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DRUG:

elzovantinib (TPX-0022)

i
Other names: TPX-0022, TPX 0022, TPX0022
Company:
BMS, ZAI Lab
Drug class:
Src kinase inhibitor, c-MET inhibitor, CSF-1R inhibitor
Related drugs:
5d
SHIELD-1: Study of TPX-0022 in Patients With Advanced NSCLC, Gastric Cancer or Solid Tumors Harboring Genetic Alterations in MET (clinicaltrials.gov)
P1, N=95, Active, not recruiting, Turning Point Therapeutics, Inc. | Phase classification: P1/2 --> P1 | N=180 --> 95 | Trial completion date: Mar 2025 --> Mar 2026 | Trial primary completion date: Mar 2025 --> Jan 2024
Phase classification • Enrollment change • Trial completion date • Trial primary completion date • Metastases
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MET (MET proto-oncogene, receptor tyrosine kinase)
|
MET amplification • MET exon 14 mutation • MET mutation • MET fusion
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elzovantinib (TPX-0022)
1year
Structural insight into the macrocyclic inhibitor TPX-0022 of c-Met and c-Src. (PubMed, Comput Struct Biotechnol J)
In addition, TPX-0022 exhibited potent activity against the resistance-relevant c-Met L1195F mutant and moderate activity against the c-Met G1163R, F1200I and Y1230H mutants but weak activity against the c-Met D1228N and Y1230C mutants. Overall, our study reveals the structural mechanism underlying the potency and selectivity of TPX-0022 and the ability to overcome acquire resistance mutations and provides insight into the development of selective c-Met macrocyclic inhibitors.
Journal
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MET (MET proto-oncogene, receptor tyrosine kinase) • CSF1R (Colony stimulating factor 1 receptor)
|
MET mutation • MET D1228N • MET F1200I • MET Y1230C • MET Y1230C
|
elzovantinib (TPX-0022)
1year
SHIELD-1: Study of TPX-0022 in Patients With Advanced NSCLC, Gastric Cancer or Solid Tumors Harboring Genetic Alterations in MET (clinicaltrials.gov)
P1/2, N=180, Active, not recruiting, Turning Point Therapeutics, Inc. | Trial completion date: Nov 2023 --> Mar 2025 | Trial primary completion date: Nov 2023 --> Mar 2025
Trial completion date • Trial primary completion date • Metastases
|
MET (MET proto-oncogene, receptor tyrosine kinase)
|
MET amplification • MET exon 14 mutation • MET mutation • MET fusion
|
elzovantinib (TPX-0022)
over1year
SHIELD-1: Study of TPX-0022 in Patients With Advanced NSCLC, Gastric Cancer or Solid Tumors Harboring Genetic Alterations in MET (clinicaltrials.gov)
P1/2, N=180, Active, not recruiting, Turning Point Therapeutics, Inc. | Recruiting --> Active, not recruiting
Enrollment closed • Metastases
|
MET (MET proto-oncogene, receptor tyrosine kinase)
|
MET amplification • MET exon 14 mutation • MET mutation • MET fusion
|
elzovantinib (TPX-0022)
almost2years
Activating MET Kinase Domain Mutations Define a Novel Targetable Molecular Subtype of Non-small Cell Lung Cancer that is Clinically Sensitive to MET Inhibitor Elzovantinib (TPX-0022) (IASLC-TTLC 2023)
"CONCLUSION Activating MET TKD mutations without concurrent MET exon 14 mutations were detected in ~ 0.2% of NSCLC, and occur in the absence of other known drivers in a subset of cases. Comprehensive genomic profiling to detect these alterations and guide treatment selection and clinical trial enrollment is warranted."
Clinical
|
EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase)
|
KRAS mutation • MET amplification • EGFR amplification • MET exon 14 mutation • MET H1094Y • MET D1228N • MET F1200I
|
elzovantinib (TPX-0022)
2years
SHIELD-1: Study of TPX-0022 in Patients With Advanced NSCLC, Gastric Cancer or Solid Tumors Harboring Genetic Alterations in MET (clinicaltrials.gov)
P1/2, N=180, Recruiting, Turning Point Therapeutics, Inc. | N=330 --> 180 | Trial primary completion date: Nov 2022 --> Nov 2023
Enrollment change • Trial primary completion date • Metastases
|
MET (MET proto-oncogene, receptor tyrosine kinase)
|
MET amplification • MET exon 14 mutation • MET mutation • MET fusion
|
elzovantinib (TPX-0022)
over2years
Preliminary interim data of elzovantinib (TPX-0022), a novel inhibitor of MET/SRC/CSF1R, in patients with advanced solid tumors harboring genetic alterations in MET: Update from the Phase 1 SHIELD-1 trial (AACR-NCI-EORTC 2022)
Elzovantinib, a novel MET/SRC/CSF1R inhibitor, was generally well tolerated with primarily low-grade dizziness, no high-grade edema, and a favorable PK profile. The RP2D is currently under evaluation and updated safety and efficacy data will be available for presentation. A global multi-cohort Phase 2 trial of pts with MET-altered tumors is planned.
Clinical • P1 data
|
MET (MET proto-oncogene, receptor tyrosine kinase) • CSF1R (Colony stimulating factor 1 receptor)
|
MET exon 14 mutation
|
elzovantinib (TPX-0022)
over2years
SHIELD-1: Study of TPX-0022 in Patients With Advanced NSCLC, Gastric Cancer or Solid Tumors Harboring Genetic Alterations in MET (clinicaltrials.gov)
P1/2, N=330, Recruiting, Turning Point Therapeutics, Inc. | Phase classification: P1 --> P1/2 | N=120 --> 330
Phase classification • Enrollment change
|
MET (MET proto-oncogene, receptor tyrosine kinase)
|
MET amplification • MET exon 14 mutation • MET mutation
|
elzovantinib (TPX-0022)
4years
[VIRTUAL] First-in-human safety, pharmacokinetics, and preliminary efficacy of TPX-0022, a novel inhibitor of MET/SRC/CSF1R in patients with advanced solid tumors harboring genetic alterations in MET (AACR-NCI-EORTC 2020)
TPX-0022 is a novel MET/SRC/CSF1R inhibitor. TPX-0022 was generally well-tolerated. Responses were observed in Δex14 NSCLC and MET amplified GC and CRC.
Clinical • P1 data • PK/PD data • Late-breaking abstract
|
HGF (Hepatocyte growth factor) • CSF1R (Colony stimulating factor 1 receptor)
|
MET amplification • MET exon 14 mutation
|
elzovantinib (TPX-0022)
over4years
Clinical • P1 data • PK/PD data
|
MET (MET proto-oncogene, receptor tyrosine kinase) • HGF (Hepatocyte growth factor) • CSF1R (Colony stimulating factor 1 receptor)
|
MET amplification • MET exon 14 mutation
|
elzovantinib (TPX-0022)
almost5years
Clinical • Trial initiation date
|
MET (MET proto-oncogene, receptor tyrosine kinase)
|
MET amplification • MET exon 14 mutation • MET exon 14 deletion
|
elzovantinib (TPX-0022)