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DRUG:

IK-930

i
Other names: IK-930
Company:
Ikena Oncology
Drug class:
TEAD1 inhibitor
Related drugs:
1m
Oral TEAD Inhibitor Targeting the Hippo Pathway in Subjects with Advanced Solid Tumors (clinicaltrials.gov)
P1, N=67, Terminated, Ikena Oncology | N=198 --> 67 | Trial completion date: Jun 2025 --> Sep 2024 | Active, not recruiting --> Terminated | Trial primary completion date: Jun 2025 --> Aug 2024; Sponsor strategic reasons
Enrollment change • Trial completion date • Trial termination • Trial primary completion date • Metastases
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YAP1 (Yes associated protein 1) • TFE3 (Transcription Factor Binding To IGHM Enhancer 3) • CAMTA1 (Calmodulin Binding Transcription Activator 1) • TAFAZZIN (Tafazzin)
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TFE3 fusion
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Tagrisso (osimertinib) • IK-930
6ms
Oral TEAD Inhibitor Targeting the Hippo Pathway in Subjects With Advanced Solid Tumors (clinicaltrials.gov)
P1, N=198, Active, not recruiting, Ikena Oncology | Recruiting --> Active, not recruiting
Enrollment closed • Metastases
|
YAP1 (Yes associated protein 1) • TFE3 (Transcription Factor Binding To IGHM Enhancer 3) • CAMTA1 (Calmodulin Binding Transcription Activator 1) • TAFAZZIN (Tafazzin)
|
Tagrisso (osimertinib) • IK-930
6ms
Advances in Targeted Therapy for Malignant Pleural Mesothelioma (PubMed, Zhongguo Fei Ai Za Zhi)
At present, it has been found the following types of targets: gene mutation targets such as BRCA associated protein 1 (BAP1) and cyclin-dependent kinase 2A (CDKN2A); epigenetic targets such as lysine (K)-specific demethylase 4A (KDM4A) and lysine-specific demethylase 1 (LSD1), and signal protein targets such as glucose-regulated protein 78 (GRP78) and signal transducer and activator of transcription 3 (STAT3). So far, available clinical trials include phase II clinical trials of histone methyltransferase inhibitor Tazemetostat, poly (ADP-ribose) polymerase (PARP) inhibitor Rucaparib and cyclin-dependent kinases 4 and 6 (CDK4/6) inhibitor Abemaciclib, as well as phase I clinical trials of mesothelin-targeting chimeric antigen receptor T-cell immunotherapy (CAR-T) cell injection in the thoracic cavity and TEA domain family member (TEAD) inhibitor VT3989 and IK-930, and the results of these trials have showed certain clinical efficacy..
Review • Journal • BRCA Biomarker • PARP Biomarker • IO biomarker
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CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • BAP1 (BRCA1 Associated Protein 1) • MSLN (Mesothelin) • BRCA (Breast cancer early onset) • STAT3 (Signal Transducer And Activator Of Transcription 3) • HSPA5 (Heat Shock Protein Family A (Hsp70) Member 5) • KDM4A (Lysine Demethylase 4A)
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Verzenio (abemaciclib) • Rubraca (rucaparib) • Tazverik (tazemetostat) • IK-930 • VT3989
8ms
Oral TEAD Inhibitor Targeting the Hippo Pathway in Subjects With Advanced Solid Tumors (clinicaltrials.gov)
P1, N=198, Recruiting, Ikena Oncology | Trial completion date: Oct 2024 --> Jun 2025 | Trial primary completion date: Oct 2024 --> Jun 2025
Trial completion date • Trial primary completion date • Metastases
|
YAP1 (Yes associated protein 1) • TFE3 (Transcription Factor Binding To IGHM Enhancer 3) • CAMTA1 (Calmodulin Binding Transcription Activator 1) • TAFAZZIN (Tafazzin)
|
TFE3 fusion
|
Tagrisso (osimertinib) • IK-930
almost2years
TY-0584: A potent, orally available small molecule YAP/TEAD inhibitor, exhibits anti-tumor effects in vitro and in vivo (AACR 2023)
Therefore, small molecules that target palmitoylation of TEAD have been explored and VT3989 (NCT04665206) and IK-930 (NCT05228015) have success to enter the clinical trials...In line with the results of the in-vitro experiments, another YAP/TEAD inhibitor TY-0536 in combination with TY-9591 significantly delay the tumor regrowth in the PC9 CDX mouse model...[Shengli Dong and Apeng Liang contributed equally to this work. Jun Li, Shengli Dong, and Apeng Liang are the corresponding authors.]
Preclinical
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NF2 (Neurofibromin 2)
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NF2 deletion
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IK-930 • TY-0584 • VT3989 • asandeutertinib (TY-9591)
almost3years
New P1 trial
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YAP1 (Yes associated protein 1) • TFE3 (Transcription Factor Binding To IGHM Enhancer 3)
|
TFE3 fusion
|
IK-930