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DRUG CLASS:

Kinase inhibitor

20d
Lactate metabolism and epigenetic reprogramming drive c-KIT hyperactivation to mediate Gilteritinib resistance: Rationale for c-KIT degraders over kinase inhibitors. (PubMed, Acta Pharm Sin B)
Furthermore, in PDX model established using AML cells from Gilteritinib-resistant patients, the degrader showed significantly superior therapeutic efficacy compared to the combination treatment of Gilteritinib and Imatinib. As a candidate drug molecule, this degrader exhibits promising potential for clinical translation.
Journal
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FLT3 (Fms-related tyrosine kinase 3) • KIT (KIT proto-oncogene, receptor tyrosine kinase)
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KIT expression
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imatinib • Xospata (gilteritinib)
20d
Src Family Kinase Inhibitors Bosutinib and Dasatinib Enhance ATRA-induced Differentiation of NB4 Leukemia Cells. (PubMed, Anticancer Res)
Clinically available SFK inhibitors, particularly dasatinib, synergistically enhance ATRA-induced myeloid differentiation of NB4 APL cells and are more effective than the conventional ATRA plus ATO combination in this in vitro model. These findings support further preclinical and clinical evaluation of SFK inhibitor plus ATRA combinations as differentiation-oriented strategies and potential alternatives or complements to ATO-containing regimens in APL.
Journal
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ITGAM (Integrin, alpha M)
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dasatinib • bosutinib • arsenic trioxide
21d
Randomized Trial of Topotecan With M6620, an ATR Kinase Inhibitor, in Small Cell Lung Cancers and Small Cell Cancers Outside of the Lungs (clinicaltrials.gov)
P2, N=104, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Jun 2026 --> May 2027
Trial completion date
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berzosertib (M6620) • topotecan
1m
MISTIK: Microsampling Approach for Monitoring of Kinase Inhibitor Targeted Therapies (clinicaltrials.gov)
P=N/A, N=160, Completed, Rennes University Hospital | Recruiting --> Completed | N=360 --> 160
Trial completion • Enrollment change
2ms
Kinase inhibition rewires the HLA-I immunopeptidome in chronic myeloid leukemia. (PubMed, iScience)
Comparing benign hematologic tissues with CML samples revealed about 90 CML-specific peptides that became more prominent after SFK or JNK inhibition. Overall, this work provides a quantitative, multi-omic framework to rationally combine kinase inhibitors with immunotherapy to boost antigen visibility and antileukemic immunity.
Journal
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
2ms
FAK Inhibitor in Patients With Advanced Solid Tumors (clinicaltrials.gov)
P1, N=75, Not yet recruiting, InxMed (Shanghai) Co., Ltd.
New P1 trial
2ms
ABL/JAK Inhibitors With Chemotherapy and Venetoclax for Ph-like ALL (clinicaltrials.gov)
P=N/A, N=92, Recruiting, Institute of Hematology & Blood Diseases Hospital, China | Not yet recruiting --> Recruiting | N=30 --> 92
Enrollment open • Enrollment change • IO biomarker
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ABL2 (ABL Proto-Oncogene 2, Non-Receptor Tyrosine Kinase)
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Venclexta (venetoclax) • cytarabine • Jakafi (ruxolitinib) • cyclophosphamide • Blincyto (blinatumomab) • Nailike (olverembatinib) • fludarabine IV
3ms
LUNG-RESIST: Understanding and Overcoming the Early Adaptive Resistance to EGFR Tyrosine-kinase Inhibitors in Lung Cancer Patients (clinicaltrials.gov)
P=N/A, N=80, Active, not recruiting, University Hospital, Toulouse | Recruiting --> Active, not recruiting
Enrollment closed
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EGFR (Epidermal growth factor receptor)
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EGFR mutation
3ms
OMX-0407-101: A Study of OMX-0407 in Patients With Previously Treated Solid Tumours That Can't be Removed Surgically (clinicaltrials.gov)
P1/2, N=68, Terminated, iOmx Therapeutics AG | N=188 --> 68 | Active, not recruiting --> Terminated; Study terminated as part of strategic considerations and not based on safety concerns.
Enrollment change • Trial termination
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OMX-0407
3ms
TQB3616-I-0001: A Phase I Study of TQB3616 on Tolerance and Pharmacokinetics (clinicaltrials.gov)
P1, N=40, Completed, Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Unknown status --> Completed | N=30 --> 40
Trial completion • Enrollment change
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
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Saitanxin (culmerciclib)
3ms
RewinD-LB - Clinical Study of Neflamapimod in Patients With Dementia With Lewy Bodies (clinicaltrials.gov)
P2, N=159, Completed, EIP Pharma Inc | Trial primary completion date: Oct 2024 --> May 2025
Trial primary completion date
4ms
CDDO-Me alleviates doxorubicin/lapatinib-induced cardiotoxicity by activating the NRF2/GPX4 axis to inhibit oxidative stress and ferroptosis. (PubMed, Free Radic Biol Med)
Furthermore, CDDO-Me did not compromise the antitumor efficacy of DOX/LAP in breast cancer cells. CDDO-Me protects against DOX/LAP-induced cardiotoxicity by stabilizing GPX4 and inhibiting ferroptosis, offering a promising therapeutic strategy that preserves cardiac function without interfering with chemotherapy.
Journal
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GPX4 (Glutathione Peroxidase 4)
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lapatinib • doxorubicin hydrochloride