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DRUG CLASS:

DHODH inhibitor

6d
Teriflunomide modulates the PD-1/PD-L1 axis and enhances antitumor immunity in colorectal cancer. (PubMed, Oncogenesis)
These findings highlight TER as a promising immune checkpoint modulator that targets the PD-1/PD-L1 axis to promote CD8+ T-cell-mediated antitumor immunity. Because of its established safety profile, TER is a readily translatable therapeutic for enhancing cancer immunotherapy in CRC.
Journal • PD(L)-1 Biomarker • IO biomarker
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CD8 (cluster of differentiation 8) • GZMB (Granzyme B)
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PD-L1 expression
7d
Leflunomide in Previously Treated Metastatic Triple Negative Cancers (clinicaltrials.gov)
P1/2, N=17, Completed, Joseph Sparano | Active, not recruiting --> Completed
Trial completion
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
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ER positive • HER-2 negative • PIK3CA mutation • HER-2 negative + ER positive
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leflunomide
16d
ARAVA PASS: A Study of the Effectiveness of Additional Risk Minimization Measures Related to ARAVA® (Leflunomide) in Saudi Arabia (clinicaltrials.gov)
P=N/A, N=3500, Active, not recruiting, Sanofi | Trial completion date: Dec 2025 --> Mar 2026 | Trial primary completion date: Nov 2025 --> Mar 2026
Trial completion date • Trial primary completion date
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leflunomide
17d
Integrating network pharmacology, microbiomics, and metabolomics to uncover the therapeutic effect of Liubao tea on osteoarthritis. (PubMed, Front Immunol)
Additionally, Brequinar, a de novo pyrimidine synthesis inhibitor, was used to verify the role of pyrimidine metabolism...The molecular docking results demonstrated that Eupatilin, 5,6,7,8-Tetramethoxyflavone, and 5-Hydroxy-6,7,3',4',5'-Pentamethoxyflavone exhibited potential interactions with the hub targets TP53, IL6, and TNF. Liubao tea attenuates OA progression by modulating the composition of the gut microbiota and inhibiting the pyrimidine metabolism pathway, highlighting its potential as a novel natural therapeutic agent for OA.
Journal • Metabolomic study
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TP53 (Tumor protein P53) • IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • IL1B (Interleukin 1, beta)
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brequinar (DUP 785)
20d
Leflunomide for the Treatment of High-Risk Smoldering Multiple Myeloma in African-American and European-American Patients (clinicaltrials.gov)
P2, N=27, Active, not recruiting, City of Hope Medical Center | Recruiting --> Active, not recruiting | N=56 --> 27 | Trial completion date: Jul 2026 --> Jan 2027 | Trial primary completion date: Jul 2026 --> Jan 2027
Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date
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leflunomide
21d
Dual metabolic reprogramming by metal-polyphenol nanoplatform enhances ferroptotic therapy for triple-negative breast cancer. (PubMed, J Colloid Interface Sci)
This work reveals for the first time that brequinar (BQR, a DHODH inhibitor) exerts dual-edged effects on ferroptotic therapy against 4T1 cells: besides its well-known disruption of cellular redox balance for ferroptosis sensitization, BQR-intervened pyrimidine metabolism blocks tumor growth, accompanied by up-regulation of lipid droplets (LDs), which paradoxically aggravates ferroptosis resistance...This work helps to accelerate DHODH inhibitors' clinical translation by elucidating previously overlooked mechanisms limiting DHODH inhibitors' efficacy and proposing synchronous DGAT1 inhibition as a countermeasure. The fabricated nanoweapon AB@HA-TA/Fe presents a novel dual metabolic intervention paradigm for ferroptosis sensitization, proposing an innovative framework for ferroptosis-integrated combination therapy of TNBC.
Journal
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GPX4 (Glutathione Peroxidase 4)
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brequinar (DUP 785)
1m
ENSURE-1: Study to Evaluate the Efficacy, Safety, and Tolerability of IMU-838 in Patients With Relapsing Multiple Sclerosis (clinicaltrials.gov)
P3, N=1121, Active, not recruiting, Immunic AG | Recruiting --> Active, not recruiting | Trial completion date: Sep 2032 --> Sep 2033 | Trial primary completion date: Sep 2024 --> Nov 2026
Enrollment closed • Trial completion date • Trial primary completion date
1m
ENSURE-2: Study to Evaluate the Efficacy, Safety and Tolerability of IMU-838 in Patients With Relapsing Multiple Sclerosis (clinicaltrials.gov)
P3, N=1100, Active, not recruiting, Immunic AG | Recruiting --> Active, not recruiting | Trial completion date: Oct 2032 --> Oct 2033 | Trial primary completion date: Oct 2024 --> Nov 2026
Enrollment closed • Trial completion date • Trial primary completion date
1m
"Effect of Vitamin E (α-Tocopherol) on Clinical Activity and Inflammation in Rheumatoid Arthritis" (clinicaltrials.gov)
P2/3, N=46, Recruiting, University of Guadalajara | Not yet recruiting --> Recruiting
Enrollment open
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leflunomide