^
Contact us  to learn more about
our Premium Content:  News alerts, weekly reports and conference planners
DRUG:

nazartinib (EGF816)

i
Other names: EGF816, EGF 816, EGF-816, NVS-816, NVS 816, NVS816
Company:
Novartis
Drug class:
EGFR inhibitor
Related drugs:
2ms
Study of EGF816 in Combination With Selected Targeted Agents in EGFR-mutant NSCLC (clinicaltrials.gov)
P1, N=105, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Dec 2024 --> Apr 2025 | Trial primary completion date: Dec 2024 --> Apr 2025
Trial completion date • Trial primary completion date • Combination therapy
|
EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR exon 20 insertion • EGFR exon 20 mutation
|
Mekinist (trametinib) • gefitinib • Kisqali (ribociclib) • Tabrecta (capmatinib) • naporafenib (ERAS-254) • nazartinib (EGF816)
4ms
Characterization of the in vitro metabolic profile of nazartinib in HLMs using UPLC-MS/MS method: In silico metabolic lability and DEREK structural alerts screening using StarDrop software. (PubMed, Heliyon)
In the context of computational software, making minor adjustments or substituting the dimethylamino-butenoyl moiety throughout the drug design process may increase the metabolic stability and safety properties of new synthesized derivatives. The efficiency of utilizing different in silico software approaches to conserve resources and reduce effort was proved by the outcomes attained from in vitro incubation experiments and the use of NZT in silico software.
Preclinical • Journal
|
EGFR (Epidermal growth factor receptor)
|
nazartinib (EGF816)
4ms
A Study of EGF816 and Gefitinib in TKI-naïve EGFR-mutant Non-Small Cell Lung Cancer (clinicaltrials.gov)
P2, N=11, Active, not recruiting, Massachusetts General Hospital | Trial completion date: Jun 2024 --> Dec 2024
Trial completion date
|
gefitinib • nazartinib (EGF816)
4ms
Capmatinib plus nazartinib in patients with EGFR-mutated non-small cell lung cancer. (PubMed, Eur J Cancer)
Capmatinib plus nazartinib showed antitumor activity in patients with EGFR-TKI-resistant, EGFR-mutated NSCLC. The overall safety profile was acceptable.
Journal
|
EGFR (Epidermal growth factor receptor)
|
Tabrecta (capmatinib) • nazartinib (EGF816)
5ms
Dose Finding Study of TNO155 in Adult Patients With Advanced Solid Tumors (clinicaltrials.gov)
P1, N=227, Active, not recruiting, Novartis Pharmaceuticals | Recruiting --> Active, not recruiting
Enrollment closed • Metastases
|
KRAS (KRAS proto-oncogene GTPase)
|
batoprotafib (TNO155) • nazartinib (EGF816)
9ms
EATON: EGF816 and Trametinib in Patients With Non-small Cell Lung Cancer Harboring Activating EGFR Mutations (clinicaltrials.gov)
P1, N=18, Completed, University of Cologne | Recruiting --> Completed | Trial completion date: Apr 2023 --> Nov 2023
Trial completion • Trial completion date
|
EGFR mutation • EGFR L858R • EGFR T790M negative
|
Mekinist (trametinib) • Tagrisso (osimertinib) • nazartinib (EGF816)
11ms
Dose Finding Study of TNO155 in Adult Patients With Advanced Solid Tumors (clinicaltrials.gov)
P1, N=255, Recruiting, Novartis Pharmaceuticals | Trial completion date: Oct 2024 --> Apr 2025 | Trial primary completion date: Oct 2024 --> Apr 2025
Trial completion date • Trial primary completion date • Metastases
|
KRAS (KRAS proto-oncogene GTPase)
|
batoprotafib (TNO155) • nazartinib (EGF816)
over1year
Study of EGF816 in Combination With Selected Targeted Agents in EGFR-mutant NSCLC (clinicaltrials.gov)
P1, N=105, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Mar 2024 --> Sep 2024 | Trial primary completion date: Mar 2024 --> Sep 2024
Trial completion date • Trial primary completion date • Combination therapy
|
EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR exon 20 insertion • EGFR exon 20 mutation
|
Mekinist (trametinib) • gefitinib • Kisqali (ribociclib) • Tabrecta (capmatinib) • naporafenib (ERAS-254) • nazartinib (EGF816)
over1year
Dose Finding Study of TNO155 in Adult Patients With Advanced Solid Tumors (clinicaltrials.gov)
P1, N=255, Recruiting, Novartis Pharmaceuticals | Trial completion date: Apr 2024 --> Aug 2024 | Trial primary completion date: Feb 2024 --> Aug 2024
Trial completion date • Trial primary completion date • Metastases
|
KRAS (KRAS proto-oncogene GTPase)
|
batoprotafib (TNO155) • nazartinib (EGF816)
over1year
A Study of EGF816 and Gefitinib in TKI-naïve EGFR-mutant Non-Small Cell Lung Cancer (clinicaltrials.gov)
P2, N=11, Active, not recruiting, Massachusetts General Hospital | Trial completion date: Oct 2025 --> Jun 2024 | Trial primary completion date: Oct 2022 --> Dec 2023
Trial completion date • Trial primary completion date
|
EGFR mutation • EGFR L858R
|
gefitinib • nazartinib (EGF816)
over1year
Integrated CRISPR screening and drug profiling identifies combination opportunities for EGFR, ALK, and BRAF/MEK inhibitors. (PubMed, Cell Rep)
Data from drug combination screens with EGF816 and ceritinib indicate that dasatinib and agents disrupting microtubules act synergistically across many cell lines. Finally, we show that a higher-order-combination screen with 26 selected drugs in two resistant EGFR-mutant lung cancer cell lines identified active triplet combinations.
Journal
|
EGFR (Epidermal growth factor receptor) • BCL2L1 (BCL2-like 1) • YAP1 (Yes associated protein 1)
|
EGFR mutation
|
dasatinib • Zykadia (ceritinib) • nazartinib (EGF816)
almost2years
Study of EGF816 in Combination With Selected Targeted Agents in EGFR-mutant NSCLC (clinicaltrials.gov)
P1, N=105, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Sep 2023 --> Mar 2024 | Trial primary completion date: Sep 2023 --> Mar 2024
Trial completion date • Trial primary completion date • Combination therapy
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR exon 20 insertion • EGFR exon 20 mutation
|
Mekinist (trametinib) • gefitinib • Kisqali (ribociclib) • Tabrecta (capmatinib) • naporafenib (ERAS-254) • nazartinib (EGF816)
over2years
Nazartinib for treatment-naive EGFR-mutant non-small cell lung cancer: Results of a phase 2, single-arm, open-label study. (PubMed, Eur J Cancer)
First-line nazartinib demonstrated promising efficacy, including clinically meaningful antitumor activity in the brain, and manageable safety in patients with EGFR-mutant NSCLC.
P2 data • Journal
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR L858R • EGFR exon 19 deletion
|
nazartinib (EGF816)
over2years
Study of EGF816 in Combination With Selected Targeted Agents in EGFR-mutant NSCLC (clinicaltrials.gov)
P1, N=105, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Nov 2022 --> Sep 2023 | Trial primary completion date: Nov 2022 --> Sep 2023
Trial completion date • Trial primary completion date • Combination therapy
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR exon 20 insertion • EGFR exon 20 mutation
|
Mekinist (trametinib) • gefitinib • Kisqali (ribociclib) • Tabrecta (capmatinib) • naporafenib (ERAS-254) • nazartinib (EGF816)
over2years
Dose Finding Study of TNO155 in Adult Patients With Advanced Solid Tumors (clinicaltrials.gov)
P1, N=255, Recruiting, Novartis Pharmaceuticals | Trial completion date: Aug 2023 --> Feb 2024 | Trial primary completion date: Aug 2023 --> Feb 2024
Trial completion date • Trial primary completion date
|
KRAS (KRAS proto-oncogene GTPase)
|
batoprotafib (TNO155) • nazartinib (EGF816)
over2years
A Phase I/II, Multicenter, Open-label Study of EGFRmut-TKI EGF816, Administered Orally in Adult Patients With EGFRmut Solid Malignancies (clinicaltrials.gov)
P1/2, N=225, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Mar 2022 --> Oct 2023
Trial completion date
|
EGFR (Epidermal growth factor receptor)
|
nazartinib (EGF816)
over2years
Study of Efficacy and Safety of Nivolumab in Combination With EGF816 and of Nivolumab in Combination With INC280 in Patients With Previously Treated Non-small Cell Lung Cancer (clinicaltrials.gov)
P2, N=64, Terminated, Novartis Pharmaceuticals | Completed --> Terminated; Sponsor decision due to low patient recruitment caused by the change in the treatment landscape of NSCLC.
Trial termination • Combination therapy
|
EGFR (Epidermal growth factor receptor)
|
EGFR T790M • EGFR wild-type
|
Opdivo (nivolumab) • Tabrecta (capmatinib) • nazartinib (EGF816)
almost3years
A Study of EGF816 and Gefitinib in TKI-naïve EGFR-mutant Non-Small Cell Lung Cancer (clinicaltrials.gov)
P2, N=11, Active, not recruiting, Massachusetts General Hospital | Recruiting --> Active, not recruiting
Enrollment closed
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR L858R
|
gefitinib • nazartinib (EGF816)
3years
Study of Safety and Efficacy of EGFR-TKI EGF816 in Combination With cMET Inhibitor INC280 in Non-small Cell Lung Cancer Patients With EGFR Mutation. (clinicaltrials.gov)
P1/2, N=177, Active, not recruiting, Novartis Pharmaceuticals | Completed --> Active, not recruiting | Trial completion date: Nov 2020 --> Jul 2025 | Trial primary completion date: Nov 2020 --> Jul 2025
Clinical • Enrollment closed • Trial completion date • Trial primary completion date • Combination therapy
|
MET (MET proto-oncogene, receptor tyrosine kinase)
|
EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR L861Q • EGFR G719X • EGFR S768I • EGFR T790M negative
|
Tabrecta (capmatinib) • nazartinib (EGF816)
3years
Mechanisms and management of 3rd‑generation EGFR‑TKI resistance in advanced non‑small cell lung cancer (Review). (PubMed, Int J Oncol)
Other 3rd‑generation EGFR‑TKIs, such as abivertinib, rociletinib, nazartinib, olmutinib and alflutinib, are also at various stages of development. The mechanisms of acquired resistance mainly include an altered EGFR signaling pathway (EGFR tertiary mutations and amplification), activation of aberrant bypassing pathways (hepatocyte growth factor receptor amplification, human epidermal growth factor receptor 2 amplification and aberrant insulin‑like growth factor 1 receptor activation), downstream pathway activation (RAS/RAF/MEK/ERK and PI3K/AKT/mTOR) and histological/phenotypic transformations (SCLC transformation and epithelial‑mesenchymal transition). The combination of targeted therapies is a promising strategy to treat osimertinib‑resistant patients, and multiple clinical studies on novel combined therapies are ongoing.
Review • Journal
|
EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • MET (MET proto-oncogene, receptor tyrosine kinase)
|
EGFR mutation • HER-2 amplification • EGFR T790M • TERT mutation • HGF amplification
|
Tagrisso (osimertinib) • Ivesa (firmonertinib) • Xegafri (rociletinib) • nazartinib (EGF816) • Olita (olmutinib) • Fujovee (abivertinib)
over3years
Study of EGF816 in Combination With Selected Targeted Agents in EGFR-mutant NSCLC (clinicaltrials.gov)
P1, N=105, Active, not recruiting, Novartis Pharmaceuticals | Recruiting --> Active, not recruiting | N=157 --> 105
Clinical • Enrollment closed • Enrollment change • Combination therapy
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR exon 20 insertion • EGFR exon 20 mutation
|
Mekinist (trametinib) • gefitinib • Kisqali (ribociclib) • Tabrecta (capmatinib) • naporafenib (ERAS-254) • nazartinib (EGF816)
over3years
Study of Efficacy and Safety of Nivolumab in Combination With EGF816 and of Nivolumab in Combination With INC280 in Patients With Previously Treated Non-small Cell Lung Cancer (clinicaltrials.gov)
P2, N=64, Completed, Novartis Pharmaceuticals | Active, not recruiting --> Completed | Trial completion date: Dec 2021 --> Feb 2021
Clinical • Trial completion • Trial completion date • Combination therapy
|
EGFR (Epidermal growth factor receptor)
|
EGFR T790M
|
Opdivo (nivolumab) • Tabrecta (capmatinib) • nazartinib (EGF816)
over3years
Clinical efficacy and safety of nazartinib for epidermal growth factor receptor mutated non-small cell lung cancer: Study protocol for a prospective, multicenter, open-label. (PubMed, Medicine (Baltimore))
The study will investigate the clinical safety and efficacy of nazartinib in patients suffering from EGFR-mutated NSCLC. The anticipated results of the study are expected to provide clinical basis for nazartinib to treat patients suffering from EGFR-mutated NSCLC.
Clinical • Clinical protocol • Journal
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation
|
nazartinib (EGF816)
over3years
Study of EGF816 in Combination With Selected Targeted Agents in EGFR-mutant NSCLC (clinicaltrials.gov)
P1, N=157, Recruiting, Novartis Pharmaceuticals | Trial completion date: Mar 2024 --> Nov 2022 | Trial primary completion date: Mar 2024 --> Nov 2022
Clinical • Trial completion date • Trial primary completion date • Combination therapy
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR exon 20 insertion • EGFR exon 20 mutation
|
Mekinist (trametinib) • gefitinib • Kisqali (ribociclib) • Tabrecta (capmatinib) • naporafenib (ERAS-254) • nazartinib (EGF816)
over3years
A Study of PDR001 in Combination With CJM112, EGF816, Ilaris® (Canakinumab) or Mekinist® (Trametinib) (clinicaltrials.gov)
P1, N=289, Completed, Novartis Pharmaceuticals | Active, not recruiting --> Completed
Clinical • Trial completion • Combination therapy
|
CD8 (cluster of differentiation 8) • FOXP3 (Forkhead Box P3)
|
Mekinist (trametinib) • spartalizumab (PDR001) • nazartinib (EGF816) • CJM112 • Ilaris (canakinumab)
over3years
Dose Finding Study of TNO155 in Adult Patients With Advanced Solid Tumors (clinicaltrials.gov)
P1, N=255, Recruiting, Novartis Pharmaceuticals | Trial completion date: Aug 2022 --> Aug 2023 | Trial primary completion date: Aug 2022 --> Aug 2023
Clinical • Trial completion date • Trial primary completion date
|
KRAS (KRAS proto-oncogene GTPase)
|
batoprotafib (TNO155) • nazartinib (EGF816)
almost4years
Study of EGF816 in Combination With Selected Targeted Agents in EGFR-mutant NSCLC (clinicaltrials.gov)
P1, N=157, Recruiting, Novartis Pharmaceuticals | Trial completion date: May 2022 --> Mar 2024 | Trial primary completion date: May 2022 --> Mar 2024
Clinical • Trial completion date • Trial primary completion date • Combination therapy
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR T790M • EGFR exon 20 insertion • EGFR exon 20 mutation
|
Mekinist (trametinib) • gefitinib • Kisqali (ribociclib) • Tabrecta (capmatinib) • naporafenib (ERAS-254) • nazartinib (EGF816)
almost4years
Beyond osimertinib: The development of 3-generation EGFR Tyrosine Kinase Inhibitors. (PubMed, J Thorac Oncol)
In this review, we profiled many of the third-generation EGFR TKIs in late stage clinical development (e.g. almonertinib, lazertinib, alflutinib, rezivertinib, ASK120069, SH-1028, D-0316 and abivertinib) of their interim results of phase 1-3 trials and their chemical structures when publicly available. Additionally, we summarized the results of clinical trials that previously reported third-generation EGFR TKIs (rociletinib, olmutinib, nazartinib, maverlertinib) including phase 3 results of rociletinib and naquotinib. We further profiled the next-generation combination clinical trial design of third-generation EGFR TKIs including FLAURA2 (NCT04035486), MARIPOSA (NCT04487080), ACROSS1 (NCT04500704) and ACROSS2 (NCT04500717).
Review • Journal
|
EGFR (Epidermal growth factor receptor)
|
EGFR T790M
|
Tagrisso (osimertinib) • Ameile (aumolertinib) • Ivesa (firmonertinib) • Lazcluze (lazertinib) • Xegafri (rociletinib) • nazartinib (EGF816) • Semena (befotertinib) • naquotinib (ASP8273) • Olita (olmutinib) • Rui Bi Da (rezivertinib) • Fujovee (abivertinib) • Sanrisso (rilertinib)
almost4years
A Study of EGF816 and Gefitinib in TKI-naïve EGFR-mutant Non-Small Cell Lung Cancer (clinicaltrials.gov)
P2, N=11, Recruiting, Massachusetts General Hospital | N=36 --> 11 | Trial completion date: Mar 2025 --> Oct 2025 | Trial primary completion date: Mar 2021 --> Oct 2022
Enrollment change • Trial completion date • Trial primary completion date
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR L858R
|
gefitinib • nazartinib (EGF816)
almost4years
A Study of PDR001 in Combination With CJM112, EGF816, Ilaris® (Canakinumab) or Mekinist® (Trametinib) (clinicaltrials.gov)
P1, N=290, Active, not recruiting, Novartis Pharmaceuticals | Trial completion date: Nov 2020 --> Mar 2021 | Trial primary completion date: Nov 2020 --> Mar 2021
Clinical • Trial completion date • Trial primary completion date • Combination therapy • PD(L)-1 Biomarker
|
CD8 (cluster of differentiation 8) • FOXP3 (Forkhead Box P3)
|
TILs
|
Mekinist (trametinib) • spartalizumab (PDR001) • nazartinib (EGF816) • CJM112 • Ilaris (canakinumab)
4years
[VIRTUAL] Pulmonary adenocarcinoma EGFR exon 20 insertion determined in liquid biopsy – case report (ECP 2020)
Exon 20 insertion mutation is associated with lack of sensitivity to first-generation EGFR TKIs (erlotinib/gefitinib) and a partial response to second-generation (afatinib) and third-generation (osimertinib/rociletinib); promising results for nazartinib and poziotinib are on line. Conclusion Studies showed that different exon 20 insertions lead to different response to EGFR TKIs depending on the location in the kinase domain that they affect. Therefore, it is important to report the mutation and make the follow up.
Clinical • Liquid biopsy
|
EGFR (Epidermal growth factor receptor) • ER (Estrogen receptor) • NKX2-1 (NK2 Homeobox 1) • VIM (Vimentin)
|
EGFR mutation • ATM mutation • EGFR exon 20 insertion • EGFR exon 20 mutation
|
Idylla™ EGFR Mutation Test • Oncomine™ Lung cfDNA Assay
|
Tagrisso (osimertinib) • erlotinib • Gilotrif (afatinib) • gefitinib • Pozenveo (poziotinib) • Xegafri (rociletinib) • nazartinib (EGF816)
4years
[VIRTUAL] Pulmonary adenocarcinoma EGFR exon 20 insertion determined in liquid biopsy – case report (ECP 2020)
Exon 20 insertion mutation is associated with lack of sensitivity to first-generation EGFR TKIs (erlotinib/gefitinib) and a partial response to second-generation (afatinib) and third-generation (osimertinib/rociletinib); promising results for nazartinib and poziotinib are on line. Conclusion Studies showed that different exon 20 insertions lead to different response to EGFR TKIs depending on the location in the kinase domain that they affect. Therefore, it is important to report the mutation and make the follow up.
Clinical • Liquid biopsy
|
EGFR (Epidermal growth factor receptor) • ER (Estrogen receptor) • NKX2-1 (NK2 Homeobox 1) • VIM (Vimentin)
|
EGFR mutation • ATM mutation • EGFR exon 20 insertion • EGFR exon 20 mutation
|
Idylla™ EGFR Mutation Test • Oncomine™ Lung cfDNA Assay
|
Tagrisso (osimertinib) • erlotinib • Gilotrif (afatinib) • gefitinib • Pozenveo (poziotinib) • Xegafri (rociletinib) • nazartinib (EGF816)
4years
[VIRTUAL] Pulmonary adenocarcinoma EGFR exon 20 insertion determined in liquid biopsy – case report (ECP 2020)
Exon 20 insertion mutation is associated with lack of sensitivity to first-generation EGFR TKIs (erlotinib/gefitinib) and a partial response to second-generation (afatinib) and third-generation (osimertinib/rociletinib); promising results for nazartinib and poziotinib are on line. Conclusion Studies showed that different exon 20 insertions lead to different response to EGFR TKIs depending on the location in the kinase domain that they affect. Therefore, it is important to report the mutation and make the follow up.
Clinical • Liquid biopsy
|
EGFR (Epidermal growth factor receptor) • ER (Estrogen receptor) • NKX2-1 (NK2 Homeobox 1) • VIM (Vimentin)
|
EGFR mutation • ATM mutation • EGFR exon 20 insertion • EGFR exon 20 mutation
|
Idylla™ EGFR Mutation Test • Oncomine™ Lung cfDNA Assay
|
Tagrisso (osimertinib) • erlotinib • Gilotrif (afatinib) • gefitinib • Pozenveo (poziotinib) • Xegafri (rociletinib) • nazartinib (EGF816)
4years
Combinations with allosteric SHP2 inhibitor TNO155 to block receptor tyrosine kinase signaling. (PubMed, Clin Cancer Res)
Our findings suggest TNO155 is an effective agent for blocking both tumor-promoting and immune-suppressive RTK signaling in RTK- and MAPK-driven cancers and their tumor microenvironment. Our data provide the rationale for evaluating these combinations clinically.
Journal • PD(L)-1 Biomarker
|
EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • CSF1R (Colony stimulating factor 1 receptor)
|
KRAS mutation • EGFR mutation • EGFR mutation + KRAS mutation
|
Kisqali (ribociclib) • batoprotafib (TNO155) • nazartinib (EGF816)
4years
Clinical • Trial completion • Combination therapy
|
MET (MET proto-oncogene, receptor tyrosine kinase)
|
EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR L861Q • EGFR G719X • EGFR S768I • EGFR T790M negative
|
Tabrecta (capmatinib) • nazartinib (EGF816)
4years
Study of Efficacy and Safety of Nivolumab in Combination With EGF816 and of Nivolumab in Combination With INC280 in Patients With Previously Treated Non-small Cell Lung Cancer (clinicaltrials.gov)
P2, N=64, Active, not recruiting, Novartis Pharmaceuticals | Recruiting --> Active, not recruiting | Trial completion date: Apr 2022 --> Dec 2021 | Trial primary completion date: Apr 2022 --> Dec 2021
Clinical • Enrollment closed • Trial completion date • Trial primary completion date • Combination therapy • PD(L)-1 Biomarker
|
EGFR (Epidermal growth factor receptor)
|
EGFR T790M
|
Opdivo (nivolumab) • Tabrecta (capmatinib) • nazartinib (EGF816)
4years
[VIRTUAL] EATON: A Phase I Dose Escalation Study of Nazartinib (EGF816) and Trametinib in Patients with EGFR Mutated Non-Small Cell Lung Cancer - Preliminary Data (DGHO 2020)
Treatment with nazartinib 100 mg QD and trametinib 1 mg QD resulted in a DLT in two of six individuals. Thus, three additional patients will be enrolled in a third cohort at the same dose level. Efficacy data are premature and needs further evaluation.
Clinical • P1 data
|
EGFR (Epidermal growth factor receptor) • MET (MET proto-oncogene, receptor tyrosine kinase)
|
EGFR mutation • MET amplification • EGFR T790M • MET mutation • EGFR mutation + EGFR T790M
|
Mekinist (trametinib) • nazartinib (EGF816)
4years
[VIRTUAL] EATON: A Phase I Dose Escalation Study of Nazartinib (EGF816) and Trametinib in Patients with EGFR Mutated Non-Small Cell Lung Cancer - Preliminary Data (DGHO 2020)
Treatment with nazartinib 100 mg QD and trametinib 1 mg QD resulted in a DLT in two of six individuals. Thus, three additional patients will be enrolled in a third cohort at the same dose level. Efficacy data are premature and needs further evaluation.
Clinical • P1 data
|
EGFR (Epidermal growth factor receptor) • MET (MET proto-oncogene, receptor tyrosine kinase)
|
EGFR mutation • MET amplification • EGFR T790M • MET mutation • EGFR mutation + EGFR T790M
|
Mekinist (trametinib) • nazartinib (EGF816)
4years
[VIRTUAL] EATON: A Phase I Dose Escalation Study of Nazartinib (EGF816) and Trametinib in Patients with EGFR Mutated Non-Small Cell Lung Cancer - Preliminary Data (DGHO 2020)
Treatment with nazartinib 100 mg QD and trametinib 1 mg QD resulted in a DLT in two of six individuals. Thus, three additional patients will be enrolled in a third cohort at the same dose level. Efficacy data are premature and needs further evaluation.
Clinical • P1 data
|
EGFR (Epidermal growth factor receptor) • MET (MET proto-oncogene, receptor tyrosine kinase)
|
EGFR mutation • MET amplification • EGFR T790M • MET mutation • EGFR mutation + EGFR T790M
|
Mekinist (trametinib) • nazartinib (EGF816)
over4years
Journal
|
EGFR (Epidermal growth factor receptor)
|
nazartinib (EGF816)
over4years
[VIRTUAL] EATON: A phase I dose-escalation trial of nazartinib (EGF816) and trametinib in EGFR-mutant NSCLC (AACR-II 2020)
Best objective response according to RECIST 1.1 was stable disease in one patient (afatinib-resistant, T790M-negative), lasting for more than 4 months and progressive disease in the other patient (osimertinib-resistant, T790M-negative). Treatment with nazartinib 100 mg QD and trametinib 1 mg QD resulted in a DLT in one of three patients. Thus, three additional patients will be enrolled at the same dose level. Efficacy data is premature.
P1 data
|
EGFR (Epidermal growth factor receptor) • MET (MET proto-oncogene, receptor tyrosine kinase)
|
EGFR mutation • EGFR L858R • MET amplification • EGFR L858R + EGFR T790M
|
Mekinist (trametinib) • Tagrisso (osimertinib) • Gilotrif (afatinib) • nazartinib (EGF816)