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3d
New P1/2 trial
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PD-L1 (Programmed death ligand 1) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog) • AKT1 (V-akt murine thymoma viral oncogene homolog 1) • CTLA4 (Cytotoxic T-Lymphocyte Associated Protein 4) • CD4 (CD4 Molecule)
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EGFR mutation • PIK3CA mutation • EGFR L858R • EGFR exon 19 deletion • PTEN mutation • AKT1 mutation
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Tagrisso (osimertinib) • Truqap (capivasertib) • simmitinib (SYHA1817)
4d
MICALL2 promotes angiogenesis of colorectal cancer by regulating the EGFR/PI3K/AKT/KLF5/VEGFA axis. (PubMed, Biochem Pharmacol)
Pharmacological inhibition of PI3K via LY294002 reversed MICALL2-induced angiogenesis. Therefore, MICALL2 facilitates CRC angiogenesis through the EGFR/PI3K/AKT/KLF5/VEGFA axis and may serve as a promising target for anti-angiogenic therapy.
Journal
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EGFR (Epidermal growth factor receptor)
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LY294002
5d
A Study to Investigate the Effect of Capivasertib on the Pharmacokinetics of Oral Rosuvastatin in Healthy Participants (clinicaltrials.gov)
P1, N=18, Recruiting, AstraZeneca | Trial completion date: Sep 2025 --> Mar 2026 | Trial primary completion date: Sep 2025 --> Mar 2026
Trial completion date • Trial primary completion date
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Truqap (capivasertib)
5d
Phase II Randomized Study of MK-2206 and Bicalutamide in Prostate Cancer Patients With Rising PSA After Primary Therapy (ECOG-ACRIN E2809). (PubMed, Prostate)
The results suggest that latent improved outcome of high-risk BCR patients (mean PSA doubling time 4.4 months) on combined MK-2206+Bic versus Bic alone was attributable to a subgroup identified by crosstalk AR activation secondary to inhibition of AKT. Toxicity may affect tolerance of sustained AKT-AR inhibition.
P2 data • Journal
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AR (Androgen receptor)
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MK-2206 • bicalutamide
5d
Overexpression of IL7R Attenuates Cerebral Ischemia-Reperfusion Injury by Inhibiting Apoptosis. (PubMed, J Integr Neurosci)
Overexpression of IL7R was shown to alleviate CIRI by suppressing apoptosis. These findings indicate IL7R as a novel target for IS treatment.
Journal • IO biomarker
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IL7R (Interleukin 7 Receptor) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • IL7 (Interleukin 7)
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LY294002
8d
A Study of ONC201 for Refractory Meningioma (clinicaltrials.gov)
P2, N=0, Withdrawn, University of Nebraska | N=27 --> 0 | Suspended --> Withdrawn | Trial primary completion date: Apr 2026 --> Apr 2027
Enrollment change • Trial withdrawal • Trial primary completion date
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Modeyso (dordaviprone)
9d
Investigating vimseltinib in tenosynovial giant cell tumors. (PubMed, Expert Opin Pharmacother)
Furthermore, there is an absence of severe toxicities that have arisen with other agents in the TGCT treatment space, specifically liver failure. Vimseltinib is a favorable option for patients with TGCTs and further efforts to determine its place in the sequence of overall management are needed.
Review • Journal
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CSF1R (Colony stimulating factor 1 receptor)
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Turalio (pexidartinib) • Romvimza (vimseltinib)
11d
ONC201 and Atezolizumab in Obesity-Driven Endometrial Cancer (clinicaltrials.gov)
P1, N=58, Recruiting, UNC Lineberger Comprehensive Cancer Center | Trial completion date: Jul 2026 --> Jul 2028 | Trial primary completion date: Feb 2026 --> Feb 2028
Trial completion date • Trial primary completion date
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Tecentriq (atezolizumab) • Modeyso (dordaviprone)
11d
High Risk of Drug-Drug Interactions Caused by Pexidartinib via UDP-Glucuronosyltransferases Inhibition. (PubMed, Chem Res Toxicol)
The results of in vitro-in vivo extrapolation (IVIVE) indicated that coadministration of pexidartinib at a clinically approved dose (400 mg twice daily) with the drugs primarily cleared by UGT1A1, UGT1A6, UGT1A7, UGT1A9, and UGT2B15 would result in a higher risk of DDI. In summary, our results provide useful information for the mechanism underlying pexidartinib-induced hepatotoxicity and clinical safe medication of pexidartinib.
Journal
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UGT1A9 (UDP Glucuronosyltransferase Family 1 Member A9) • UGT1A6 (UDP Glucuronosyltransferase Family 1 Member A6) • UGT1A7 (UDP Glucuronosyltransferase Family 1 Member A7) • UGT2B15 (UDP Glucuronosyltransferase Family 2 Member B15)
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Turalio (pexidartinib)
11d
Kupffer cell M2-like polarization increases liver metastatic burden via the uptake of exosomal KRAS mutant protein from hypoxic colorectal carcinoma cells. (PubMed, RSC Med Chem)
In vitro model HMDMs were used to explore polarization phenotype and therapeutic effects of GSK690693 (AKT inhibitor) inhibited AKT... our findings reveal that exosomal mutant KRAS drives Kupffer cell M2-like polarization via the hyperactivation of AKT signaling, establishing this axis as a key mediator of colorectal cancer liver metastasis. Pharmacological inhibition of AKT effectively disrupts this immunosuppressive reprogramming, proposing targeted AKT blockade as a promising strategy to intercept the metastatic niche in CRC patients.
Journal
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KRAS (KRAS proto-oncogene GTPase)
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KRAS mutation
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GSK690693
11d
Dordaviprone/ONC201 Activation of the ClpP Mitochondrial Protease Inhibits the Growth of KRAS-Mutant Pancreatic Cancer and Overcomes RAS Inhibitor Resistance. (PubMed, bioRxiv)
We propose that concurrent treatment with ONC201 may delay onset of resistance to RAS inhibitor therapy. ClpP activation by dordaviprone/ONC201 suppressed PDAC cell growth and overcame resistance to the RAS(ON) multi-selective inhibitor RMC-7977, providing support for investigating this combination as a potential combination treatment for KRAS-mutant pancreatic cancer.
Journal
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KRAS (KRAS proto-oncogene GTPase) • KEAP1 (Kelch Like ECH Associated Protein 1)
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KRAS mutation
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Modeyso (dordaviprone) • RMC-7977
12d
GDC-0084 in Combination With Trastuzumab for Patients With HER2-Positive Breast Cancer Brain Metastases (clinicaltrials.gov)
P2, N=17, Terminated, Dana-Farber Cancer Institute | N=47 --> 17 | Active, not recruiting --> Terminated; participants are no longer being examined or receiving intervention
Enrollment change • Trial termination
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HER-2 (Human epidermal growth factor receptor 2) • EIF4EBP1 (Eukaryotic translation initiation factor 4E binding protein 1)
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HER-2 positive • HER-2 overexpression • HER-2 amplification • HER-2 positive + HER-2 overexpression
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Herceptin (trastuzumab) • paxalisib (GDC-0084)