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DRUG CLASS:

TGF-β1 inhibitor

6d
Selective blockade of latent TGF-β1 activation suppresses tissue fibrosis with good safety. (PubMed, Commun Med (Lond))
Selective blockade of latent TGF-β1 activation represents a promising approach for treating a broad range of fibrotic diseases and cancers. By specifically targeting TGF-β1, SOF10 may offer a safer and more effective therapeutic option compared to non-selective TGF-β inhibitors. This strategy has the potential to transform the treatment paradigm for fibrosis-related conditions.
Journal • PD(L)-1 Biomarker • IO biomarker
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TGFB1 (Transforming Growth Factor Beta 1)
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RG6440
13d
Identification of siRNA silencing TGFβ1 and VEGFR2 and utility of the combination in targeting immune modulation and angiogenesis in treating melanoma in vivo. (PubMed, NAR Cancer)
STP355 also reduced tumor weight significantly, without the toxicity observed with cisplatin, resulting in prolonged survival of mice compared with this small molecule. It increased immune cell penetration into TME and reduced metastases to the lung. STP355 was more efficacious than, and somewhat additive with, immune checkpoint inhibitory monoclonal antibodies.
Preclinical • Journal • IO biomarker
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KDR (Kinase insert domain receptor) • TGFB1 (Transforming Growth Factor Beta 1)
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cisplatin
14d
Enrollment closed • Enrollment change • Adverse events
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ALK (Anaplastic lymphoma kinase)
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ALK mutation
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Keytruda (pembrolizumab) • cisplatin • carboplatin • pemetrexed • budigalimab (ABBV-181) • livmoniplimab (ABBV-151)
19d
Gemogenovatucel-T Advantage in Clonal Tumor Mutation Burden-High Ovarian Cancer. (PubMed, JCO Precis Oncol)
These results demonstrate OS advantage for maintenance treatment of adult females with newly diagnosed, advanced stage IIIb-IV ovarian cancer with HRP status and cTMB-H profile who are in complete response after debulking surgery and frontline platinum-based doublet chemotherapy.
Clinical • Journal • Tumor mutational burden • PD(L)-1 Biomarker • IO biomarker
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TMB (Tumor Mutational Burden)
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TMB-H
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Avastin (bevacizumab) • Vigil (gemogenovatucel-T)
21d
Linavonkibart and pembrolizumab in immune checkpoint blockade-resistant advanced solid tumors: a phase 1 trial. (PubMed, Nat Med)
Biomarker data provide proof of mechanism and a potential ccRCC patient selection strategy. ClinicalTrials.gov identifier: NCT04291079 .
P1 data • Journal • Checkpoint inhibition • PD(L)-1 Biomarker • IO biomarker
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TGFB1 (Transforming Growth Factor Beta 1)
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Keytruda (pembrolizumab) • linavonkibart (SRK-181)
25d
Tranilast Does Not Inhibit TRPV2. (PubMed, Cells)
Instead, tranilast seems to indirectly suppress channel activation by reducing reactive oxygen species (ROS). This refined understanding of how tranilast modulates TRPV2 has important implications for the interpretation of prior and future pharmacological studies targeting TRPV2.
Journal
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TRPA1 (Transient Receptor Potential Cation Channel Subfamily A Member 1) • TRPV2 (Transient Receptor Potential Cation Channel Subfamily V Member 2)
29d
PSMD14 drives lung adenocarcinoma progression through HMMR stabilization and dual activation of TGF-β/Smad and PI3K/AKT/mTOR signaling. (PubMed, Front Immunol)
The PSMD14 inhibitor Capzimin exhibited potent anti-tumor effects in vitro and in vivo, and combination therapy with the TGF-β inhibitor galunisertib demonstrated enhanced efficacy...Consequently, the PSMD14-HMMR axis emerges as a promising therapeutic target. Inhibition of PSMD14 exhibited significant anti-tumor efficacy, underscoring its potential for clinical translation in LUAD treatment.
Journal
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TGFB1 (Transforming Growth Factor Beta 1) • HMMR (Hyaluronan Mediated Motility Receptor) • PSMD14 (Proteasome 26S Subunit, Non-ATPase 14)
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galunisertib (LY2157299)
1m
TGF-βRII/IL-15 immunotherapeutic complex targets exhausted CD8+ T-cell subsets in lymph nodes and tumors. (PubMed, J Immunother Cancer)
Our findings demonstrate that combination therapy targeting immune cells critical for antitumor responses and blocking immune-suppressive environment significantly improves antitumor therapeutic efficacy. These findings provide a strong basis for using HCW9218 to enhance the efficacy of ICIs against solid tumors in the clinical setting.
Journal
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CD8 (cluster of differentiation 8) • TGFB1 (Transforming Growth Factor Beta 1) • IL15 (Interleukin 15)
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HCW9218
1m
Study of TGF-β Receptor Inhibitor Galunisertib (LY2157299) and Enzalutamide in Metastatic Castration-resistant Prostate Cancer (clinicaltrials.gov)
P2, N=60, Active, not recruiting, Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins | Trial completion date: May 2026 --> Dec 2026
Trial completion date
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Xtandi (enzalutamide) • galunisertib (LY2157299)
2ms
Targeting hepatocytic TβRI ameliorates liver metastatic outcomes by revitalizing stem-like CD8+ Tex subsets. (PubMed, Nat Commun)
Furthermore, therapeutic delivery of Galunisertib using choline-modified lipid nanoparticles synergizes with αPD-1, fostering the conversion of exhausted CD8⁺ T cells into responsive Ly108⁺CX3CR1⁺ subsets and suppressing liver metastases. Collectively, our results identify hepatocyte TGFβ signaling as a targetable checkpoint against liver metastases.
Journal • PD(L)-1 Biomarker • IO biomarker
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CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule) • CX3CR1 (C-X3-C Motif Chemokine Receptor 1) • LGALS9 (Galectin 9)
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galunisertib (LY2157299)
2ms
HCW9218 for Advanced Pancreatic Cancer (clinicaltrials.gov)
P1/2, N=21, Completed, ImmunityBio, Inc. | Active, not recruiting --> Completed | N=60 --> 21
Trial completion • Enrollment change
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HCW9218
2ms
MIST: A Study Evaluating the Safety and Efficacy of Inhaled AP01 in Participants With Progressive Pulmonary Fibrosis (clinicaltrials.gov)
P2, N=375, Recruiting, Avalyn Pharma Inc. | Trial completion date: Apr 2026 --> Jun 2027 | Trial primary completion date: Apr 2026 --> Jun 2027
Trial completion date • Trial primary completion date