Cetrorelix

Description

Cetrorelix was launched in Germany for the treatment of female infertility. It is a decapeptidic analog of luteinizing hormone-releasing hormone (LH-RH) bearing structural modifications in the crucial positions 1, 2, 3, 6 and 10 : [Ac-D-Nal1, D-4-CI Phe-2, D-Pal3, D-Cit6, D-Alal0]-GnRH. Cetrorelix is an extremely potent and long acting gonadotrophin releasing hormone (GnRH) antagonist and thus blocks gonadotrophins and sex steroid secretion immediately after administration. Moreover, it has a low histamine-releasing potency. Cetrorelix will be the first LH-RH antagonist approved worldwide. In several Phase III clinical trials, female patients receiving Cetrorelix had a successful controlled ovulation thus avoiding a premature LH-surge. Cetrorelix could be a first-choice in-vitro fertilization (IVF) treatment without the complications of current controlled ovarian hyperstimulation protocols. Cetrorelix is currently under clinical investigation for the treatment of diverse sex hormone dependent disorders such as benign prostate hypertrophy, breast, ovarian or prostate cancers and diverse gynaecological disorders.

Originator

Asta Medica (Germany)

Uses

Cetrorelix Acetate is an gonadotropin-releasing hormone antagonist and is used to treat hormone-sensitive cancers of the prostate and breast.

Definition

ChEBI: Cetrorelix is a synthetic ten-membered oligopeptide comprising N-acetyl-3-(naphthalen-2-yl)-D-alanyl, 4-chloro-D-phenylalanyl, 3-(pyridin-3-yl)-D-alanyl, L-seryl, L-tyrosyl, N(5)-carbamoyl-D-ornithyl, L-leucyl, L-arginyl, L-prolyl, and D-alaninamide residues coupled in sequence. A gonadotrophin-releasing hormone (GnRH) antagonist, it is used for treatment of infertility and of hormone-sensitive cancers of the prostate and breast. It has a role as a GnRH antagonist and an antineoplastic agent.

Indications

Cetrorelix is used to delay your ovaries from releasing eggs too early (ovulation). It is indicated for the inhibition of premature LH surges in women undergoing controlled ovarian stimulation.

brand name

Cetrotide (Serono).

Side effects

Cetrorelix is usually administered by subcutaneous injection. The most common side effects include: pain, itching, swelling, discolouration or redness near the injection site; nausea and headache. Other possible effects may include: abdominal or stomach pain, reduced urine output, diarrhoea, indigestion, weight gain, pelvic pain, etc. Severe allergic reactions are rare.

Description

Cetrorelix acetate is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity. Cetrorelix acetate is an analog of native GnRH with substitutions of amino acids at positions 1, 2, 3, 6, and 10. The molecular formula is C₇₀H₉₂CIN₁₇O₁₄ (Ac-D-Nal1-D-Cpa2-D-Pal3-Ser4-Tyr5- D-Cit6-Leu7-Arg8-Pro9-D -Ala10-NH₂), and the molecular weight is 1431 Dalton, calculated as the anhydrous free base.