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- || tuspetinib (HM43239) / Aptose Biosci
Trial completion date, Trial primary completion date: APTIVATE: Clinical Trial to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Tuspetinib (HM43239) in Patients With Relapsed or Refractory Acute Myeloid Leukemia (clinicaltrials.gov) - Sep 4, 2024
P1/2, N=260, Recruiting, Sponsor: Aptose Biosciences Inc.
Trial completion date: Aug 2024 --> Dec 2026 | Trial primary completion date: Feb 2024 --> May 2026
- | Xospata (gilteritinib) / Astellas, tuspetinib (HM43239) / Aptose Biosci
Journal: Deciphering the mechanism of HM43239 inhibiting the mutant F691L resistant to gilteritinib in FMS-like tyrosine kinase 3. (Pubmed Central) - Jun 13, 2024
The F691L mutation had relatively larger effect on gilteritinib than HM43239, which showed as the changed and fixed conformation, respectively. These observations rationalized that the binding affinity of gilteritinib decreased more than that of HM43239 in the F691L mutant.Communicated by Ramaswamy H. Sarma.
- PHI-101 As a Potent Next-Generation FLT3 Inhibitor, Overcome Resistances in Previously Treated Patients with FLT3-ITD or TKD Acute Myeloid Leukemia: Results of a Phase Ia/Ib Clinical Trial (SDCC - Halls G-H) - Nov 3, 2023 - Abstract #ASH2023ASH_5718;
P1a/1b
Phase Ib dose-expansion trials with 160 mg daily dosing are currently ongoing. PHI-101 has delivered CRcs at 120 mg and 160 mg.
- Venclexta (venetoclax) / Roche, AbbVie, Walter and Eliza Hall Institute, tuspetinib (HM43239) / Aptose Biosci
Tuspetinib Myeloid Kinase Inhibitor Safety and Efficacy As Monotherapy and Combined with Venetoclax in Phase 1/2 Trial of Patients with Relapsed or Refractory (R/R) Acute Myeloid Leukemia (A... (SDCC - Room 6A) - Nov 3, 2023 - Abstract #ASH2023ASH_1176;
Tuspetinib was well-tolerated and delivered single agent clinical responses across four dose levels among diverse AML genotypes; with a RP2D of 80 mg chosen for future single agent studies. Although early, the VEN/TUS combination has been well tolerated with preliminary objective responses noted.
- Venclexta (venetoclax) / Roche, AbbVie, Walter and Eliza Hall Institute, tuspetinib (HM43239) / Aptose Biosci
IN VITRO ACQUIRED RESISTANCE TO THE ORAL MYELOID KINASE INHIBITOR TUSPETINIB CREATES SYNTHETIC LETHAL VULNERABILITY TO VENETOCLAX () - May 12, 2023 - Abstract #EHA2023EHA_2577;
P1/2
The fact that FLT3 remained fully inhibited in TUS/R cells growing in 75 nM TUS suggests that resistance is not due to a mutation of FLT3. Drug resistance in TUS/R cells in the absence of TUS over 60 days indicates a stable phenotype, distinct from "persister cell resistance" in which resistance fades during subsequent passages.
- ||| tuspetinib (HM43239) / Aptose Biosci, AFM13 / Affimed
#Ash2022 preview-1 多発性骨髄腫以外のがん領域では、投資家が2つの早期勝者を選んだ。#Aptose 社のHanmi由来の #キナーゼ阻害剤 #tuspetinib と #Affimed 社のCD30をターゲットとする #AFM13 だ。 https://t.co/wWhdfIZ3gJ #Evaluate (Twitter) - Nov 9, 2022
- tuspetinib (HM43239) / Aptose Biosci
A Phase 1/2 Dose Escalation Study of the Myeloid Kinase Inhibitor HM43239 in Patients with Relapsed or Refractory Acute Myeloid Leukemia (ENMCC - Hall D) - Nov 4, 2022 - Abstract #ASH2022ASH_4189;
Pharmacokinetic data illustrate increasing drug exposures through 120 mg and observed objective responses through 160 mg in both FLT3-WT and FLT3-mutated R/R AML patients even after gilteritinib and midostaurin treatment. An update of this study, including a planned single agent and venetoclax combination expansion, will be presented at the meeting.
- Xospata (gilteritinib) / Astellas, tuspetinib (HM43239) / Aptose Biosci, Vanflyta (quizartinib) / Daiichi Sankyo
A Potent Small Molecule Inhibitor of FLT3, PHI-101 Overcomes Resistance in Acute Myeloid Leukemia: Efficacy and PK/PD Profile in Phase 1 First in Human Study (ENMCC - Hall D) - Nov 4, 2022 - Abstract #ASH2022ASH_2296;
P1a/1b
PHI-101 showed good tolerance and favorable safety profile and reduced leukemic blasts significantly with 28-day dosing. PHI-101 sustained its activity to clear FLT3-ITD and/or FLT3-TKD mutations including D835Y or N676K identified in AML patients.
- || luxeptinib (CG-806) / Aptose Biosci, tuspetinib (HM43239) / Aptose Biosci
Note these are data on tuspetinib (=HM43239, ex Hanmi, Flt3/Syk/cKit/Jak), not luxeptinib (=CG-806, Flt3/BTK, formerly non-covalent BTK). All clear $APTO #ASH22 (Twitter) - Nov 3, 2022
- ||| tuspetinib (HM43239) / Aptose Biosci
Enrollment change, Trial completion date, Trial primary completion date: APTIVATE: Clinical Trial to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Tuspetinib (HM43239) in Patients With Relapsed or Refractory Acute Myeloid Leukemia (clinicaltrials.gov) - Sep 15, 2022
P1/2, N=218, Recruiting, Sponsor: Aptose Biosciences Inc.
PHI-101 sustained its activity to clear FLT3-ITD and/or FLT3-TKD mutations including D835Y or N676K identified in AML patients. N=120 --> 218 | Trial completion date: Jun 2023 --> Aug 2024 | Trial primary completion date: Jan 2023 --> Feb 2024
- HM43239 / Aptose Biosci
MYELOID KINOME INHIBITOR HM43239 OVERCOMES ACQUIRED RESISTANCE IN ACUTE MYELOID LEUKEMIA MODELS () - May 13, 2022 - Abstract #EHA2022EHA_715;
P1/2
Its ability to also inhibit SYK and, by reducing the activity of these upstream kinases, to also impair the activity of EKR1/2 and JAK/STAT5 that participate in rescue pathways, makes this a particularly interesting molecule with the potential of offsetting the development of resistance that is common with other FLT3 inhibitors. A Phase 1/2 trial of HM43239 in patients with AML is open and accruing patients (NCT03850574).
- ||| HM43239 / Aptose Biosci
$APTO HM43239 80% (4 of 5) responders advanced to HSCT (Twitter) - Apr 25, 2022
- HM43239 / Aptose Biosci
First in Human (FIH) FLT3 and SYK Inhibitor HM43239 Shows Single Agent Activity in Patients (pts) with Relapsed or Refractory (R/R) FLT3 Mutated and Wild-Type Acute Myeloid Leukemia (AML) (GWCC - Georgia Ballroom 1-3) - Nov 5, 2021 - Abstract #ASH2021ASH_2190;
P1/2
At 80 mg dose, HM43239 demonstrates clinical activity in both FLT3m (including a prior gilteritinib failure pt) and FLT3wt AML (including >1 year CR without HSCT in a relapsed TP53m AML). We continue to further evaluate doses above 80 mg to determine the optimal recommended Phase 2 Dose (RP2D).
- || HM43239 / Hanmi
$APTO Hanmi deal covering HM43239, $5m cash + $7.5m shares. Seems to hit several kinases beyond Flt3 (Twitter) - Nov 4, 2021
- ||| tuspetinib (HM43239) / Aptose Biosci
Enrollment change, Trial completion date, Trial primary completion date: APTIVATE: Clinical Trial to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Tuspetinib (HM43239) in Patients With Relapsed or Refractory Acute Myeloid Leukemia (clinicaltrials.gov) - Jun 4, 2021
P1/2, N=120, Recruiting, Sponsor: Hanmi Pharmaceutical Company Limited
We continue to further evaluate doses above 80 mg to determine the optimal recommended Phase 2 Dose (RP2D). N=200 --> 120 | Trial completion date: Dec 2021 --> Jun 2023 | Trial primary completion date: Dec 2020 --> Jan 2023
- HM43239 / Hanmi
[VIRTUAL] HM43239, a novel FLT3 inhibitor, has the potential to inhibit mutations resistant to FLT3 inhibitors () - Mar 11, 2021 - Abstract #AACR2021AACR_461;
P1/2
These results suggest that HM43239 could overcome the resistance induced by bone marrow microenvironment in AML patients.Taken together, HM43239 showed strong anticancer activity through various in vitro and in vivo preclinical models of AML, implicating the mechanism of overcoming resistance and preventing relapse. The effect of HM43239 in human would be demonstrated in ongoing Phase I/II clinical trials (NCT03850574) to develop promising therapeutics for patients with AML.
- HM43239 / Hanmi
[VIRTUAL] HM43239, a Novel Small Molecule Inhibitor of FLT3, in Acute Myeloid Leukemia (AML) with and without FMS-like Tyrosine Kinase 3 (FLT3) Mutations: Phase 1/2 Study (Poster Hall (Virtual Meeting)) - Nov 5, 2020 - Abstract #ASH2020ASH_1979;
P1/2
This study is currently recruiting patients at multiple sites in the Republic of Korea and the USA. Clinical trial information: NCT03850574.
- HM43239 / Hanmi
HM43239, a Novel Potent Small Molecule FLT3 Inhibitor, in Acute Myeloid Leukemia (AML) with FMS-like Tyrosine Kinase 3 (FLT3) Mutations: Phase 1 /2 Study (Hall B, Level 2 (Orange County Convention Center)) - Nov 7, 2019 - Abstract #ASH2019ASH_2153;
P1/2
Clinical trial information: NCT03850574 . 3,800 characters allowed 3,580 characters in abstract
- |||| tuspetinib (HM43239) / Aptose Biosci
New P1/2 trial: APTIVATE: Clinical Trial to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Tuspetinib (HM43239) in Patients With Relapsed or Refractory Acute Myeloid Leukemia (clinicaltrials.gov) - Feb 22, 2019
P1/2, N=200, Recruiting, Sponsor: Hanmi Pharmaceutical Company Limited