A phase II study of pegylated-camptothecin (pegamotecan) in the treatment of locally advanced and metastatic gastric and gastro-oesophageal junction adenocarcinoma

Abstract

Pegamotecan has activity in this patient population and was generally well-tolerated. The favourable rate of haematological toxicities and diarrhoea compared with irinotecan in similar studies suggests that pegamotecan could be combined with other active agents in further studies in this disease.

Advanced targeted therapies in cancer: Drug nanocarriers, the future of chemotherapy

“…They are based on the traditional cytotoxic drugs (e.g. platinates [145,146], doxorubicin [147,148], camptothecin and analogues [149][150][151][152][153][154][155][156][157][158][159], paclitaxel/docetaxel [160][161][162][163][164], methotrexate [165], and irinotecan [166,167]). Xyotax (CT-2103 or OPAXIO), a PGA-paclitaxel conjugate, and NKTR-102, a polymer conjugate of irinotecan, are both currently in phase III clinical trials, being the conjugates closest to approval and market availability [164,[166][167][168].…”

Effects of pharmaceutical PEGylation on drug metabolism and its clinical concerns

“…Results from clinical trials showed that the conjugate was highly tolerated with significantly reduced toxicity as compared to the commercial formulation. However, quick hydrolysis in vivo of the linkage caused a parallel toxicity to that of the native drug, leading to the failure of drug development of this conjugate [49,50]. In short, the in vivo metabolism of small-molecule drugs can be manipulated through PEGylation, for example, utilizing a suitable linkage and controlling the release speed of parent drugs.…”

Synthesis and pharmacokinetic characterization of a pH-sensitive polyethylene glycol ginsenoside CK (PEG-CK) conjugate

“…PEG conjugation enhances the solubility, bioavailability, and anti-tumor activity of various anticancer drugs, including camptothecin and curcumin. 16,17) Owing to the hydrophilic nature of PEG, the prepared PEG-CK conjugate (0.7 mg) was readily soluble in 450 μL of water, whereas, due to the hydrophobic nature of free CK, it was insoluble even at much lower concentrations (Fig. 1(D)).…”