Drugs / AV-412
last change May 2010 re-read 3 minutes ago

AV-412

also known as Mp 412 · MP-412 DITOSYLATE

Small molecule targets EGFR, ERBB2 via inhibition

Developed for
cancer of unknown primary site · neoplasm · refractory malignant neoplasm
Investigated by
AVEO Pharmaceuticals, Inc.

Trials 2

200720082009201020112012201320142015201620172018201920202021202220232024202520262027
PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 1 NCT00551850 Oct 2007 → Oct 2009 cancer of unknown primary site, refractory malignant neoplasm AVEO Pharmaceuticals, Inc. Completed No outcome recorded
Phase 1 NCT00381654 Oct 2006 → Dec 2009 neoplasm AVEO Pharmaceuticals, Inc. Terminated No outcome recorded

News releases announcing trial results or a regulatory action · 3

DateIssuerRelease
2007-11-13 AVEO Pharmaceuticals, Inc. Results Preclinical Data Published in Cancer Science Show AVEO’s Novel Oral EGFR Inhibitor AV-412 Effective in Drug-Resistant Cancers aveooncology.com ↗
In addition, AV-412 also demonstrated significant anti-tumor effects on the ErbB2-overexpressing breast cancer KPL-4 cell line, which is resistant to gefitinib.
2007-04-17 AVEO Pharmaceuticals, Inc. Results AVEO Presents Preclinical Efficacy Data on AV-412, A Novel Oral Tyrosine Kinase Inhibitor of EGFR/HER2 for EGFR Mutant and Drug-resistant Lung Cancer aveooncology.com ↗
The results from the preclinical study showed that AV-412 is greater than 10 times more potent than erlotinib in genetically engineered lung tumor models with the EGFR L858R mutation, producing rapid and complete tumor regression at a daily dose of 1 mg/kg.
2006-04-04 AVEO Pharmaceuticals, Inc. Results AV-412 Preclinical Efficacy Data Presented at AACR 2006 aveooncology.com ↗
Importantly, AV-412 also demonstrated potent anti-tumor activity against tumors that were resistant to treatment with erlotinib and gefitinib.

Evidence & citations 8 cited values

Every value below carries the sentence it was read from. 3 sources stand behind the page.

FieldValueCited text
Known as AV 412 “AV 412 is a potent inhibitor of human epidermal growth factor family receptor tyrosine kinases (TKIs) and represents a growing class of anti-cancer agents.” NCT00381654 ↗
2

NCT00381654 ↗

NCT00551850 ↗

Known as Mp 412 ChEMBL registry synonym — accepted as the source's own label CHEMBL2138625 ↗
Known as MP-412 DITOSYLATE ChEMBL registry synonym — accepted as the source's own label CHEMBL2138625 ↗
Action Inhibit “AV 412 is a potent inhibitor of human epidermal growth factor family receptor tyrosine kinases (TKIs)” NCT00381654 ↗
1

“Receptor protein-tyrosine kinase erbB-2 inhibitor” CHEMBL2138625 ↗

Modality Small molecule — CHEMBL2138625 ↗
Route Oral “daily oral administration of AV 412” NCT00381654 ↗
Target EGFR “inhibitor of the EGFR-tyrosine kinase” NCT00551850 ↗
Target ERBB2 “Receptor protein-tyrosine kinase erbB-2 inhibitor” CHEMBL2138625 ↗