Last update 01 Nov 2024

HER2 x EGFR L858R x EGFR x HER4 x EGFR T790M

Last update 01 Nov 2024

Basic Info

Related Targets

HER2EGFR L858REGFR[+2]

Drugs associated with HER2 x EGFR L858R x EGFR x HER4 x EGFR T790M

JRF-103

Target

EGFR x EGFR L858R x EGFR T790M x HER2 x HER4

Mechanism

EGFR T790M inhibitors [+4]

Active Org.

Jinrui FoundationStartup [+1]

Originator Org.

Jinrui FoundationStartup

Active Indication

Advanced Malignant Solid Neoplasm [+1]

Inactive Indication-

Drug Highest PhasePhase 2

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with HER2 x EGFR L858R x EGFR x HER4 x EGFR T790M

CTR20241885 / Not yet recruitingPhase 2

评价JRF103片在晚期实体瘤患者中的安全性和有效性的开放、平行、多中心、II期临床研究

[Translation] An open, parallel, multicenter, phase II clinical study to evaluate the safety and efficacy of JRF103 tablets in patients with advanced solid tumors

评价JRF103对晚期实体瘤患者的客观缓解率

[Translation]

To evaluate the objective response rate of JRF103 in patients with advanced solid tumors

Start Date-

Sponsor / Collaborator

Jinrui FoundationStartup

CTR20210232 / RecruitingPhase 1/2

评价JRF103片在晚期实体瘤患者中的安全性、耐受性、药代动力学特征及初步有效性的开放、多中心、I/II期临床研究

[Translation] An open, multicenter, phase I/II clinical study to evaluate the safety, tolerability, pharmacokinetic characteristics and preliminary efficacy of JRF103 tablets in patients with advanced solid tumors

试验主要目的是评价JRF103片在晚期实体瘤患者的安全性和耐受性，同时评价JRF103片在晚期实体瘤患者的药代动力学特征和JRF103片的初步抗肿瘤疗效，为后续研究提供推荐剂量。

[Translation]

The main purpose of the trial is to evaluate the safety and tolerability of JRF103 tablets in patients with advanced solid tumors, as well as to evaluate the pharmacokinetic characteristics of JRF103 tablets in patients with advanced solid tumors and the preliminary anti-tumor efficacy of JRF103 tablets, and to provide recommended doses for subsequent studies.

Start Date16 Apr 2021

Sponsor / Collaborator

Jinrui FoundationStartup

ChiCTR2100043599 / SuspendedPhase 1IIT

An open, multi-center, phase I/II clinical study to evaluate the safety, tolerability, pharmacokinetic characteristics and preliminary effectiveness of JRF103 tablets in patients with advanced solid tumors

Start Date05 Mar 2021

Sponsor / Collaborator-

100 Clinical Results associated with HER2 x EGFR L858R x EGFR x HER4 x EGFR T790M

100 Translational Medicine associated with HER2 x EGFR L858R x EGFR x HER4 x EGFR T790M

0 Patents (Medical) associated with HER2 x EGFR L858R x EGFR x HER4 x EGFR T790M

Literatures (Medical) associated with HER2 x EGFR L858R x EGFR x HER4 x EGFR T790M

OncoTargets and TherapyQ4 · MEDICINE

Next-generation EGFR/HER tyrosine kinase inhibitors for the treatment of patients with non-small-cell lung cancer harboring <em>EGFR</em> mutations: a review of the evidence

Q4 · MEDICINE

ReviewOA

Author: Crowe, Philip J ; Yang, Jia-Lin ; Wang, Xiaochun ; Goldstein, David

Tyrosine kinase inhibitors (TKIs) against human epidermal growth factor receptor (EGFR/HER) family have been introduced into the clinic to treat cancers, particularly non-small-cell lung cancer (NSCLC). There have been three generations of the EGFR/HER-TKIs. First-generation EGFR/HER-TKIs, binding competitively and reversibly to the ATP-binding site of the EGFR TK domain, show a significant breakthrough treatment in selected NSCLC patients with activating EGFR mutations (actEGFRm) EGFR (L858R) and EGFR (Del19), in terms of safety, efficacy, and quality of life. However, all those responders inevitably develop acquired resistance within 12 months, because of the EGFR (T790M) mutation, which prevents TKI binding to ATP-pocket of EGFR by steric hindrance. The second-generation EGFR/HER-TKIs were developed to prolong and maintain more potent response as well as overcome the resistance to the first-generation EGFR/HER-TKIs. They are different from the first-generation EGFR/HER-TKIs by covalently binding to the ATP-binding site, irreversibly blocking enzymatic activation, and targeting EGFR/HER family members, including EGFR, HER2, and HER4. Preclinically, these compounds inhibit the enzymatic activation for actEGFRm, EGFR (T790M), and wtEGFR. The second-generation EGFR/HER-TKIs improve overall survival in cancer patients with actEGFRm in a modest way. However, they are not clinically active in overcoming EGFR (T790M) resistance, mainly because of dose-limiting toxicity due to simultaneous inhibition against wtEGFR. The third-generation EGFR/HER-TKIs selectively and irreversibly target EGFR (T790M) and actEGFRm while sparing wtEGFR. They yield promising efficacy in NSCLC patients with actEGFRm as well as EGFR (T790M) resistant to the first- and second-generation EGFR-TKIs. They also appear to have a lower incidence of toxicity due to the reduced inhibitory effect on wtEGFR. Currently, the first-generation EGFR/HER-TKIs gefitinib and erlotinib and second-generation EGFR/HER-TKI afatinib have been approved for use as the first-line treatment of metastatic NSCLC with actEGFRm. This review will summarize and evaluate a broad range of evidence of recent development of EGFR/HER-TKIs, with a focus on the second- and third-generation EGFR/HER-TKIs, in the treatment of patients with NSCLC harboring EGFR mutations.

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