Therapy Detail
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| Therapy Name | Gefitinib |
| Synonyms | |
| Therapy Description |
Iressa (gefitinib) is a first-generation EGFR inhibitor that binds EGFR and inhibits downstream signaling, potentially resulting in decreased growth of tumors with EGFR activation (PMID: 26980062, PMID: 25302162, PMID: 15284455). Iressa (gefitinib) is FDA approved for use in patients with non-small cell lung cancer harboring an EGFR exon 19 deletion or EGFR L858R (FDA.gov). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Gefitinib | Iressa | ZD1839 | EGFR Inhibitor (Pan) 45 EGFR Inhibitor 1st gen 3 | Iressa (gefitinib) is a first-generation EGFR inhibitor that binds EGFR and inhibits downstream signaling, potentially resulting in decreased growth of tumors with EGFR activation (PMID: 26980062, PMID: 25302162, PMID: 15284455). Iressa (gefitinib) is FDA approved for use in patients with non-small cell lung cancer harboring an EGFR exon 19 deletion or EGFR L858R (FDA.gov). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| ERBB2 Y772_A775dup | lung cancer | no benefit | Gefitinib | Preclinical | Actionable | In a preclinical study, bronchial epithelial cells expressing ERBB2 (HER2) Y772_A775dup (also referred to as A775_G776insYVMA) did not demonstrate sensitivity to Iressa (gefitinib) in culture (PMID: 26545934). | 26545934 |
| ERBB2 G660D | lung cancer | no benefit | Gefitinib | Preclinical | Actionable | In a preclinical study, bronchial epithelial cells cells expressing ERBB2 (HER2) G660D did not demonstrate sensitivity to Iressa (gefitinib) in culture (PMID: 26545934). | 26545934 |
| ERBB2 G776delinsVC | lung cancer | no benefit | Gefitinib | Preclinical | Actionable | In a preclinical study, bronchial epithelial cells expressing ERBB2 (HER2) G776delinsVC did not demonstrate sensitivity to Iressa (gefitinib) in culture (PMID: 26545934). | 26545934 |
| ERBB2 G776delinsLC | lung cancer | no benefit | Gefitinib | Preclinical | Actionable | In a preclinical study, bronchial epithelial cells expressing ERBB2 (HER2) G776delinsLC did not demonstrate sensitivity to Iressa (gefitinib) in culture (PMID: 26545934). | 26545934 |
| ERBB2 P489L | cancer | no benefit | Gefitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) P489L did not demonstrate sensitivity to growth inhibition by Iressa (gefitinib) in culture (PMID: 32366937). | 32366937 |
| ERBB2 G660D | Advanced Solid Tumor | no benefit | Gefitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) G660D did not benefit from treatment with Iressa (gefitinib) in culture when compared to Erbb2 (Her2) inhibitors (PMID: 30449325). | 30449325 |
| ERBB2 G778_P780dup | lung cancer | no benefit | Gefitinib | Preclinical | Actionable | In a preclinical study, bronchial epithelial cells expressing ERBB2 (HER2) G778_P780dup (also referred to as P780_Y781insGSP) did not demonstrate sensitivity to Iressa (gefitinib) in culture (PMID: 26545934). | 26545934 |
| ERBB2 S310F | urinary bladder cancer | sensitive | Gefitinib | Preclinical - Cell culture | Actionable | In a preclinical study, a bladder cancer cell line harboring ERBB2 S310F demonstrated decreased viability when treated with Iressa (gefitinib) in culture (PMID: 31635022). | 31635022 |
| ERBB2 Q709L | Advanced Solid Tumor | no benefit | Gefitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) Q709L did not benefit from treatment with Iressa (gefitinib) in culture when compared to Erbb2 (Her2) inhibitors (PMID: 30449325). | 30449325 |
| ERBB2 L663P | Advanced Solid Tumor | no benefit | Gefitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) L663P did not benefit from treatment with Iressa (gefitinib) in culture when compared to Erbb2 (Her2) inhibitors (PMID: 30449325). | 30449325 |
| ERBB2 G660R | Advanced Solid Tumor | no benefit | Gefitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) G660R did not benefit from treatment with Iressa (gefitinib) in culture when compared to Erbb2 (Her2) inhibitors (PMID: 30449325). | 30449325 |
| ALK rearrange | lung non-small cell carcinoma | no benefit | Gefitinib | Guideline | Actionable | EGFR tyrosine kinase inhibitors including Tarceva (erlotinib), Iressa (gefitinib), Gilotrif (afatinib), and Tagrisso (osimertinib) are not indicated for use as subsequent therapy in ALK rearranged non-small cell lung cancer patients who relapsed on Alecensa (alectinib), Xalkori (crizotinib), or Zykadia (ceritinib) (NCCN.org). | detail... |
| ERBB2 V659E | Advanced Solid Tumor | predicted - resistant | Gefitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) V659E did not benefit from treatment with Iressa (gefitinib) in culture when compared to Erbb2 (Her2) inhibitors (PMID: 30449325). | 30449325 |
| ERBB2 R678Q | Advanced Solid Tumor | no benefit | Gefitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) R678Q did not benefit from treatment with Iressa (gefitinib) in culture when compared to Erbb2 (Her2) inhibitors (PMID: 30449325). | 30449325 |
| ERBB2 L755_T759del | breast cancer | sensitive | Gefitinib | Preclinical | Actionable | In a preclinical study, breast cancer cells expressing ERBB2 (HER2) L755_T759del were sensitive to treatment with Iressa (gefitinib) (PMID: 23220880). | 23220880 |
| ERBB2 G776delinsVC | lung non-small cell carcinoma | resistant | Gefitinib | Preclinical | Actionable | In a preclinical study, non-small cell lung cancer cells harboring ERBB2 (HER2) G776delinsVC demonstrated resistance to treatment with Iressa (gefitinib) in culture (PMID: 26545934). | 26545934 |
| ERBB2 L726I | breast cancer | resistant | Gefitinib | Preclinical | Actionable | In a preclinical study, an ERBB2 (HER2) L726I mutation was detected in a murine breast cancer cell line that acquired resistance to Iressa (gefitinib) in culture (PMID: 17638894). | 17638894 |
| ERBB2 R188C | cancer | no benefit | Gefitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) R188C did not demonstrate sensitivity to growth inhibition by Iressa (gefitinib) in culture (PMID: 32366937). | 32366937 |
| ERBB2 amp | lung squamous cell carcinoma | resistant | Gefitinib | Preclinical | Actionable | In a preclinical study, a lung squamous cell carcinoma cell line with ERBB2 (HER2) amplification demonstrated resistance to treatment with Iressa (gefitinib) in culture (PMID: 26545934). | 26545934 |
| ERBB2 L1157R | cancer | no benefit | Gefitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ERBB2 (HER2) L1157R did not demonstrate sensitivity to growth inhibition by Iressa (gefitinib) in culture (PMID: 32366937). | 32366937 |
| ERBB2 V659E | lung cancer | no benefit | Gefitinib | Preclinical | Actionable | In a preclinical study, bronchial epithelial cells expressing ERBB2 (HER2) V659E did not demonstrate sensitivity to Iressa (gefitinib) in culture (PMID: 26545934). | 26545934 |
| ROS1 rearrange | lung non-small cell carcinoma | no benefit | Gefitinib | Guideline | Actionable | EGFR tyrosine kinase inhibitors including Tarceva (erlotinib), Iressa (gefitinib), Gilotrif (afatinib), and Tagrisso (osimertinib) are not indicated for use as subsequent therapy in ROS1 rearranged non-small cell lung cancer patients who relapsed on Alecensa (alectinib), Xalkori (crizotinib), or Zykadia (ceritinib) (NCCN.org). | detail... |
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