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- ulocuplumab (BMS-936564) / BMS
Combined CXCR-4 Inhibition with Novel Agent GPC-100 (burixafor) and Beta 2 Adrenergic Receptor Blockade Enhances Cytarabine Response for Acute Myeloid Leukemia Blasts on Stroma (Halls G-H (San Diego Convention Center)) - Nov 6, 2024 - Abstract #ASH2024ASH_5275;
P1
Clinical trials of CXCR4 inhibitors have been conducted to mobilize AML out of the protected BM niche, including plerixafor with 7+3 or MEC, BL-8040 with cytarabine (araC), LY2510924 with idarubicin/araC, and ulocuplumab (human IgG4 antibody) with MEC...In addition, high throughput drug screening of AML on stroma, but not in suspension or on CXCL12 coated plates, revealed that combination of the CXCR4 inhibitor GPC-100 and beta blocker propranolol, with araC, increased drug sensitivity (reduced IC50 by ?4 to >10 fold) as compared to araC alone for AML cells on HS-5 human stromal cell line or autologous patient mesenchymal stromal cells...Conclusions : These studies support further investigation of whether simultaneous blockade of CXCR4 and ADRB2 may potentiate chemotherapy response in AML, perhaps by disrupting microenvironment mediated chemotherapy protection. Patients with new diagnosis AML may be more susceptible to this approach than R/R AML due to higher CXCR4 expression by both blasts and LSCs.
- burixafor (GPC-100) / GPCR Therap
An Open-Label, Multi-Center Phase 2 Study to Assess the Safety and Efficacy of Burixafor (GPC-100) and Propranolol with G-CSF for the Mobilization of Stem Cells in Patients with Multiple Myeloma Undergoing Autologous Stem Cell Transplant (Halls G-H (San Diego Convention Center)) - Nov 6, 2024 - Abstract #ASH2024ASH_3750;
P2
Notably, burixafor allowed for same day administration of both mobilizing agent and leukapheresis. This quick kinetics of mobilization is differentiated from the FDA approved plerixafor or motixafortide, which require overnight pre-treatment prior to leukapheresis.
- burixafor (GPC-100) / GPCR Therap
Strategy to Improve Functional T-Cell Yield in Peripheral Blood By Co-Inhibition of Beta-2 Adrenergic and CXCR4 Signaling Pathways (Halls G-H (San Diego Convention Center)) - Nov 6, 2024 - Abstract #ASH2024ASH_3744;
P2
A significant increase in PB lymphocyte count was only observed when propranolol was combined with GPC-100, but not with AMD3100 or BL8040...Treatment of stimulated PBMC with epinephrine inhibited IFNy release, which was fully reversed when propranolol and GPC-100 were added...Therefore, we propose that propranolol can be safely combined with GPC-100 for improving CAR-T efficiency. Comprehensive analysis of immune cell subsets mobilized by propranolol and GPC-100 in our clinical study (NCT05561751) is also ongoing to evaluate this treatment for improving current approaches to cell and gene therapy.
- | burixafor (GPC-100) / GPCR Therap
Trial completion date, Trial primary completion date: Ph2, Study to Assess the Safety and Efficacy of GPC 100 and Propranolol With and Without G-CSF for the Mobilization of Stem Cells in Patients With Multiple Myeloma Undergoing Autologous Stem Cell Transplant (clinicaltrials.gov) - Apr 26, 2024
P2, N=40, Recruiting, Sponsor: GPCR Therapeutics, Inc.
Comprehensive analysis of immune cell subsets mobilized by propranolol and GPC-100 in our clinical study (NCT05561751) is also ongoing to evaluate this treatment for improving current approaches to cell and gene therapy. Trial completion date: Jun 2024 --> Jun 2025 | Trial primary completion date: Mar 2024 --> Mar 2025
- Toward optimizing CXCR4 inhibition with beta adrenergic blockade to enhance chemotherapy response in acute myeloid leukemia (Section 29) - Mar 5, 2024 - Abstract #AACR2024AACR_2576;
The CXCR4 inhibitor plerixafor is used to increase mobilization of peripheral blood stem cells in combination with filgrastim...These have included use of plerixafor with 7+3 or MEC, BL-8040 with cytarabine, and ulocuplumab with MEC...The objective of this preclinical study is to identify the AML patient population most likely to respond to CXCR4 inhibition, and the role of combined beta-adrenergic blockade, as the latter has been shown pre-clinically to augment mobilization of HSCs when combined with a CXCR4 inhibitor, GPC-100 (Sukhtankar et al... These studies support further investigation of whether simultaneous blockade of CXCR4 and ADBR2 may potentiate chemotherapy response in AML by limiting microenvironment mediated chemotherapy protection and reveal that patients with new diagnosis may be more susceptible to this approach.
- || burixafor (GPC-100) / GPCR Therap
Clinical, PK/PD data, Preclinical, Journal: Pharmacokinetics and Pharmacodynamics of Burixafor Hydrobromide (GPC-100), a Novel C-X-C Chemokine Receptor 4 Antagonist and Mobilizer of Hematopoietic Stem/Progenitor Cells, in Mice and Healthy Subjects. (Pubmed Central) - Nov 3, 2023
At maximal levels, the CD34 cell counts increased 3- to 14-fold from baseline levels. These results provide support for continued clinical development of burixafor.
- burixafor (GPC-100) / GPCR Therap
Combination of Propranolol and a Novel CXCR4 Antagonist Burixafor (GPC-100) for Enhanced Hematopoietic Cell Mobilization (SDCC - Halls G-H) - Nov 3, 2023 - Abstract #ASH2023ASH_4371;
P2
These results provide support for continued clinical development of burixafor. In cell-based assays, co-activation of both receptors with their respective ligands, CXCL12 and epinephrine, leads to a synergistic increase in calcium flux (Figure 1) as well as
- | burixafor (GPC-100) / GPCR Therap
Preclinical, Journal: GPC-100, a novel CXCR4 antagonist, improves in vivo hematopoietic cell mobilization when combined with propranolol. (Pubmed Central) - Oct 29, 2023
P2
Addition of propranolol to the G-CSF and GPC-100 combination resulted in greater stem cell mobilization than the G-CSF and plerixafor combination. Together, our studies suggest that the combination of GPC-100 and propranolol is a novel strategy for stem cell mobilization and support the current clinical trial in multiple myeloma registered as NCT05561751 at www.clinicaltrials.gov.
- | burixafor (GPC-100) / GPCR Therap, Viberzi (eluxadoline) / AbbVie
Journal: Identification of core therapeutic targets for Monkeypox virus and repurposing potential of drugs against them: An in silico approach. (Pubmed Central) - Jun 5, 2023
The affinity of these inhibitors suggests their repurposing potential. This work can encourage further experimental validation for possible therapeutic management of mpox.
- || burixafor (GPC-100) / GPCR Therap
Enrollment open: Ph2, Study to Assess the Safety and Efficacy of GPC 100 and Propranolol With and Without G-CSF for the Mobilization of Stem Cells in Patients With Multiple Myeloma Undergoing Autologous Stem Cell Transplant (clinicaltrials.gov) - Feb 16, 2023
P2, N=40, Recruiting, Sponsor: GPCR Therapeutics, Inc.
This work can encourage further experimental validation for possible therapeutic management of mpox. Not yet recruiting --> Recruiting
- burixafor (GPC-100) / GPCR Therap
GPC-100 Is a Novel CXCR4 Inhibitor That Leads to Improved in Vitro Potency and In Vivo Efficacy in Stem Cell Mobilization When Combined with a Beta-Blocker (ENMCC - Hall D) - Nov 4, 2022 - Abstract #ASH2022ASH_2823;
Previous studies indicate that stress hormones like epinephrine and norepinephrine exert stimulatory effects on cancer progression by modulating tumorigenesis, proliferation, and metastasis via B2AR signaling...Propranolol improved mobilization induced by a single administration of both GPC-100 and AMD3100...Additionally, combination treatment with G-CSF, GPC-100 and Pro may prove to be best-in-class mobilization therapy for ASCT in MM patients, especially those that fail to mobilize with standard of care. As a result, we will initiate a 2 arm, Phase 2 clinical trial evaluating both GPC-100 + Pro, and the triple combination of G-CSF + GPC-100 + Pro in Q4 of 2022.
- || burixafor (GPC-100) / GPCR Therap
New P2 trial: Ph2, Study to Assess the Safety and Efficacy of GPC 100 and Propranolol With and Without G-CSF for the Mobilization of Stem Cells in Patients With Multiple Myeloma Undergoing Autologous Stem Cell Transplant (clinicaltrials.gov) - Sep 30, 2022
P2, N=40, Not yet recruiting, Sponsor: GPCR Therapeutics, Inc.
- | burixafor (TG-0054) / TaiGen
Journal: Microglial Cytokines Induce Invasiveness and Proliferation of Human Glioblastoma through Pyk2 and FAK Activation. (Pubmed Central) - Dec 27, 2021
siRNA knockdown against Pyk2 or FAK in three primary glioblastoma cell lines, developed from the investigated specimens, in combination with the cytokine receptor inhibitors gefitinib (1 μM), DMPQ (200 nM), and burixafor (1 μM) identified EGF, PDGFβ, and SDF-1α as key extracellular factors in the Pyk2- and FAK-dependent activation of invadopodia formation and the migration of glioma cells. EGF and IL-6 were identified as regulators of the Pyk2- and FAK-dependent activation of cell viability and mitosis.
- | burixafor (TG-0054) / TaiGen, pemetrexed / Generic mfg., quisinostat (JNJ 26481585) / J&J, ChemRar
Journal: Prioritizing potential ACE2 inhibitors in the COVID-19 pandemic: Insights from a molecular mechanics-assisted structure-based virtual screening experiment. (Pubmed Central) - Sep 25, 2020
This study is among the rare ones in the relevant scientific literature to search for potential ACE2 inhibitors. In practical terms, the drugs, unmodified as they are, may be introduced into the therapeutic armamentarium of the ongoing fight against COVID-19 now, or their scaffolds may serve as rich skeletons for designing novel ACE2 inhibitors in the near future.
- | burixafor (TG-0054) / TaiGen
Journal: CXCR4 Antagonist Reduced the Incidence of Acute Rejection and Controlled Cardiac Allograft Vasculopathy in a Swine Heart Transplant Model Receiving a Mycophenolate-Based Immunosuppressive Regimen. (Pubmed Central) - May 7, 2019
Future studies are warranted into optimizing the therapeutic regimens for humans.This is an open-access article distributed under the terms of the Creative Commons Attribution-Non Commercial-No Derivatives License 4.0 (CCBY-NC-ND), where it is permissible to download and share the work provided it is properly cited. The work cannot be changed in any way or used commercially without permission from the journal.
- burixafor (GPC-100) / GPCR Therap, NN1213 / Novo Nordisk
Enrollment change, Trial completion date, Trial termination, Trial primary completion date, Tumor cell, Metastases: Pilot Study of Mobilization and Treatment of Disseminated Tumor Cells in Men With Metastatic Prostate Cancer (clinicaltrials.gov) - Jan 18, 2019
P1, N=3, Terminated, Sponsor: Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins
The work cannot be changed in any way or used commercially without permission from the journal. N=23 --> 3 | Trial completion date: Jul 2019 --> May 2017 | Active, not recruiting --> Terminated | Trial primary completion date: Jul 2018 --> May 2017; Low accrual
- | burixafor (GPC-100) / GPCR Therap
Enrollment closed, Trial primary completion date, Tumor cell, Metastases: Pilot Study of Mobilization and Treatment of Disseminated Tumor Cells in Men With Metastatic Prostate Cancer (clinicaltrials.gov) - Aug 1, 2017
P1, N=23, Active, not recruiting, Sponsor: Sidney Kimmel Comprehensive Cancer Center
N=23 --> 3 | Trial completion date: Jul 2019 --> May 2017 | Active, not recruiting --> Terminated | Trial primary completion date: Jul 2018 --> May 2017; Low accrual Recruiting --> Active, not recruiting | Trial primary completion date: Jul 2017 --> Jul 2018
- burixafor (GPC-100) / GPCR Therap
Enrollment open, Trial primary completion date, Tumor cell, Metastases: Pilot Study of Mobilization and Treatment of Disseminated Tumor Cells in Men With Metastatic Prostate Cancer (clinicaltrials.gov) - Feb 23, 2016
P1, N=23, Recruiting, Sponsor: Kenneth Pienta, MD
Recruiting --> Active, not recruiting | Trial primary completion date: Jul 2017 --> Jul 2018 Not yet recruiting --> Recruiting | Trial primary completion date: Jul 2016 --> Jul 2017
- | burixafor (GPC-100) / GPCR Therap
Trial completion: PD and Safety of TG-0054 Combined With G-CSF in Multiple Myeloma, Non-Hodgkin Lymphoma and Hodgkin Disease Patients (clinicaltrials.gov) - Jan 15, 2016
P2, N=12, Completed, Sponsor: TaiGen Biotechnology Co., Ltd.
Not yet recruiting --> Recruiting | Trial primary completion date: Jul 2016 --> Jul 2017 Recruiting --> Completed
- burixafor (GPC-100) / GPCR Therap
New P1 trial, Tumor cell, Metastases: Pilot Study of Mobilization and Treatment of Disseminated Tumor Cells in Men With Metastatic Prostate Cancer (clinicaltrials.gov) - Jun 23, 2015
P1, N=23, Not yet recruiting, Sponsor: Kenneth Pienta, MD
- | burixafor (GPC-100) / GPCR Therap
Enrollment open: PD and Safety of TG-0054 Combined With G-CSF in Multiple Myeloma, Non-Hodgkin Lymphoma and Hodgkin Disease Patients (clinicaltrials.gov) - Apr 13, 2015
P2, N=12, Recruiting, Sponsor: TaiGen Biotechnology Co., Ltd.
Recruiting --> Completed Not yet recruiting --> Recruiting
- | burixafor (GPC-100) / GPCR Therap
Trial initiation date: PD and Safety of TG-0054 Combined With G-CSF in Multiple Myeloma, Non-Hodgkin Lymphoma and Hodgkin Disease Patients (clinicaltrials.gov) - Dec 7, 2014
P2, N=12, Not yet recruiting, Sponsor: TaiGen Biotechnology Co., Ltd.
Not yet recruiting --> Recruiting Initiation date: May 2014 --> Dec 2014
- | burixafor (GPC-100) / GPCR Therap
New P2 trial: PD and Safety of TG-0054 Combined With G-CSF in Multiple Myeloma, Non-Hodgkin Lymphoma and Hodgkin Disease Patients (clinicaltrials.gov) - Apr 2, 2014
P2, N=12, Not yet recruiting, Sponsor: TaiGen Biotechnology Co., Ltd.
- burixafor (GPC-100) / GPCR Therap
Trial initiation date, Combination therapy: A Study to Evaluate the Safety, Pharmacokinetics, and Hematopoietic Stem Cell Mobilization of TG-0054 Alone or in Combination With G-CSF in Patients With Multiple Myeloma, Non-Hodgkin Lymphoma or Hodgkin Disease (clinicaltrials.gov) - Mar 24, 2014
P2, N=12, Completed, Sponsor: TaiGen Biotechnology Co., Ltd.
Initiation date: May 2014 --> Dec 2014 Initiation date: Dec 2011 --> Oct 2012
- || burixafor (GPC-100) / GPCR Therap
Enrollment change: Evaluating the Safety, Tolerability, Pharmacokinetics and Efficacy of TG-0054 With Single IV Doses Escalation in Healthy Volunteers (clinicaltrials.gov) - Mar 24, 2014
P1, N=64, Completed, Sponsor: TaiGen Biotechnology Co., Ltd.
Initiation date: Dec 2011 --> Oct 2012 N=48 --> 64
- burixafor (GPC-100) / GPCR Therap
Trial completion, Combination therapy: A Study to Evaluate the Safety, Pharmacokinetics, and Hematopoietic Stem Cell Mobilization of TG-0054 Alone or in Combination With G-CSF in Patients With Multiple Myeloma, Non-Hodgkin Lymphoma or Hodgkin Disease (clinicaltrials.gov) - Mar 24, 2014
P2, N=12, Completed, Sponsor: TaiGen Biotechnology Co., Ltd.
N=48 --> 64 Recruiting --> Completed
- | burixafor (GPC-100) / GPCR Therap
Enrollment change: Safety and PK/PD of TG-0054 in Multiple Myeloma, Non-Hodgkin Lymphoma and Hodgkin Disease Patients (clinicaltrials.gov) - Aug 8, 2012
P2, N=19, Completed, Sponsor: TaiGen Biotechnology Co., Ltd.
Recruiting --> Completed N=15 --> 19
- | burixafor (GPC-100) / GPCR Therap
Trial completion: Safety and PK/PD of TG-0054 in Multiple Myeloma, Non-Hodgkin Lymphoma and Hodgkin Disease Patients (clinicaltrials.gov) - Aug 8, 2012
P2, N=19, Completed, Sponsor: TaiGen Biotechnology Co., Ltd.
N=15 --> 19 Recruiting --> Completed
- burixafor (GPC-100) / GPCR Therap
New P2 trial, Combination therapy: A Study to Evaluate the Safety, Pharmacokinetics, and Hematopoietic Stem Cell Mobilization of TG-0054 Alone or in Combination With G-CSF in Patients With Multiple Myeloma, Non-Hodgkin Lymphoma or Hodgkin Disease (clinicaltrials.gov) - Oct 20, 2011
P2, N=12, Completed, Sponsor: TaiGen Biotechnology Co., Ltd.