Telavancin

Therapeutic

For the treatment of complicated skin and skin structure infections (cSSSI) caused by gram-positive bacteria like methicillin-susceptible or -resistant Staphylococcus aureus, vancomycin-susceptible Enterococcus faecalis, and Streptococcus pyogenes, Streptococcus agalactiae, or Streptococcus anginosus group. Also for the treatment of adult patients with hospital-acquired bacterial pneumonia (HAP) and ventilator-associated bacterial pneumonia (VAP), known or suspected to be caused by susceptible isolates of Staphylococcus aureus (including methicillin-susceptible and methicillin-resistant S. aureus).

Structural features

SMILES

CCCCCCCCCCNCCN[C@]1(C[C@@H](O[C@H]([C@H]1O)C)O[C@@H]2[C@H]([C@@H]([C@H](O[C@H]2OC3=C4C=C5C=C3OC6=C(C=C(C=C6)[C@H]([C@H](C(=O)N[C@H](C(=O)N[C@H]5C(=O)N[C@@H]7C8=CC(=C(C=C8)O)C9=C(C(=C(C=C9[C@H](NC(=O)[C@H]([C@@H](C1=CC(=C(O4)C=C1)Cl)O)NC7=O)C(=O)O)O)CNCP(=O)(O)O)O)CC(=O)N)NC(=O)[C@@H](CC(C)C)NC)O)Cl)CO)O)O)C

Sequence

-

Molar mass

1755.65 g/mol

Constitutional members:

N.A.

Natural amino acids

N.A.

D-Amino acids

N.A.

N-terminus

CH3

C-terminus

COOH

Cyclic

yes

Members/cycle

multicyclic

Bond to form cycle

C-O-C; C-C

Lipidation

yes

Glycosylation

yes - 2 sugars

Route of administration

IV

Terminal half-life

 8 ± 1.5 hours

Protein binding

>90%

Absorption and Bioavailability

Telavancin has poor bioavailability and must be administered over 30-120 minutes IV.

References