Buserelin

Therapeutic

Used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, estrogen-dependent conditions (such as endometriosis or uterine fibroids), and in assisted reproduction.

Structural features

SMILES

CCN=C(O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)N=C(O)[C@H](CC(C)C)N=C(O)[C@@H](COC(C)(C)C)N=C(O)[C@H](CC1=CC=C(O)C=C1)N=C(O)[C@H](CO)N=C(O)[C@H](CC1=CNC2=CC=CC=C12)N=C(O)[C@H](CC1=CN=CN1)N=C(O)[C@@H]1CCC(O)=N1

Sequence

XHWSYXLRP-NHEt

Molar mass

1239.447 g/mol

Constitutional members:

9

Natural amino acids

7

D-Amino acids

1

N-terminus

pyroglutamyl

C-terminus

NHEt

Cyclic

no

Members/cycle

N.A.

Bond to form cycle

N.A.

Lipidation

no

Glycosylation

no

Route of administration

NASAL, SC

Terminal half-life

50-80 min (IV), 80 min (SC), 1-2hour (NS)

Protein binding

0.15

Absorption and Bioavailability

Buserelin is water soluble and readily absorbed after subcutaneous injection (70% bioavailable). However, bioavailability after oral absorption. When administered correctly via the nasal route, it may be absorbed in the nasal mucosa to achieve sufficient plasma levels.

References