Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: UMLS:C0027947 (
neutropenia
)
17,527
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Paclitaxel-lipoate (
IDD
-1040) is a conjugate formed by the chemical joining of the two compounds, by condensing a lipoic acid moiety to the C2' of paclitaxel.
IDD
-1040 was evaluated for its anti-tumor activity and potential druggability, using an in vivo non-small-cell, lung cancer (NSCLC) xenograft mouse model. In the in vivo studies,
IDD
-1040 showed a maximum tolerated dose (MTD) of 250 mg/kg compared to paclitaxel (PTX), with an MTD of 20 mg/kg. Most interesting,
IDD
-1040 demonstrated higher anti-tumor activity, and its inhibitory activity on tumor volume (cell growth) was dose-dependent. That anti-tumor activity persisted for two weeks after cessation of
IDD
-1040 treatment, as opposed to PTX cessation, after which the tumor relapsed, confirming that
IDD
-1040 exhibits superior tumor inhibition. Similar to PTX treatment, no marked body weight decrease was observed during
IDD
-1040 treatment, indicating a low toxicity profile. The increase in animal body weight noted over time was due to the increasing weight of tumors, recorded in all the mouse test groups. The results also showed that mortality rate of mice was reduced by treatment with
IDD
-1040, more so than with PTX. Furthermore, in a preliminary study on the ex vivo distribution of
IDD
-1040,
neutropenia
was primarily concentrated in the liver 1 h after injection, and most of the drug was metabolized by the liver in 24 h. All of these results demonstrate
IDD
-1040's great potential as a candidate drug for cancer treatment.
...
PMID:A Novel Paclitaxel Conjugate with Higher Efficiency and Lower Toxicity: A New Drug Candidate for Cancer Treatment. 3159 61