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DRUG:

Nailike (olverembatinib)

i
Other names: HQP1351, APG-1351, APG 1351, HQP1351, GZD824, D824, IBI-348, APG1351, D 824, GZD 824, HQP 1351, IBI 348, D-824, GZD-824, HQP-1351, IBI348
Company:
Ascentage Pharma, Innovent Biologics, Takeda
Drug class:
Bcr-abl inhibitor
4d
Observational Study on Dose Optimization of Olverembatinib in Patients with Chronic Myeloid Leukemia in Chronic or Accelerated Phase (ChiCTR2500115245)
P=N/A, N=100, Not yet recruiting, Peking University People's Hospital; Peking University People's Hospital
New trial
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ABL1 (ABL proto-oncogene 1)
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Nailike (olverembatinib)
4d
VOP regimen for the treatment of adult de novo Ph+ B/myeloid mixed phenotype acute leukemia (ChiCTR2500112802)
P2, N=10, Not yet recruiting, The First Affiliated Hospital, College of Medicine, Zhejiang University; The First Affiliated Hospital, College of Medicine, Zhejiang University
New P2 trial
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Venclexta (venetoclax) • Nailike (olverembatinib)
7d
Advances in Targeting BCR-ABLT315I Mutation with Imatinib Derivatives and Hybrid Anti-Leukemic Molecules. (PubMed, Molecules)
Combination strategies, such as vorinostat with ponatinib, provide complementary therapeutic avenues...Hybrid molecules derived from approved TKIs, including GNF-7, olverembatinib, and HG-7-85-01, exemplify rational design trends that balance efficacy with improved safety. Molecular modeling continues to deepen understanding of ligand engagement within the T315I-mutated active site, supporting the development of next-generation inhibitors. In this review, we summarized recent progress in the design, optimization, and biological evaluation of small molecules targeting the BCR-ABLT315I mutation.
Review • Journal
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
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imatinib • Iclusig (ponatinib) • Zolinza (vorinostat) • Nailike (olverembatinib)
20d
Phase II Study Assessing the Efficacy and Toxicity of Olverembatinib Monotherapy in Patients With Newly Diagnosed Chronic Myeloid Leukemia in Chronic Phase (clinicaltrials.gov)
P2, N=50, Recruiting, M.D. Anderson Cancer Center | Initiation date: Jul 2026 --> Oct 2025 | Not yet recruiting --> Recruiting
Enrollment open • Trial initiation date
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ABL1 (ABL proto-oncogene 1)
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Nailike (olverembatinib)
1m
Pharmacokinetics of Olverembatinib in Participants With Hepatic Impairment (clinicaltrials.gov)
P1, N=48, Recruiting, Ascentage Pharma Group Inc. | Not yet recruiting --> Recruiting
Enrollment open
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Nailike (olverembatinib)
2ms
New P1 trial
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Nailike (olverembatinib)
2ms
Overcoming Multidrug Resistance in Cancer Cells Targeting ABC Transporter ABCB1 with Tyrosine Kinase Inhibitor: Olverembatinib. (PubMed, Exp Cell Res)
Non-cytotoxic concentrations of olverembatinib significantly increased the sensitivity of ABCB1-overexpressing cells to paclitaxel and vincristine. Additionally, olverembatinib activated the ATPase activity of ABCB1 in a concentration-dependent manner and exhibited potent binding affinity to ABCB1 in docking simulations. These findings suggest that olverembatinib holds promise as a potent reversal agent for MDR, paving the way for its integration into novel combination chemotherapy regimens to improve cancer treatment outcomes.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1)
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paclitaxel • vincristine • Nailike (olverembatinib)
2ms
Olverembatinib for 8p11 myeloproliferative syndrome with a positive BCR-FGFR1 fusion gene: a case report. (PubMed, Ann Hematol)
The treatment safety of the entire process was excellent. In summary, olverembatinib provides more treatment options for rare diseases such as 8p11 myeloproliferative syndrome.
Journal
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BCR (BCR Activator Of RhoGEF And GTPase) • FGFR1 (Fibroblast growth factor receptor 1)
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Nailike (olverembatinib)
3ms
Case Report: Dual resistance to dasatinib/olverembatinib in accelerated-phase cml: identification of a novel SPECC1L-inserted e8a2 BCR::ABL1 transcript and ABL1 V379I mutation. (PubMed, Front Oncol)
She ultimately achieved Major Molecular Response (MMR) after haploidentical hematopoietic stem-cell transplantation (haplo-HSCT). This case highlights the importance of comprehensive molecular profiling at diagnosis and the need to develop alternative therapeutic strategies for rare BCR::ABL1 variants.
Journal
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ABL1 (ABL proto-oncogene 1) • SPECC1L (Sperm Antigen With Calponin Homology And Coiled-Coil Domains 1 Like)
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ABL1 fusion
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dasatinib • Nailike (olverembatinib)
3ms
Efficacy, safety and predictive biomarker of third-generation tyrosine kinase inhibitors with azacitidine in myeloid blast phase of chronic myeloid leukemia. (PubMed, Cancer)
3G-TKI with azacitidine is an effective and safe therapy providing more chance to receive a transplantation for CML in myeloid blast phase. Potential biomarkers associated with outcomes were identified.
Journal
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KRAS (KRAS proto-oncogene GTPase) • ABL1 (ABL proto-oncogene 1) • PTPN11 (Protein Tyrosine Phosphatase Non-Receptor Type 11)
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KRAS mutation
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Iclusig (ponatinib) • azacitidine • Nailike (olverembatinib)
3ms
HQP1351CU101: Study of HQP1351 in Subjects With Refractory CML and Ph+ ALL (clinicaltrials.gov)
P1, N=242, Recruiting, Ascentage Pharma Group Inc. | N=62 --> 242 | Trial completion date: Jan 2024 --> Mar 2030 | Trial primary completion date: Jan 2024 --> Dec 2029
Enrollment change • Trial completion date • Trial primary completion date
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
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ABL1 T315I
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Blincyto (blinatumomab) • Nailike (olverembatinib)
3ms
Olverembatinib, a multikinase inhibitor that modulates lipid metabolism, in advanced succinate dehydrogenase-deficient gastrointestinal stromal tumors: a phase 1b study and translational research. (PubMed, Signal Transduct Target Ther)
Succinate dehydrogenase (SDH)-deficient gastrointestinal stromal tumors (GISTs) are generally resistant to targeted therapy with tyrosine kinase inhibitors (TKIs), such as imatinib, and there are no standard therapeutic options for advanced SDH-deficient GISTs. As a putative mechanism of action, translational research revealed significant lipid enrichment with the overexpression of lipid uptake-related genes and proteins, including CD36, fatty acid binding proteins, fatty acid transport proteins, and lipid metabolites, in SDH-deficient GIST patients, and olverembatinib suppressed lipid uptake and CD36 expression in GIST cells. Olverembatinib also exerts antitumor effects by inhibiting tumorigenic signaling pathways associated with hypoxia, angiogenesis, proliferation, and survival.
P1 data • Journal
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CD36 (thrombospondin receptor)
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imatinib • Nailike (olverembatinib)