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DRUG CLASS:

DHODH inhibitor

3d
Enrollment closed • Enrollment change
4d
Leflunomide in Patients With PTEN-Altered Advanced Solid Malignancies and HER2 Negative Breast Cancer (clinicaltrials.gov)
P1, N=23, Recruiting, Deborah Doroshow | Trial completion date: Dec 2027 --> Jul 2028
Trial completion date
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PTEN (Phosphatase and tensin homolog)
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ER positive • HER-2 negative • PTEN deletion • PTEN mutation • HER-2 negative + ER positive
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leflunomide
8d
Trial completion • Enrollment change
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leflunomide
9d
Multi-omics analysis identifies stemness-driven molecular subtypes, prognostic signature, epigenetic target APCDD1, and drug candidate Leflunomide in Wilms tumor. (PubMed, Front Oncol)
Mechanistic investigations uncovered that the tumor-suppressive effect of APCDD1 was mediated by promoter hypermethylation, and its expression could be restored by the demethylating agent Decitabine. We further propose Leflunomide as a novel therapeutic strategy for high-risk WT patients. These findings advance our understanding of WT biology and provide actionable insights for risk stratification and targeted intervention.
Journal
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ANXA5 (Annexin A5)
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decitabine • leflunomide
9d
Diselenide-Bridged Iron-Porphyrin MOF for MRI-Guided Radiotherapy via Triple-Pathway Ferroptosis. (PubMed, Int J Nanomedicine)
This system employs a siderophore-based framework PCN(Fe) as the core, loaded with two specific drugs: RAS-selective lethal compound 3 (RSL3) to block the glutathione peroxidase 4 (GPX4) pathway, and brequinar (BQR) to inhibit the dihydroorotate dehydrogenase (DHODH) pathway...PRBP demonstrates favorable T1-weighted magnetic resonance imaging performance, significantly inhibits tumor cell proliferation in vitro, effectively suppresses 4T1 tumor growth in vivo, and exhibits good biosafety. PRBP induces ferroptosis through multiple targets, providing a potent strategy to overcome radiotherapy resistance.
Journal
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GPX4 (Glutathione Peroxidase 4)
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brequinar (DUP 785)
15d
Mapping metabolic reprogramming in lung and breast cancer through integrative bioinformatics. (PubMed, PLoS One)
Integration of pharmacological evidence highlighted clinically actionable interactions between metabolic genes and FDA-approved drugs, including ASNS-asparaginase, DHODH-teriflunomide, and G6PD-rasburicase. This integrative analysis shows that cancer metabolism is altered in subtype-specific ways that can be systematically mapped to reveal potential therapeutic targets. By linking transcriptomic evidence with drug-gene interactions and clinical context, this framework provides a scalable approach for cancer metabolism research and supports the prioritization of pathways with potential translational relevance.
Journal
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BRCA (Breast cancer early onset) • SLC2A1 (Solute Carrier Family 2 Member 1)
17d
Critical role of keratinocytes and protease-activated receptor 2 in secondary lymphedema development. (PubMed, Clin Transl Med)
Activated keratinocytes play a key role in the pathophysiology of secondary lymphedema through PAR2 by producing Th2-inducing cytokines that modulate skin inflammatory responses.
Journal
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TSLP (Thymic Stromal Lymphopoietin)
22d
ELF: The Efficacy of Everolimus With Reduced-dose Tacrolimus Versus Reduced-dose Tacrolimus and Leflunomide in Treatment of BK Virus Infection in Kidney Transplantation Recipient (clinicaltrials.gov)
P=N/A, N=50, Active, not recruiting, King Chulalongkorn Memorial Hospital | Recruiting --> Active, not recruiting | Trial completion date: Jul 2026 --> Jul 2028 | Trial primary completion date: Dec 2025 --> Dec 2027
Enrollment closed • Trial completion date • Trial primary completion date
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everolimus • leflunomide
1m
Progressive alopecia areata during TNF-α inhibition with intralesional corticosteroid failure and subsequent improvement following JAK1 inhibition. (PubMed, J Dermatolog Treat)
To report a case of AA developing during golimumab and leflunomide treatment for seropositive rheumatoid arthritis, with subsequent improvement following initiation of selective Janus kinase 1 (JAK1) inhibition...Upadacitinib was initiated for rheumatoid arthritis management and escalated from 15 mg to 30 mg...Although spontaneous remission and delayed corticosteroid effects cannot be excluded, the timing and magnitude of improvement support a temporal association with JAK1 inhibition. This case highlights a pragmatic therapeutic consideration when alopecia arises during TNF-α inhibitor therapy.
Journal
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JAK1 (Janus Kinase 1)
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Simponi (golimumab) • leflunomide
2ms
Roles of RRM2 and RRM2B in pyrimidine stress responses and differentiation of acute myeloid leukemia cells. (PubMed, Cell Death Discov)
Although brequinar and cytarabine altered nucleotide metabolism through distinct mechanisms, differentiation induced by all agents was abolished by supplementation with high levels of ribo- and deoxyribonucleosides, confirming that nucleotide imbalance is a central driver. Consistent with these differences, RRM2 depletion enhanced differentiation in U937 cells without affecting viability but impaired differentiation and survival in MOLM-13 cells. These findings position nucleotide metabolism as a key regulator of AML differentiation and suggest that combining RNR-targeted and checkpoint-modulating strategies could optimize therapeutic responses.
Journal
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RRM2 (Ribonucleotide Reductase Regulatory Subunit M2)
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TP53 mutation • TP53 wild-type
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cytarabine • brequinar (DUP 785)
2ms
Study on teriflunomide in the treatment of multiple sclerosis (ChiCTR2600120683)
P4, N=100, The Affiliated Hospital of Xuzhou Medical University; The Affiliated Hospital of Xuzhou Medical University
New P4 trial • Real-world evidence
2ms
A Study Evaluating the Safety and Efficacy of AUR108 in Patients With Relapsed Advanced Lymphomas (ASHA-1) (clinicaltrials.gov)
P1, N=40, Recruiting, Aurigene Discovery Technologies Limited | Trial primary completion date: Aug 2025 --> Aug 2027
Trial primary completion date • First-in-human