Navigation Links
Phase I pharmacokinetic study of ECO-4601, a novel bifunctional targeting agent
Date:10/24/2007

SAN FRANCISCO -- Researchers report positive results from a Phase I/II clinical trial of a novel anti-cancer drug which offers two modes of action. In 26 patients with advanced solid tumors, treatment with ECO-4601 is safe and well tolerated, including at doses yielding plasma concentrations above the expected therapeutic threshold, says Pierre Falardeau, Ph.D., chief operating officer at Thallion Pharmaceuticals in Montreal, Canada. Thallion has produced and tested ECO-4601 in association with the Segal Cancer Centre of McGill University.

Falardeau says that ECO-4601 has a unique mechanism of action comprising two distinct activities. It inhibits the RAS/MAPK intracellular signaling pathway, which is mutated in many cancer types, and which is the target of several approved cancer drugs such as Erbitux, Avastin, Tarceva, Nexavar, and Sutent. However, unlike these drugs, our preclinical experiments suggest that ECO-4601 acts at a unique point within the pathway, specifically at the level of RAS itself, Falardeau said.

As a target for inhibition, RAS presented researchers with a chance to affect the signaling pathway with less fear that loops in the pathway will compensate for its loss. Because RAS sits at a crossroad of multiple signaling pathways, targeting RAS may avoid some of the redundancies inherent in intracellular signaling, Falardeau said.

The agent also binds to the peripheral benzodiazepine receptor (PBR), which is over-expressed in multiple cancers. This intracellular PBR binding may allow the drug to accumulate within tumor cells, providing a more efficient way to inhibit the RAS/MAPK signaling pathway. In other words, ECO-4601 may preferentially target and accumulate within tumor cells because of the over-expression of the PBR, Falardeau said.

In addition to its safety, the researchers also found that, while blood concentrations of the drug increased linearly along with an increase in dosage, at the end of the treatments two-week infusion, ECO-4601 was cleared from the blood relatively quickly. Therefore, there is unlikely to be drug accumulation from cycle to cycle. This is important as the drug is intended to be used chronically and if a drug accumulates, side effects and toxicities may develop, Falardeau said. The anti-tumor activity of ECO-461 is further maximized by continuous infusion, he explains.

The researchers say that of seven patients who completed three cycles of drug treatment in the dose escalation portion of the trial, six demonstrated stable disease, which Falardeau suggests is a preliminary sign of efficacy. These data, together with extensive non-clinical data and the data presented at this conference, support the continued development of ECO-4601 for the treatment of cancer, said Falardeau.


'/>"/>

Contact: Greg Lester
greg.lester@aacr.org
267-646-0554
American Association for Cancer Research
Source:Eurekalert

Related medicine news :

1. FDA approves Phase 0 trial which tests experimental drugs on humans
2. SARS-Free Taiwan to Mark End Phase of Global Fight
3. S. Africa AIDS in death phase
4. Spray on contraceptive clears Phase I trial
5. Phase 3 trials of two multi-kinase inhibitors against cancer
6. Antigenics Pharmaceuticals plans for Phase III trial of its Melanoma vaccine
7. Phase II trails of new HIV vaccine to be held in South Africa
8. Phase 1 Drug Trials on Humans to Be Made Public
9. Jalgaon: Third Phase Of Culling Operations Begin
10. Lupin Gets DCGI Nod For Phase II Clinical Trials On Desoside-P
11. Cadila to Commence Phase I Clinical Trials On ZYH2
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:4/29/2016)... , ... April 29, 2016 , ... ... by the Accreditation Council for Graduate Medical Education (ACGME) that it has received ... is the first accreditation of three residency programs that Memorial is currently pursuing, ...
(Date:4/29/2016)... ... April 29, 2016 , ... ... of our nation’s productivity, stability, even security. Most importantly, employees are the single ... Then why are American workers so unhappy? , Just under half of American ...
(Date:4/29/2016)... ... , ... Coast Dental Fort Stewart is celebrating its grand opening with an ... Furniture Mall at 112 Vilseck Road in Fort Stewart. There will be refreshments, giveaways, ... have the opportunity to meet general dentists Thomas Richards, DDS, and Josh Faulk, DMD, ...
(Date:4/29/2016)... ... 29, 2016 , ... Mobility Designed is redefining mobility with their patent ... M+D Crutch evenly distributes body weight from the elbow to the forearm. In ... crutches than with other crutches. , Co-founders Max and Liliana Younger were inspired to ...
(Date:4/29/2016)... ... ... Dr. Robert Mondavi, one of the dentists in Torrance , is ... field as more patients are discovering the many different ways they can change and ... available to them and which ones might work for their smiles. , “One ...
Breaking Medicine News(10 mins):
(Date:4/29/2016)... , April 29, 2016 ... Life Sciences, Product Development Capabilities in ... Customer Base . Indegene ( ... announced the acquisition of Skura Corporation,s life science ... in adaptive sales enablement technology for life science ...
(Date:4/28/2016)... 28, 2016   Click here for supplemental ... (NYSE: DPLO), the nation,s largest independent specialty pharmacy, ... agreement to acquire Valley Campus Pharmacy, Inc., doing ... leading specialty pharmacy that provides individualized patient care, ... . In 2015, TNH generated approximately $400 million ...
(Date:4/28/2016)... Dr. ... und Stephen Schmidt werden Teil ... ein führender Anbieter cloudbasierter Softwarelösungen für den ... neue Führungskräfte zum Team Sicherheit und Pharmakovigilanz ... Erfahrungen mitbringen.  Dies wird die Geschäftseinheit Sicherheit ...
Breaking Medicine Technology: