folate-tubulysin (EC1456) / Novartis - LARVOL DELTA

Phase 1 Dose Escalation Study of the Folate Receptor-Targeted Small Molecule Drug Conjugate EC1456 (ESMO 2017) - No abstract available.

P1 data • Oncology

Phase 1 dose escalation study of the folate receptor-targeted small molecule drug conjugate EC1456. (ASCO 2017) - P1; "All Part A EC1456 schedules have been well tolerated. RP2 dose for BIW is 6.0 mg/m2 and QW is 12.5 mg/m2; dose escalation is ongoing for CWD and QIW. Early signs of efficacy in an unselected pt population may be suggested by durable stable disease."

Clinical • P1 data • Biosimilar • Non Small Cell Lung Cancer • Pain

Pre-clinical studies of EC2629, a highly potent folate- receptor-targeted DNA crosslinking agent. (PubMed, Sci Rep) - "Folate receptor (FR)-targeted small molecule drug conjugates (SMDCs) have shown promising results in early stage clinical trials with microtubule destabilizing agents, such as vintafolide and EC1456...Complete responses were also observed against FR-positive paclitaxel (KB-PR) and cisplatin (KB-CR) resistant models. When evaluated against FR-positive patient derived xenograft (PDX) models of ovarian (ST070), endometrial (ST040) and triple negative breast cancers (ST502, ST738), EC2629 showed significantly greater anti-tumor activity compared to their corresponding standard of care treatments. Taken together, these studies thus demonstrated that EC2629, with its distinct DNA reacting mechanism, may be useful in treating FR-positive tumors, including those that are classified as drug resistant."

Journal • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer

Folic Acid-Tubulysin Conjugate EC1456 In Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1; N=N/A; Recruiting; Sponsor: Endocyte

Clinical • New P1 trial

Folic Acid-Tubulysin Conjugate EC1456 In Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1; N=93; Completed; Sponsor: Endocyte; Active, not recruiting ➔ Completed; Trial completion date: Jul 2018 ➔ Apr 2018

Clinical • Trial completion • Trial completion date

Pre-clinical evaluation of EC1456, a folate-tubulysin anti-cancer therapeutic. (PubMed, Sci Rep) - "Combinations of low dose EC1456 with standard of care agents such as platins, taxanes, topotecan and bevacizumab, safely and significantly augmented the growth inhibitory effects of these commonly used agents. When tested against FR-positive human tumor xenograft models having confirmed resistance to a folate-vinca alkaloid (vintafolide), cisplatin or paclitaxel, EC1456 was found to generate partial to curative responses. Taken together, these studies demonstrate that EC1456 has significant anti-proliferative activity against FR-positive tumors, including models which were anticancer drug resistant, thereby justifying a Phase 1 trial of this agent for the treatment of advanced human cancers."

Journal

An Exploratory Study of the Folic Acid-tubulysin Conjugate EC1456 in Ovarian Cancer Subjects Undergoing Surgery (clinicaltrials.gov) - P1; N=3; Completed; Sponsor: Endocyte; Active, not recruiting ➔ Completed

Clinical • Trial completion