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Therapy Name | Pyrotinib |
Synonyms | |
Therapy Description |
Pyrotinib inhibits EGFR and ERBB2 (HER2), potentially resulting in decreased growth of EGFR and/or HER2-positive tumors (NCI Drug Dictionary). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Pyrotinib | SHR-1258|SHR1258 | EGFR Inhibitor (Pan) 47 HER2 Inhibitor 26 | Pyrotinib is an irreversible dual inhibitor of EGFR and ERBB2 (HER2), which potentially leads to decreased growth of EGFR and/or HER2-positive tumor cells (PMID: 28115222, PMID: 30596880). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
ERBB2 exon20 | lung non-small cell carcinoma | predicted - sensitive | Pyrotinib | Phase II | Actionable | In a Phase II trial, non-small cell lung cancer patients harboring an ERBB2 exon 20 mutation demonstrated an objective response rate of 53.3% (8/15) and a median progression-free survival of 6.4 months when treated with Pyrotinib (PMID: 30596880; NCT02535507). | 30596880 |
ERBB2 G778_S779insLPS | Advanced Solid Tumor | sensitive | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) G778_S779insLPS in culture (PMID: 31588020). | 31588020 |
ERBB2 D769N | Advanced Solid Tumor | sensitive | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) D769N in culture (PMID: 31588020). | 31588020 |
ERBB2 act mut | lung non-small cell carcinoma | predicted - sensitive | Pyrotinib | Phase II | Actionable | In a Phase II trial, Pyrotinib treatment resulted in an objective response rate of 30% (18/60), with 55% (33/60) demonstrating stable disease, median duration of response of 6.9 mo, and median progression-free survival of 6.9 mo, and median overall survival of 14.4 mo in non-small cell lung cancer patients harboring ERBB2 (HER2) activating mutations, including exon 20 insertions and mutations occurring at L755, G776, and V777, who had received prior platinum-based chemotherapy (PMID: 32614698; NCT02834936). | 32614698 |
ERBB2 Y772_A775dup | lung non-small cell carcinoma | sensitive | Pyrotinib | Case Reports/Case Series | Actionable | \In a Phase II trial, Pyrotinib treatment led to an objective response rate of 50% (5/10) and a progression-free survival of 4.1 mon., in non-small cell lung cancer patients harboring ERBB2 (HER2) Y772_A775dup (also referred to as A775_G776insYVMA, M774_A775insAYVM, E770_A771insAYVM, E770delinsEAYVM), and reduced cell viability in patient-derived organoids, and inhibited tumor growth and induced regression in patient-derived xenograft (PDX) models (PMID: 30596880; NCT02535507). | 30596880 |
ERBB2 Y772_A775dup | lung non-small cell carcinoma | sensitive | Pyrotinib | Phase II | Actionable | In a Phase II trial, Pyrotinib treatment resulted in an objective response rate of 27.3% (12/44) in non-small cell lung cancer patients harboring ERBB2 (HER2) Y772_A775dup (also reported as A775_G776insYVMA or M774_A775insAYVM) who had received prior platinum-based chemotherapy (PMID: 32614698; NCT02834936). | 32614698 |
ERBB2 over exp | estrogen-receptor positive breast cancer | predicted - sensitive | Pyrotinib | Case Reports/Case Series | Actionable | In a clinical case study, Pyrotinib treatment resulted in stable disease for 4 months in a patient with advanced metastatic ER-positive, ERBB2 (HER2)-overexpressing breast cancer (PMID: 32547945). | 32547945 |
ERBB2 D769H | Advanced Solid Tumor | sensitive | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) D769H in culture (PMID: 31588020). | 31588020 |
ERBB2 G778_P780dup | lung non-small cell carcinoma | predicted - sensitive | Pyrotinib | Case Reports/Case Series | Actionable | In a Phase II trial, Pyrotinib treatment resulted in an objective response rate of 60% (3/5) in non-small cell lung cancer patients harboring ERBB2 (HER2) G778_P780dup (also reported as P780_Y781insGSP) who had received prior platinum-based chemotherapy (PMID: 32614698; NCT02834936). | 32614698 |
ERBB2 G778_P780dup | lung non-small cell carcinoma | predicted - sensitive | Pyrotinib | Case Reports/Case Series | Actionable | In a Phase II trial, a patient with non-small cell lung cancer harboring ERBB2 G778_P780dup (also reported as P780_Y781insGSP) demonstrated stable disease and progression-free survival for more than one year when treated with Pyrotinib (PMID: 30596880; NCT02535507). | 30596880 |
ERBB2 V777L | lung non-small cell carcinoma | predicted - sensitive | Pyrotinib | Case Reports/Case Series | Actionable | In a Phase II trial, a non-small cell lung cancer patient harboring ERBB2 (HER2) V777L who had received prior platinum-based chemotherapy demonstrated a partial response when treated with Pyrotinib (PMID: 32614698; NCT02834936). | 32614698 |
ERBB2 G778_P780dup | lung adenocarcinoma | predicted - sensitive | Pyrotinib | Case Reports/Case Series | Actionable | In a clinical study, three lung adenocarcinoma patients harboring ERBB2 (HER2) G778_P780dup (also reported as V777_G778insGSP) demonstrated a clinical benefit when treated with Pyrotinib, including a patient with three months of stable disease who had progressed on several prior lines of therapy, a patient with an ongoing partial response of six months, and a patient with an ongoing partial response of eight months who had prior disease progression with Gilotrif (afatinib) (PMID: 32036069). | 32036069 |
ERBB2 L786V | Advanced Solid Tumor | sensitive | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) L786V in culture (PMID: 31588020). | 31588020 |
ERBB2 L869R | Advanced Solid Tumor | sensitive | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) L869R in culture (PMID: 31588020). | 31588020 |
ERBB2 G776delinsVC | lung non-small cell carcinoma | predicted - sensitive | Pyrotinib | Case Reports/Case Series | Actionable | In a Phase II trial, a patient with non-small cell lung cancer harboring ERBB2 G776delinsVC demonstrated a partial response and an ongoing progression-free survival when treated with Pyrotinib (PMID: 30596880; NCT02535507). | 30596880 |
ERBB2 L755S | Advanced Solid Tumor | resistant | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) L755S were resistant to Pyrotinib in culture (PMID: 31588020). | 31588020 |
ERBB2 V773M | Advanced Solid Tumor | sensitive | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) V773M in culture (PMID: 31588020). | 31588020 |
ERBB2 G776delinsIC | lung non-small cell carcinoma | no benefit | Pyrotinib | Case Reports/Case Series | Actionable | In a Phase II trial, a patient with non-small cell lung cancer harboring ERBB2 G776delinsIC did not respond to treatment with Pyrotinib and developed progressive disease (PMID: 30596880; NCT02535507). | 30596880 |
ERBB2 G776delinsVC | Advanced Solid Tumor | conflicting | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, Pyrotinib inhibited growth of transformed cells expressing ERBB2 (HER2) G776delinsVC in culture (PMID: 30527195). | 30527195 |
ERBB2 G776delinsVC | Advanced Solid Tumor | conflicting | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC were resistant to Pyrotinib in culture (PMID: 31588020). | 31588020 |
ERBB2 L755P | lung non-small cell carcinoma | predicted - sensitive | Pyrotinib | Case Reports/Case Series | Actionable | In a Phase II trial, a patient with non-small cell lung cancer harboring ERBB2 L755P demonstrated a partial response when treated with Pyrotinib (PMID: 30596880; NCT02535507). | 30596880 |
ERBB2 L755P | lung non-small cell carcinoma | predicted - sensitive | Pyrotinib | Case Reports/Case Series | Actionable | In a Phase II trial, Pyrotinib treatment resulted in an objective response rate of 25% (1/4) in non-small cell lung cancer patients harboring ERBB2 (HER2) L755P who had received prior platinum-based chemotherapy (PMID: 32614698; NCT02834936). | 32614698 |
ERBB2 L755P | Advanced Solid Tumor | resistant | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) L755P were resistant to Pyrotinib in culture (PMID: 31588020). | 31588020 |
ERBB2 D769Y | Advanced Solid Tumor | sensitive | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) D769Y in culture (PMID: 31588020). | 31588020 |
ERBB2 G776C | lung non-small cell carcinoma | predicted - sensitive | Pyrotinib | Case Reports/Case Series | Actionable | In a Phase II trial, a patient with non-small cell lung cancer harboring ERBB2 G776C demonstrated a partial response when treated with Pyrotinib (PMID: 30596880; NCT02535507). | 30596880 |
ERBB2 G776delinsLC | Advanced Solid Tumor | sensitive | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) G776delinsLC in culture (PMID: 31588020). | 31588020 |
ERBB2 G778_P780dup | Advanced Solid Tumor | sensitive | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) G778_P780dup in culture (PMID: 31588020). | 31588020 |
ERBB2 Y772_A775dup | Advanced Solid Tumor | conflicting | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) Y722_A755dup were resistant to Pyrotinib in culture (PMID: 31588020). | 31588020 |
ERBB2 Y772_A775dup | Advanced Solid Tumor | conflicting | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, Pyrotinib inhibited growth of transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) in culture (PMID: 30527195). | 30527195 |
ERBB2 G776delinsVV | Advanced Solid Tumor | resistant | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVV were resistant to Pyrotinib in culture (PMID: 31588020). | 31588020 |
ERBB2 V842I | Advanced Solid Tumor | sensitive | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) V842I in culture (PMID: 31588020). | 31588020 |
ERBB2 Y772_A775dup ERBB2 C805S | Advanced Solid Tumor | resistant | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) Y772_A775dup (reported as A775_G776insYVMA) and an acquired ERBB2 (HER2) C805S were resistant to Pyrotinib in culture (PMID: 30527195). | 30527195 |
ERBB2 positive | Her2-receptor positive breast cancer | sensitive | Pyrotinib | Phase I | Actionable | In a Phase I trial, Pyrotinib treatment resulted in an objective response rate of 50% (18/36, all partial responses), and a clinical benefit rate of 61.1% (22/36), and a median progression-free survival of 35.4 weeks in patients with ERBB2 (HER2)-positive breast cancer (PMID: 28498781, NCT01937689). | detail... 28498781 |
ERBB2 G776delinsVC ERBB2 C805S | Advanced Solid Tumor | resistant | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) G776delinsVC and an acquired ERBB2 (HER2) C805S were resistant to Pyrotinib in culture (PMID: 30527195). | 30527195 |
ERBB2 G778_P780dup ERBB2 amp | lung adenocarcinoma | predicted - sensitive | Pyrotinib | Case Reports/Case Series | Actionable | In a clinical case study, Pyrotinib treatment resulted in 11 months of stable disease in a lung adenocarcinoma patient harboring ERBB2 (HER2) G778_P780dup (also reported as V777_G778insGSP) and ERBB2 (HER2) amplification (PMID: 32036069). | 32036069 |
ERBB2 mutant | lung non-small cell carcinoma | sensitive | Pyrotinib | Phase II | Actionable | In a Phase II trial, Pyrotinib treatment in non-small cell lung cancer patients harboring an ERBB2 (HER2) mutation resulted in a partial response in 54.5% (6/11) of patients and stable disease in 27.3% (3/11) of patients, and a PFS of 6.2 months (Journal of Thoracic Oncology, Vol. 12, Issue 1, S359). | detail... |
ERBB2 V777L | Advanced Solid Tumor | sensitive | Pyrotinib | Preclinical - Cell culture | Actionable | In a preclinical study, Pyrotinib inhibited survival of transformed cells expressing ERBB2 (HER2) V777L in culture (PMID: 31588020). | 31588020 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT02500199 | Phase I | Pyrotinib | Phase I Study of Pyrotinib in Patients With HER2-positive Solid Tumors | Active, not recruiting | USA | 0 |
NCT04447118 | Phase III | Pyrotinib Docetaxel | Phase 3 Study of Pyrotinib Versus Docetaxel in Patients With Advanced Non-squamous NSCLC Harboring a HER2 Exon 20 Mutation Who Failed Platinum Based Chemotherapy (PYRAMID-1) | Recruiting | USA | 2 |