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DRUG CLASS:

TGF-β RI kinase inhibitor

9d
Single-cell and immune-context integration identifies basement-membrane/metastasis signatures that sharpen bladder-cancer diagnosis and prognosis. (PubMed, Discov Oncol)
The MBRG-based model effectively predicts BLCA prognosis, integrates mechanisms of basement membrane remodeling, EMT, and immune suppression, and identifies DDR2 and SERPINF1 in CAFs as potential targets for personalized therapy.
Journal • IO biomarker
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TMB (Tumor Mutational Burden) • CD8 (cluster of differentiation 8) • DDR2 (Discoidin domain receptor 2) • SLIT2 (Slit Guidance Ligand 2)
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dasatinib • LY2109761 • WNT974
22d
Phase I Study to Assess Safety, Tolerability, PK and PD of AGMB-447 in Healthy Participants and Participants With IPF (clinicaltrials.gov)
P1, N=145, Recruiting, Agomab Spain S.L. | N=107 --> 145 | Trial completion date: Dec 2025 --> Jun 2026 | Trial primary completion date: Dec 2025 --> Jun 2026
Enrollment change • Trial completion date • Trial primary completion date
2ms
Mitochondrial-targeted photodynamic therapy combined with TGF-β inhibition potentiates anti-PD-1 therapy in pancreatic ductal adenocarcinoma. (PubMed, J Nanobiotechnology)
To address these challenges, we develop a liposomal nanodrug that co-encapsulates a mitochondrial-targeted photosensitizer (MP) and a TGF-β receptor inhibitor (LY2109761) to synergize PDT with PD-1 checkpoint blockade...In murine PDAC models, this dual-action strategy transforms the immune-cold TME into an immune-inflamed phenotype, sensitizing tumors to PD-1 therapy and leading to pronounced tumor regression and prolonged survival. Our findings present a promising nanodrug-based approach to remodel the fibrotic and immunosuppressive TME of PDAC and enhance immunotherapeutic outcomes.
Journal
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TGFB1 (Transforming Growth Factor Beta 1)
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LY2109761
2ms
A Multiple Ascending Dose Study With AGMB-129 in Healthy Participants (clinicaltrials.gov)
P1, N=30, Completed, Agomab Spain S.L.U. | Trial completion date: Dec 2025 --> Sep 2025 | Trial primary completion date: Dec 2025 --> Sep 2025 | Recruiting --> Completed
Trial completion • Trial completion date • Trial primary completion date
2ms
Combination of THU/ALK-5i exhibits profound anti-MASH activity through suppression of lipogenesis and fibrogenesis. (PubMed, Sci Rep)
While these findings highlight a synergistic anti-MASH effect of THU and EW-7197, the study is positioned as proof-of-concept. Further validation in metabolically relevant models (e.g., HFD/HFHC) and pharmacokinetic analyses are warranted before clinical translation can be considered.
Journal
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TGFB1 (Transforming Growth Factor Beta 1) • TGFBR1 (Transforming Growth Factor Beta Receptor 1)
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vactosertib (TEW-7197)
3ms
CD44 knockdown and TGF‑β inhibition modulate cell proliferation and invasion in claudin‑low breast cancer cells. (PubMed, Oncol Rep)
CD44 was knocked down in claudin‑low breast cancer cell lines (SUM159 and MDA‑MB‑231), and the TGF‑β receptor (TGFBR) inhibitor LY2109761 (LY‑61) was applied for treatment...Although CD44 depletion may increase EMT‑related signaling, invasion was primarily suppressed by TGF‑β blockade, and the combination with CD44 knockdown further enhanced the inhibition of proliferative phenotypes compared with either treatment alone. This dual‑targeting approach warrants further investigation in claudin‑low breast cancer.
Journal
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CD44 (CD44 Molecule) • CD24 (CD24 Molecule) • TGFB1 (Transforming Growth Factor Beta 1) • ANXA5 (Annexin A5)
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LY2109761
3ms
A Study of LY3200882 in Participants With Solid Tumors (clinicaltrials.gov)
P1, N=223, Active, not recruiting, Eli Lilly and Company | Trial completion date: Aug 2025 --> Aug 2026
Trial completion date
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cisplatin • gemcitabine • albumin-bound paclitaxel • lodapolimab (LY3300054) • LY3200882
4ms
Trial completion
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cisplatin • carboplatin • paclitaxel • Loqtorzi (toripalimab-tpzi) • pemetrexed • GFH018
5ms
LY3200882 and Capecitabine in Advanced Resistant TGF-beta Activated Colorectal Cancer (EORTC1615) (clinicaltrials.gov)
P1/2, N=0, Withdrawn, The Netherlands Cancer Institute | N=31 --> 0 | Unknown status --> Withdrawn
Enrollment change • Trial withdrawal
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TGFB1 (Transforming Growth Factor Beta 1)
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Vectibix (panitumumab) • capecitabine • LY3200882
5ms
A Multiple Ascending Dose Study With AGMB-129 in Healthy Participants (clinicaltrials.gov)
P1, N=40, Recruiting, Agomab Spain S.L. | Not yet recruiting --> Recruiting
Enrollment open
5ms
Role of the TGF-β/SMAD pathway in tumor radioresistance to boron neutron capture therapy (BNCT) in a human cell line of colon adenocarcinoma. (PubMed, Appl Radiat Isot)
The activation of the TGF-β/SMAD pathway and its interaction with the DNA repair via through ATR transductor was demonstrated. LY2109761 could act as a radiosensitizer for BNCT.
Preclinical • Journal
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TGFB1 (Transforming Growth Factor Beta 1) • SMAD7 (SMAD Family Member 7)
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LY2109761
5ms
Unveiling therapeutic potential: In Silico discovery of prognostic markers and potential inhibitors for TGFßR1 in pancreatic cancer. (PubMed, Comput Biol Chem)
These hits exhibited lower free energies (ΔG) as compared to the benchmark inhibitors, Galunisertib and Vactosertib. The results offer valuable insights into the binding mechanism of protein TGFßR1 and its role in the disease, suggesting that targeting the TGF-ß signaling pathway may represent a promising therapeutic strategy.
Journal
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SMAD4 (SMAD family member 4) • TSC2 (TSC complex subunit 2) • AHNAK2 (AHNAK Nucleoprotein 2) • LAMC2 (Laminin subunit gamma 2) • IGFBP3 (Insulin-like growth factor binding protein 3)
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galunisertib (LY2157299) • vactosertib (TEW-7197)