^
Contact us to learn more about
our Premium Content: News alerts, weekly reports and conference plannersBIOMARKER:
BCR-ABL1 Q252H
i
Other names: BCR, BCR Activator Of RhoGEF And GTPase, BCR, RhoGEF And GTPase Activating Protein, Breakpoint Cluster Region Protein, Renal Carcinoma Antigen NY-REN-26, Breakpoint Cluster Region, D22S11, BCR1, BCR/FGFR1 Chimera Protein, FGFR1/BCR Chimera Protein, D22S662, ALL, CML, PHL, ABL proto-oncogene 1, ABL, c-ABL, JTK7, p150, ABL1
Contact us to learn more about our Premium Content:
News alerts, weekly reports and conference planners
6ms
Tgrx-678, a Novel Allosteric Inhibitor of BCR-ABL1, Demonstrates Preclinical Anti-Leukemia Activity, High Oral Bioavailability and Synergism with Ponatinib to Suppress the Highly Resistant Compound Mutations (ASH 2023)
ABL1 is subject to auto-inhibition mediated by myristoylation-triggered conformational change, which can be exploited to overcome resistance, as validated by allosteric inhibitors such as GNF2, GNF5 and asciminib. Furthermore, TGRX-678 and ponatinib synergize to overcome the clinically challenging resistance conferred by T315M or T315I-inclusive compound mutations. This data warrant further clinical investigation of TGRX-678 for the treatment of resistant or refractory CML patients.
Preclinical
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
|
BCR-ABL1 T315I • BCR-ABL1 E255K • BCR-ABL1 Y253H • BCR-ABL1 E255V • BCR-ABL1 G250E • ABL1 T315I • BCR-ABL1 Q252H • ABL1 E255K • ABL1 G250E • ABL1 Y253H • BCR-ABL1 T315M • BCR-ABL1 Y253H + BCR-ABL1 T315I
|
Iclusig (ponatinib) • Scemblix (asciminib) • TGRX-678
9ms
Adding Ruxolitinib to a Combination of Dasatinib Plus Dexamethasone in Remission Induction Therapy in Newly Diagnosed Philadelphia Chromosome-Positive Acute Lymphoblastic Leukemia Patients Aged 40 Years or Older (clinicaltrials.gov)
P1, N=12, Active, not recruiting, Memorial Sloan Kettering Cancer Center | Trial completion date: Jun 2023 --> Jun 2025 | Trial primary completion date: Jun 2023 --> Jun 2025
Trial completion date • Trial primary completion date
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase) • PDGFRB (Platelet Derived Growth Factor Receptor Beta) • CRLF2 (Cytokine Receptor Like Factor 2) • JAK3 (Janus Kinase 3) • CSF1R (Colony stimulating factor 1 receptor) • TSLP (Thymic Stromal Lymphopoietin)
|
BCR-ABL1 E255K • BCR-ABL1 V299L • BCR-ABL1 F317L • ABL1 T315I • BCR-ABL1 L248V • BCR-ABL1 Q252H • BCR-ABL1 F317V • JAK3 mutation • ABL1 E255K • BCR-ABL1 F317C • BCR-ABL1 T315A • ABL1 F317L • BCR-ABL1 L248R
|
dasatinib • Jakafi (ruxolitinib) • dexamethasone
over2years
Adding Ruxolitinib to a Combination of Dasatinib Plus Dexamethasone in Remission Induction Therapy in Newly Diagnosed Philadelphia Chromosome-Positive Acute Lymphoblastic Leukemia Patients Aged 40 Years or Older (clinicaltrials.gov)
P1, N=12, Active, not recruiting, Memorial Sloan Kettering Cancer Center | Trial completion date: Jun 2021 --> Jun 2023 | Trial primary completion date: Jun 2021 --> Jun 2023
Clinical • Trial completion date • Trial primary completion date
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase) • PDGFRB (Platelet Derived Growth Factor Receptor Beta) • CRLF2 (Cytokine Receptor Like Factor 2) • JAK3 (Janus Kinase 3) • CSF1R (Colony stimulating factor 1 receptor) • TSLP (Thymic Stromal Lymphopoietin)
|
BCR-ABL1 E255K • BCR-ABL1 V299L • BCR-ABL1 F317L • ABL1 T315I • BCR-ABL1 L248V • BCR-ABL1 Q252H • BCR-ABL1 F317V • JAK3 mutation • ABL1 E255K • BCR-ABL1 F317C • BCR-ABL1 T315A • ABL1 F317L • BCR-ABL1 L248R
|
dasatinib • Jakafi (ruxolitinib) • dexamethasone
over3years
FINESTdm: Evaluating Efficacy and Safety of Flumatinib Versus Nilotinib for Chronic Phase Chronic Myeloid Leukemia(CML-CP) Without Optimal Response (Warning,Failure) to Imatinib or Dasatinib (clinicaltrials.gov)
P, N=200, Recruiting, Wuhan Union Hospital, China
Clinical • New trial
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
|
BCR-ABL1 V299L • BCR-ABL1 F317L • BCR-ABL1 M244V • BCR-ABL1 M351T • BCR-ABL1 H396R • BCR-ABL1 Q252H • BCR-ABL1 mutation • BCR-ABL1 E355G • BCR-ABL1 L387M • ABL1 F317L • ABL1 L387M • ABL1 M351T
|
dasatinib • imatinib • Tasigna (nilotinib) • Hansoh Xinfu (flumatinib)
over3years
[VIRTUAL] Clonal Hematopoiesis with Somatic Mutations in „AYA“ Generation of Patients with Chronic Myeloid Leukemia (ASH 2020)
In patient #6, G645delinsGWfs was found at the diagnosis and on the 3rd line nilotinib treatment...In patient #3, the CSF3R mutation A593V was found at diagnosis and confirmed 14 months after the imatinib initiation...Despite the clonal hematopoiesis with somatic mutations is considered as age-related phenomenon, in AYA CML patients, it may represent a critical problem in achieving sustained molecular response on solo TKI therapy, or even worse, it may result in higher risk of therapy failure and disease progression. Supported by MZCR 00023736
Clinical
|
ABL1 (ABL proto-oncogene 1) • RUNX1 (RUNX Family Transcription Factor 1) • ASXL1 (ASXL Transcriptional Regulator 1) • TET2 (Tet Methylcytosine Dioxygenase 2) • ATRX (ATRX Chromatin Remodeler) • CSF3R (Colony Stimulating Factor 3 Receptor) • SIRT1 (Sirtuin 1)
|
BCR-ABL1 T315I • ASXL1 mutation • BCR-ABL1 E255K • BCR-ABL1 F317L • BCR-ABL1 M244V • ABL1 T315I • BCR-ABL1 M351T • BCR-ABL1 Q252H • BCR-ABL1 V379I • ABL1 E255K • ABL1 F317L • ABL1 M351T
|
imatinib • Tasigna (nilotinib)
4years
Adding Ruxolitinib to a Combination of Dasatinib Plus Dexamethasone in Remission Induction Therapy in Newly Diagnosed Philadelphia Chromosome-Positive Acute Lymphoblastic Leukemia Patients Aged 40 Years or Older (clinicaltrials.gov)
P1, N=12, Active, not recruiting, Memorial Sloan Kettering Cancer Center | Trial completion date: Jun 2020 --> Jun 2021 | Trial primary completion date: Jun 2020 --> Jun 2021
Clinical • Trial completion date • Trial primary completion date
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase) • PDGFRB (Platelet Derived Growth Factor Receptor Beta) • CRLF2 (Cytokine Receptor Like Factor 2) • JAK3 (Janus Kinase 3) • CSF1R (Colony stimulating factor 1 receptor) • TSLP (Thymic Stromal Lymphopoietin)
|
BCR-ABL1 E255K • BCR-ABL1 V299L • BCR-ABL1 F317L • ABL1 T315I • BCR-ABL1 L248V • BCR-ABL1 Q252H • BCR-ABL1 F317V • JAK3 mutation • ABL1 E255K • BCR-ABL1 F317C • BCR-ABL1 T315A • ABL1 F317L • BCR-ABL1 L248R
|
dasatinib • Jakafi (ruxolitinib) • dexamethasone
Share via
