CRLX101 (formerly IT-101) – A Novel Nanopharmaceutical of Camptothecin in Clinical Development

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CRLX101 (formerly IT-101)–A Novel Nanopharmaceutical of Camptothecin in Clinical Development

CRLX101 (formerly IT-101) is a first-in-class nanopharmaceutical, currently in Phase 2a development, which has been developed by covalently conjugating camptothecin (CPT) to a linear, cyclodextrin-polyethylene glycol (CD-PEG) co-polymer that self-assembles into nanoparticles. As a nanometer-scale drug carrier system, the cyclodextrin polymeric nanoparticle technology, referred to as "CDP", has ...

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Polymeric Nanoparticles and Cancer: Lessons Learnt from CRLX101

CRLX101 (formerly IT-101) is a novel cyclodextrin-based polymer that selfassembles into nanoparticles. CRLX101 was designed to deliver sustained levels of the cytotoxic agent camptothecin (CPT) to tumour cells while minimizing delivery to normal tissue. Covalent conjugation of hydrophobic CPT to the cyclodextrin polymer increases its water solubility by three orders of magnitude and prevents in...

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Pharmacodynamic and pharmacogenomic study of the nanoparticle conjugate of camptothecin CRLX101 for the treatment of cancer.

CRLX101 is a nanopharmaceutical consisting of cyclodextrin-based polymer molecule and camptothecin. The CRLX101 nanoparticle is designed to concentrate and slowly release camptothecin in tumors over an extended period of time. Tumor biopsy and blood samples collected from patients with advanced solid malignancies before and after CRLX101 treatment are subjected to immunohistochemistry and pharm...

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Preclinical results of camptothecin-polymer conjugate (IT-101) in multiple human lymphoma xenograft models.

PURPOSE Camptothecin (CPT) has potent broad-spectrum antitumor activity by inhibiting type I DNA topoisomerase (DNA topo I). It has not been used clinically because it is water-insoluble and highly toxic. As a result, irinotecan (CPT-11), a water-soluble analogue of CPT, has been developed and used as salvage chemotherapy in patients with relapsed/refractory lymphoma, but with only modest activ...

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Preclinical efficacy of the camptothecin-polymer conjugate IT-101 in multiple cancer models.

Preclinical efficacy of i.v. IT-101, a nanoparticulate conjugate of 20(S)-camptothecin and a cyclodextrin-based polymer, was investigated in several mouse xenografts. The effects of different multiple dosing schedules on tumor growth of LS174T colon carcinoma xenografts are elucidated. All multiple dosing schedules administered over 15 to 19 days resulted in enhanced efficacy compared with untr...

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ژورنال

عنوان ژورنال: Current Bioactive Compounds

سال: 2011

ISSN: 1573-4072

DOI: 10.2174/157340711795163866