DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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Chemical structure of CRLX-101
(source: Svenson S, Wolfgang M, Hwang J, Ryan J, Eliasof S. J Control Release. 2011 Jul 15;153(1):49-55. Epub 2011 Mar 23.).
CRLX101 is a novel approach to cancer chemotherapy that is currently under investigation in human trials, and is an example of ananomedicine.
The agent represents a nanoparticle conjugate that consists of a drug delivery molecule, namely a cyclodextrin-based polymer (CDP) and an anti-cancer compound (camptothecin). It was developed by Dr. Mark E. Davis, professor of Chemical Engineering at theCalifornia Institute of Technology, and associates at Insert Therapeutics, Inc., now Calando Pharmaceuticals, Inc., hence the original name “IT-101”. Its novel delivery mode allows the agent, and thus the toxic anti-cancer component, to be preferentially accumulated in cancer tissue. In turn, toxic side effect are expected to be reduced. The technology was licensed by Calando and Caltech to Cerulean Pharma Inc., in June, 2009.
CRLX101 is a camptothececin-nanoparticle conjugate, which is a novel approach to cancer chemotherapy that is currently under investigation in human trials. CRLX101 represents a nanoparticle conjugate that consists of a drug delivery molecule, namely a cyclodextrin-based polymer (CDP) and an anti-cancer compound (camptothecin). It was developed by Dr. Mark E. Davis, professor of Chemical Engineering at the California Institute of Technology, and associates at Insert Therapeutics, Inc., now Calando Pharmaceuticals, Inc., hence the original name “IT-101”. Its novel delivery mode allows the agent, and thus the toxic anti-cancer component, to be preferentially accumulated in cancer tissue. In turn, toxic side effect are expected to be reduced. The technology was licensed by Calando and Caltech to Cerulean Pharma Inc., in June, 2009. (source: http://en.wikipedia.org/wiki/CRLX101).
Camptothecin (CPT) is a potent broad-spectrum anticancer agent that acts through inhibition of topoisomerase 1. Clinical development of CPT was unsuccessful due to poor drug solubility, insufficient in vivo stability of the active form, and toxicity. In order to address these issues, a polymeric nanoparticle comprised of cyclodextrin-poly(ethylene glycol) copolymer (CDP) conjugated to CPT (CRLX101) has been developed and Phase 2 clinical studies are ongoing. Camptothecin is conjugated to the polymer in its active form at 10-12 wt.% loading. CRLX101 self-assembles in solution into nanoparticles with an apparent solubility increase of >1000-fold as compared to the parent drug camptothecin.
Current developer: Calando Pharmaceuticals, Inc/Cerulean Pharma Inc.
Cerulean Pharma has dosed the first patient in a Phase 2 study of its investigational CRLX101 drug, designed for the treatment of extensive-stage small cell lung cancer (SCLC) patients sensitive to first-line platinum-based chemotherapy.
CRLX101, a tumor-targeted nanopharmaceutical, is a dual inhibitor of topoisomerase 1 and hypoxia-inducible factor-1a and releases camptothecin over an extended period of time.
The randomized study, which is being conducted at the University of Chicago School of Medicine and affiliated institutions, has enrolled 150-patient to compare the efficacy of CRLX101 with topotecan, a second-line therapy for relapsed SCLC.
The trial has co-primary endpoints of progression-free survival (PFS) and three-month PFS rate, claims the company.
During the company’s preclinical and Phase 1/2a clinical trial, CRLX101 has demonstrated significant anti-tumor activity.
Cerulean Pharma chief medical officer Edward Garmey said the company’s clinical experience with CRLX101 shows a benign safety profile.
“The standard of care in SCLC is not well tolerated, so if we can demonstrate an efficacy benefit versus standard of care, CRLX101 would have the added benefit of improved quality of life for these very sick patients,” Garmey added.
New Drug Approvals 
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