Drug Class Detail

Drug Class EGFR Inhibitor (Pan)

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Epitinib HMPL-813 EGFR Inhibitor (Pan) 38 HMPL-813 (Epitinib) is a small molecule inhibitor of EGFR, including T790M (J Clin Oncol 31, 2013 (suppl; abstr e19042).
BGB-283 BRAF Inhibitor 18 EGFR Inhibitor (Pan) 38 BGB-283 is a dual RAF kinase and EGFR inhibitor, which may lead to decreased tumor cell proliferation and reduced growth of tumors with activation of BRAF and/or EGFR (PMID: 26208524).
S-222611 EGFR Inhibitor (Pan) 38 HER2 Inhibitor 20 S-222611 is a dual inhibitor of EGFR and ERBB2 (HER2), leading to decreased kinase activity and potentially inhibiting growth of tumors expressing EGFR and/or ERBB2 (HER2) (PMID: 24837299).
TAS6417 EGFR Inhibitor (Pan) 38 TAS6417 is a small molecule that inhibits EGFR and has selectivity for EGFR mutations including exon 20 insertions, resulting in decreased EGFR signaling and potentially leading to decreased growth of EGFR-mutant tumors (PMID: 29748209).
Sapitinib AZD8931|AZD89311 EGFR Inhibitor (Pan) 38 HER2 Inhibitor 20 HER3 Inhibitor 2 Sapitinib (AZD8931) binds to and inhibits the ERBB family members EGFR, ERBB2 (HER2), and ERBB3, which may lead to decreased tumor cell proliferation and increased apoptosis (PMID: 20145185).
ZM39923 ZM449829 EGFR Inhibitor (Pan) 38 JAK1 Inhibitor 8 JAK3 Inhibitor 4 ZM39923 is the prodrug of ZM449829, an inhibitor of JAK1/3, TGM2, and EGFR (PMID: 18804034, PMID: 10741557).
AP32788 TAK-788 EGFR Inhibitor (Pan) 38 HER2 Inhibitor 20 AP32788 inhibits EGFR and ERBB2 (HER2), with selectivity for mutant forms including EGFR exon 20 insertions, potentially resulting in growth inhibition in EGFR or ERBB2-mutant cancer cells (AACR, Cancer Res: April 2016; Volume 57, Abstract #2644).
Varlitinib ARRY-334543|ARRY-543 EGFR Inhibitor (Pan) 38 HER2 Inhibitor 20 Varlitinib is a selective inhibitor of EGFR and ERBB2 (HER2), which inhibits downstream signaling, potentially resulting in decreased tumor cell proliferation and increased cell death (NCI Drug Dictionary).
Vandetanib Caprelsa ZD6474 ABL1 Inhibitor 4 EGFR Inhibitor (Pan) 38 RET Inhibitor 36 SRC Inhibitor 26 VEGFR Inhibitor (Pan) 30 Caprelsa (vandetanib) is a multi-tyrosine kinase inhibitor with activity against VEGFR, EGFR, RET, SRC, and ABL1 kinases, potentially resulting in decreased tumor growth (PMID: 25031937, PMID: 25490448). Caprelsa (vandetanib) is FDA approved for use in medullary thyroid cancer (FDA.gov).
EKI-285 CL-387,785|CL-387785 EGFR Inhibitor (Pan) 38 EKI-285 is a small molecule inhibitor of EGFR, leading to decreased growth of EGFR-expressing tumors (PMID: 10086326, PMID: 11818567).
EAI045 EGFR Inhibitor (Pan) 38 EAI045 is a 4th generation epidermal growth factor receptor (EGFR) inhibitor that selectively inhibits L858R/T790M-mutant EGFR, resulting in inhibition of tumor cell proliferation (PMID: 27251290).
BMS-690514 EGFR Inhibitor (Pan) 38 HER2 Inhibitor 20 VEGFR Inhibitor (Pan) 30 BMS-690514 is a pan-EGFR/VEGFR inhibitor, which may result in increased tumor cell apoptosis, and decreased tumor cell proliferation and angiogenesis (PMID: 21531814, PMID: 17616683).
CLM3 EGFR Inhibitor (Pan) 38 RET Inhibitor 36 VEGFR2 Inhibitor 34 CLM3 is an small molecule multi-kinase inhibitor with activity against several kinases including Ret, Vegfr2, and Egfr, which potentially leads to decreased tumor cell growth (PMID: 21459081, PMID: 24423321).
Poziotinib HM781-36B|NOV120101 EGFR Inhibitor (Pan) 38 HER inhibitor (Pan) 6 Poziotinib (HM781-36B) is a pan-ErbB inhibitor that inhibits EGFR (HER1), ERBB2 (HER2) and ERBB4 (HER4), thereby reducing proliferation of tumor cells that overexpress these receptors (PMID: 21306821).
Brigatinib Alunbrig AP26113 ALK Inhibitor 19 EGFR Inhibitor (Pan) 38 FLT3 Inhibitor 48 IGF-1R Inhibitor 17 ROS1 Inhibitor 14 Alunbrig (brigatinib) is a multi-kinase inhibitor with selected activity against ALK, ROS1 fusions, FLT3, IGF1R and mutant EGFR, potentially resulting in decreased tumor growth (PMID: 27780853). Alunbrig (brigatinib) is FDA approved for use in patients with ALK-positive non-small cell lung cancer who have progressed on or are intolerant to crizotinib (FDA.gov).
Lapatinib Tykerb FMM EGFR Inhibitor (Pan) 38 HER2 (ERBB2) Antibody 26 Tykerb (lapatinib) reversibly inhibits ERBB2 (HER2) and EGFR, resulting in decreased downstream signaling and potentially leading to reduced tumor growth (PMID: 22477724). Tykerb (lapatinib) is FDA approved for ERBB2 (HER2)-positive breast cancer (FDA.gov).
Ibrutinib Imbruvica PCI-32765 BTK inhibitor 20 EGFR Inhibitor (Pan) 38 HER2 Inhibitor 20 Imbruvica (ibrutinib) is a selective, irreversible inhibitor of Bruton's tyrosine kinase (BTK), which promotes apoptosis and inhibits B-cell mediated signaling pathways, and has additional activity against ERBB2 (HER2) and EGFR (PMID: 20615965, PMID: 21422473, PMID: 27678331). Imbruvica (Ibrutinib) is approved for mantle cell lymphoma and first line treatment of chronic lymphocytic leukemia (FDA.gov).
JANEX-1 WHI-P131 EGFR Inhibitor (Pan) 38 JAK3 Inhibitor - ATP competitive 4 JANEX-1 (WHI-P131) is a dual JAK3/EGFR inhibitor, whic may prevent the development of intestinal tumors (PMID: 20924972, PMID: 20486473).
Pelitinib EKB-569 EGFR Inhibitor (Pan) 38 HER2 Inhibitor 20 Pelitinib is a nonselective inhibitor of EGFR, ERBB2 (HER2), and HER4, which induces apoptosis and inhibits cell proliferation (NCI Drug Dictionary).
Gefitinib Iressa ZD1839 EGFR Inhibitor (Pan) 38 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).
unspecified EGFR tyrosine kinase inhibitor EGFR Inhibitor (Pan) 38
Canertinib CI-1033 EGFR Inhibitor (Pan) 38 HER inhibitor (Pan) 6 Canertinib (CI-1033) is a pan-ERBB inhibitor that inhibits EGFR, ERBB2 (HER2), ERBB3 (HER3), and ERBB4 (HER4) signaling, which may result in decreased tumor growth (PMID: 11706399, PMID: 17342332).
Tyrphostin B42 AG-490 EGFR Inhibitor (Pan) 38 JAK2 Inhibitor 17 Tyrphostin B42 (AG-490) is an inhibitor of EGFR and JAK2, which inhibits cell proliferation (PMID: 1676428, PMID: 8628398).
XL647 KD019|Tesevatinib EGFR Inhibitor (Pan) 38 EPHB4 Inhibitor 6 HER2 Inhibitor 20 VEGFR2 Inhibitor 34 VEGFR3 Inhibitor 5 XL647 is an inhibitor of multiple receptor tyrosine kinases, including ERBB2 (HER2), EGFR, VEGFR2 and VEGFR3, and EphB4, potentially resulting in decreased tumor growth and angiogenesis (PMID: 17575237).
AZD3759 EGFR Inhibitor (Pan) 38 AZD3759 inhibits EGFR, potentially resulting in decreased growth of EGFR-expressing tumors (NCI Drug Dictionary).
TAK-285 EGFR Inhibitor (Pan) 38 HER2 Inhibitor 20 TAK-285 inhibits EGFR, ERBB2 (HER2), and ERBB4, resulting in decreased tumor cell growth (PMID: 23983820).
CUDC-101 EGFR Inhibitor (Pan) 38 HDAC Inhibitor 34 HER2 Inhibitor 20 CUDC-101 is a small-molecule inhibitor of EGFR, ERBB2 (HER2), and class I and II HDACs, which has demonstrated activity in EGFR-inhibitor resistant tumor cell lines (PMID: 20388807, PMID: 23536719).
Hemay022 EGFR Inhibitor (Pan) 38 Hemay022 inhibits EGFR, potentially resulting in decreased growth of EGFR over expressing tumors (NCI Drug Dictionary).
Afatinib Gilotrif BIBW 2992 EGFR Inhibitor (Pan) 38 EGFR Inhibitor 2nd gen 3 HER inhibitor (Pan) 6 HER3 Inhibitor 2 Gilotrif (afatinib) is a second-generation pan-Egfr inhibitor with activity against EGFR T790M and EGFR exon 19 and 21 deletions, and also inhibits ERBB2 (HER2), ERBB3 (HER3), ERBB4 (HER4) (PMID: 24435321, PMID: 25505694). Gilotrif (afatinib) is FDA approved for use in non-small cell lung cancer patients harboring non-resistant EGFR mutations, including exon 19 deletions, L858R, S768I, G719X, and L861Q, and for patients with metastatic squamous NSCLC (FDA.gov).
JNJ-26483327 EGFR Inhibitor (Pan) 38 HER2 Inhibitor 20 RET Inhibitor 36 JNJ-26483327 is a multi-kinase inhbitor, which inhibits wild-type and mutant EGFR, RET, and has activity against VEGFR3, ERBB2 (HER2), ERBB4, and SRC family members (PMID: 20823884).
AEE788 EGFR Inhibitor (Pan) 38 HER2 Inhibitor 20 AEE788 is a multi-kinase inhibitor with activity against EGFR and ERBB2 (HER2), which reduces kinase activity resulting in decreased tumor cell proliferation (PMID: 15256466)
AC480 BMS-599626 EGFR Inhibitor (Pan) 38 HER2 Inhibitor 20 AC480 is an inhibitor of EGFR and ERBB2 (HER2), which may prevent downstream signaling and inhibit the proliferation of tumor cells that overexpress these receptors (PMID: 17062696).
Erlotinib Tarceva CP358774 EGFR Inhibitor (Pan) 38 EGFR Inhibitor 1st gen 3 Tarceva (erlotinib) is a first-generation EGFR inhibitor, which is FDA approved for non-small cell lung carcinoma patients with EGFR exon 19 deletions and/or EGFR L858R and in combination with gemcitabine for patients with advanced pancreatic cancer (FDA.gov; PMID: 25302162).
AV-412 MP-412 EGFR Inhibitor (Pan) 38 EGFR Inhibitor 2nd gen 3 HER2 Inhibitor 20 AV-412 binds and inhibits EGFR and ERBB2 (HER2), which may result in the inhibition of tumor growth and angiogenesis in EGFR/HER2-expressing tumors (PMID: 17888033).
PR610 EGFR Inhibitor (Pan) 38 HER2 Inhibitor 20 PR610 is a prodrug that is converted to a pan-HER inhibitor in hypoxic tumor conditions, thus inhibiting cellular proliferation and differentiation of tumor cells overexpressing HER kinases and potentially sparing healthy normal tissue (NCI Drug Dictionary).
Tarloxotinib TRLX EGFR Inhibitor (Pan) 38 HER2 Inhibitor 20 Tarloxotinib (TRLX) is a prodrug that is converted to an irreversible Egfr/Erbb2 (Her2) inhibitor under hypoxia, thus inhibits tumor cell growth (Mol Cancer Ther 2018;17(1 Suppl):Abstract nr A157).
EGFR Antisense DNA EGFR Inhibitor (Pan) 38 EGFR antisense DNA is synthetic DNA that runs antisense to the EGFR sequence and suppresses endogenous EGFR expression, potentially resulting in decreased tumor cell proliferation (NCI Drug Dictionary).
Theliatinib HMPL-309 EGFR Inhibitor (Pan) 38 Theliatinib is a selective, ATP-competitive Egfr inhibitor that demonstrates anti-tumor activity in animal models (PMID: 28881608).
Molecular Profile Protein Effect Treatment Approaches