 4T1 cell migration, suggesting combined antiproliferative and antimetastatic effects. Computational analyses further supported 1A4HP's drug‐like potential by predicting favourable physicochemical properties, including balanced lipophilicity and high solubility. Molecular docking studies indicated a strong binding affinity to oestrogen receptor alpha (ERα), surpassing that of tamoxifen. Notably, despite 4T1's ER‐negative status, 1A4HP suppressed cell growth, suggesting possible ER‐independent or off‐target mechanisms, similar to tamoxifen's secondary effects. Collectively, these results identify 1A4HP as a promising lead compound for further exploration in breast cancers.

13 Nov 2025·ACS Medicinal Chemistry Letters

Identification and Preliminary Characterization of a Novel Tasquinimod Analog that Unexpectedly Induces Mitotic Arrest by Alteration of Microtubule Dynamics

Article

Author: Abushaikha, Ghassan M. ; Bayazid, Abdel ; Wadwekar, Shreyas ; Kaba, Isaac ; Chitwood, Tyler J. ; Nickelson, Kierra ; Hasan, Safiyyah ; Taylor, William R. ; Rathnayake, Dewmi ; Abdollahi, Negin

While investigating the SAR associated with tasquinimod, whose anticancer activity is primarily derived from inhibition of S100A9 and HDAC4, we designed and prepared several analogues. We identified a potent hit (FB2) that showed cytotoxicity against several cancer cells with IC₅₀s between 0.3 and 2.0 μM. Surprisingly, FB2 appeared to halt cells during mitosis. To better define the relevance of FB2's unanticipated action, we further explored its mechanism and found that it significantly alters microtubule dynamics. KT-1 exposed to FB2 showed an elongated cellular morphology with condensed chromosomes and mitotic spindles. FB2 also reduced the rate of microtubule regrowth in cells; however, we are unable to conclude whether this is due to direct binding to tubulin or to some indirect mechanism involving initial interaction with some other target sites. These effects on tubulin dynamics are likely responsible for defects in spindle structure, mitotic arrest, and the observed robust killing of cancer cells.

27

News (Medical) associated with Tasquinimod

12 Feb 2026

·www.activebiotech.com

Active Biotech Year End Report 2025

FOURTH QUARTER IN BRIEF Active Biotech announced a fully secured rights issue, subject to approval by an extraordinary general meeting, of approximately SEK 70 million before transaction costs (October 17) Active Biotech announced that preclinical data of tasquinimod in combination with T cell activation will be presented at ASH 2025 (November 3) Active Biotech announced that positive preclinical tasquinimod data in myelofibrosis has been published in Blood Advances (November 24). Active Biotech announced that a patent related to a pharmaceutical formulation of tasquinimod will be granted in the United States (November 25). Active Biotech disclosed the outcome of the rights issue (December 10). OTHER SIGNIFICANT EVENTS JAN-DEC 2025 US Patent Office granted Active Biotech’s patent application for laquinimod in eye disorders (January 28). Active Biotech announced that the first patient was enrolled in the European clinical study of tasquinimod in myelofibrosis (February 24). Active Biotech announced that the first patient was dosed in the phase II study of tasquinimod in myelofibrosis in the US (March 10). Active Biotech reported positive top-line results from the LION study on ocular absorption and distribution of laquinimod in the eye (May 5). Active Biotech reported study results with tasquinimod in heavily pre-treated patients with relapsed refractory multiple myeloma (May 23). EVENTS AFTER THE END OF THE PERIOD Active Biotech receives positive feedback on its clinical study with tasquinimod in myelofibrosis (February 10, 2026) FINANCIAL SUMMARY The report is also available at www.activebiotech.com The information was submitted, through the agency of the contact person below, for public disclosure on 2026-02-12 at 08:30 CEST.

Clinical ResultPhase 2Drug Approval

25 Nov 2025

·www.activebiotech.com

Active Biotech’s patent related to a pharmaceutical formulation of tasquinimod will be granted in the US

“This patent marks an important step in our strategy to optimize the global multi-layer protection for tasquinimod. In addition, tasquinimod is covered by multiple patents and patent applications mainly for medical use in relevant indications and has been granted orphan drug status by the FDA for the treatment of myelofibrosis and multiple myeloma,” said Active Biotech’s CEO Helén Tuvesson. The patent application relates to a pharmaceutical formulation of tasquinimod with a high oral bioavailability.

Orphan Drug

24 Nov 2025

·www.activebiotech.com

Positive preclinical tasquinimod data in myelofibrosis published in Blood Advances

The article, titled Preclinical efficacy of tasquinimod -based combinations in advanced myeloproliferative neoplasms in blastic phase, has been published in Blood Advances with Warren Fiskus, Ph.D. Assistant Professor of Leukemia at The University of Texas MD Anderson Cancer Center, as lead author. The article is the result of a collaboration between Active Biotech and a research group at MD Anderson led by Kapil Bhalla, M.D., professor of Leukemia, and aims to support the clinical development of tasquinimod in myelofibrosis. The data presented show that tasquinimod reduces the expression of, among others, S100A9 in disease cells in cell models of advanced myelofibrosis and thereby increases the mortality of these disease cells but not in normal cells. Data also show that treatment with tasquinimod reduces leukemia burden and improves survival in advanced myelofibrosis models. Combination therapy with tasquinimod and ruxolitinib or a BET inhibitor further improved survival in these models. ”These findings clearly highlight the potential of tasquinimod as monotherapy and in combination with other drugs in the treatment of advanced myelofibrosis,” said Marie Törngren, VP R&D Active Biotech. Clinical phase I/II studies of tasquinimod as monotherapy and in combination with JAK2 inhibitor in patients with myelofibrosis are ongoing in US and Europe. Link to the article: Preclinical efficacy of tasquinimod-based combinations in advanced myeloproliferative neoplasms in blastic phase | Blood Advances | American Society of Hematology

ASH

100 Deals associated with Tasquinimod

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
-	Tasquinimod	-	DB05861

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Castration-Resistant Prostatic Cancer	Phase 3	China	Ipsen SA	01 Jan 2014
Castration-Resistant Prostatic Cancer	Phase 3	South Korea	Ipsen SA	01 Jan 2014
Adenocarcinoma of prostate	Phase 3	United States	Active Biotech AB	24 Mar 2011
Adenocarcinoma of prostate	Phase 3	United States	Apoteket AB	24 Mar 2011
Adenocarcinoma of prostate	Phase 3	Argentina	Active Biotech AB	24 Mar 2011
Adenocarcinoma of prostate	Phase 3	Argentina	Apoteket AB	24 Mar 2011
Adenocarcinoma of prostate	Phase 3	Australia	Apoteket AB	24 Mar 2011
Adenocarcinoma of prostate	Phase 3	Australia	Active Biotech AB	24 Mar 2011
Adenocarcinoma of prostate	Phase 3	Belgium	Active Biotech AB	24 Mar 2011
Adenocarcinoma of prostate	Phase 3	Belgium	Apoteket AB	24 Mar 2011

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04405167 (ASCO 12023 \| ASCO 22023) Manual	Phase 1	Relapse multiple myeloma	10	tasquinimod	zdixkfrlli(plwdgrsbfl) = 0.5 mg qd x1 wk, then 1 mg qd (a single-agent MTD of 1 mg daily after a 1-week dose escalation) yznkeebzxh (yenckrfyrb ) View more	Positive	26 May 2023
NCT02057666 (TasQ003, CTgov)	Phase 3	Castration-Resistant Prostatic Cancer \| Metastatic castration-resistant prostate cancer	146	Tasquinimod (Tasquinimod)	kbuaqfdsnt(rxqtyungzc) = jepogkabnu iqkmiuaxsu (ermisdhape, ialpzdyipo - xgwlrcwqjt) View more	-	23 Apr 2021
				Placebo (Placebo)	kbuaqfdsnt(rxqtyungzc) = kifpdupuml iqkmiuaxsu (ermisdhape, vwguxwendr - cexxbdboql) View more
NCT01743469 (CTgov)	Phase 2	Metastatic Renal Cell Carcinoma \| Ovarian Cancer \| Neoplasm Metastasis ... View more	201	Tasquinimod (Hepatocellular Carcinoma Cohort)	bnietlgagu = qugjmrdovz denhqnnqvw (hkqrxljynt, xxvpjiidbl - zwvznjllxp) View more	-	07 May 2018
				Tasquinimod (Ovarian Carcinoma Cohort)	bnietlgagu = oimpjhlwot denhqnnqvw (hkqrxljynt, blzkyljgyh - shhxxkftwd) View more
NCT01732549 (Pubmed \| Ann Oncol) Manual	Phase 2	Metastatic castration-resistant prostate cancer First line	144	tasquinimod	nnchweezdi(zxzwageide) = hoxwpiqbvz wlelnhxyub (siakoxoggu, 24.3 - 53.7) View more	Positive	01 Nov 2017
				Placebo	nnchweezdi(zxzwageide) = kqjgumysbv wlelnhxyub (siakoxoggu, 16.1 - 25.9) View more
NCT01732549 (Pubmed)	Phase 2	Metastatic castration-resistant prostate cancer Maintenance	144	Tasquinimod	zngzsmqxnm(mpabkynudi) = mnrjjozsvk zvhzuelwcr (rjfjgxtwuh, 24.3 - 53.7)	Positive	01 Nov 2017
				Placebo	zngzsmqxnm(mpabkynudi) = dsoqxmkdbv zvhzuelwcr (rjfjgxtwuh, 16.1 - 25.9)
NCT01743469 (Pubmed \| Target Oncol)	Phase 2	Stomach Cancer	201	Tasquinimod (Hepatocellular cancer)	ajsigxhbin(yopowpnjol) = jiigvtxbrd vzlmqryaht (fjbcqiyowu )	Negative	01 Oct 2017
				Tasquinimod (Ovarian cancer)	ajsigxhbin(yopowpnjol) = iocdctenzs vzlmqryaht (fjbcqiyowu )
NCT01732549 (CTgov)	Phase 2	Castration-Resistant Prostatic Cancer	144	Tasquinimod (Tasquinimod)	aihaeiddpj(vhdvypblkb) = titmhmatwx jseemconog (jqmkrhytot, iztjffzolg - dsiqexzwou) View more	-	03 Oct 2016
				Placebo (Placebo)	aihaeiddpj(vhdvypblkb) = lftlcbaqsg jseemconog (jqmkrhytot, uccdamnjfq - jzwfktozpu) View more
NCT01234311 (Pubmed \| J Clin Oncol)	Phase 3	Metastatic castration-resistant prostate cancer	-	Tasquinimod	uwdllrjspe(cfpfkusnqu) = okjnzfcnxj ghobiuafmm (osmpnxtwbu, 19.5 - 23.0) View more	Positive	01 Aug 2016
				Placebo	uwdllrjspe(cfpfkusnqu) = hwubpihunx ghobiuafmm (osmpnxtwbu, 21.4 - 26.9) View more
NCT02159950 (CTgov)	Phase 2	Recurrent Prostate Carcinoma \| Castration-Resistant Prostatic Cancer \| Metastatic castration-resistant prostate cancer ... View more	2	Laboratory Biomarker Analysis+Sipuleucel-T (Arm I (Sipuleucel-T))	cisgpgdkch(jhikyipgwa) = wjxwzoftqj eewniyfjha (iplrptxoph, ycozmchelb - lsbnmhikmb) View more	-	20 May 2016
				Laboratory Biomarker Analysis+Tasquinimod+Sipuleucel-T (Arm II (Tasquinimod, Sipuleucel-T))	lgilpiqqci = xjsmoeewvr oqtfgotgvt (yusbmzxcum, ttbnslxjbb - wboijiarvn) View more
NCT01732549 (ASCO2013)	Phase 2	Metastatic castration-resistant prostate cancer Maintenance	140	Tasquinimod	tbvcguepga(tpwenawuoe) = wjyowlcvky juwcpoglyr (admfqlxbuw )	-	20 May 2013
				Placebo	tbvcguepga(tpwenawuoe) = jvwxyybknv juwcpoglyr (admfqlxbuw )