Background:

Oleandomycin is an antibiotic produced by strains of Streptomyces.

In vitro: Oleandomycin has been identified as a macrolide antibiotic demonstrating antimicrobial activity similar to penicillin and erythromycin. In addition, oleandomycin structurally has a macrocyclic lactone ring of 14 carbon atoms with one sugar, oleandrose, and one amino sugar, desoxamine [1].

In vivo: The PK of oleandomycin after i.v. and po administration, both alone and after i.m. pretreatment with metamizole or dexamethasone, was studied in healthy dogs. Results showed that after i.v. injection of oleandomycin alone at 10 mg/kg, the t1/2β, Vd, Cl and AUC were 1.60 h, 1.11 L/kg, 7.36 ml/kg/min and 21.66 μg h/ml, respectively. There were no statistically significant differences following pretreatment with metamizole or dexamethasone. In addition, after po administration of oleandomycin alone, the t1/2β, Cmax, tmax), MAT and Fabs were 1.68 h, 5.34 μg/ml, 1.5 h, 1.34 h and 84.29%, respectively, and the pretreatment with metamizole showed a significantly decreased value for Cmax but the MAT was increased significantly. Statistically significant changes in the PK parameters of oleandomycin following po administration were also seen as a result of pretreatment with dexamethasone. The Cmax was increased and the tmax and MAT were lower [2].

Clinical trial: Up to now, oleandomycin is still in the preclinical development stage.

参考文献:
[1] C.  Vilches, C. Méndez, C. Hardisson, et al. Biosynthesis of oleandomycin by Streptomyces antibioticus: Influence of nutritional conditions and development of resistance. J.Gen.Microbiol. 136(8), 1447-1454 (1990).
[2] Milanova A, Lashev L.  Pharmacokinetics of oleandomycin in dogs after intravenous or oral administration alone and after pretreatment with metamizole or dexamethasone. Vet Res Commun. 2002 Jan;26(1):61-71.