| Stereochemistry | ABSOLUTE |
| Molecular Formula | C29H48O4 |
| Molecular Weight | 460.689 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 6 / 6 |
| E/Z Centers | 2 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]1(CC[C@@]2([H])\C(CCC[C@]12C)=C\C=C3\C[C@@H](O)C[C@H](O)C3=C)[C@@H](C)OCCCC(O)(CC)CC
InChI
InChIKey=KLZOTDOJMRMLDX-YBBVPDDNSA-N
InChI=1S/C29H48O4/c1-6-29(32,7-2)16-9-17-33-21(4)25-13-14-26-22(10-8-15-28(25,26)5)11-12-23-18-24(30)19-27(31)20(23)3/h11-12,21,24-27,30-32H,3,6-10,13-19H2,1-2,4-5H3/b22-11+,23-12-/t21-,24-,25-,26+,27+,28-/m1/s1
Lexacalcitol (KH1060) is over 100 times more active than 1alpha,25-dihydroxyvitamin D3 and is of potential interest in the treatment of psoriasis and other diseases characterized by accelerated cell growth and T lymphocyte activation, which was studied in the clinical trial. KH1060 also prevents type I diabetes in the preclinical investigation without significant effects on calcium or bone metabolism. In addition also was shown that neuroblastoma (NB) cell lines were more susceptible to growth inhibition by KH1060, suggesting its possible use in NB to potentiate the action of retinoids, which are in clinical use for this disease. The underlying biochemical reasons for the increased biological activity of KH1060 are unknown, but it can include 1) metabolic considerations in addition to explanations based upon 2) enhanced stability of KH1060-liganded transcriptional complexes.
Originator
Approval Year
Sourcing
PubMed
Patents
Sample Use Guides
It was investigated the possible synergistic effect exerted by Cyclosporin A (CsA) in combination with KH 1060 (Lexacalcitol), on the proliferative response of T lymphocytes obtained from active ulcerative colitis patients. The T lymphocyte-enriched population was treated with phytohemagglutinin and CsA (doses from 1 ng to 1000 ng/ml) alone or in association with KH 1060 (0.1, 1, 10 nM final concentration). Cell proliferation was determined by [3H]thymidine incorporation and analyzed on day 5 of culture. There was obtained the lowest CsA dose and the lowest KH 1060 concentration, in addition, there was suggested an alternative therapeutic approach in these patients, reducing the dose, and consequently the toxicity, of CsA.
ACTIVE MOIETY
