[Clinical effects of a 3-month formulation LH-RH agonist, TAP-144-SR (3M) in prostate cancer patients].
TAP-144-SR (3M) is a 3-month sustained releasing injection of a super-active agonist of luteinizing hormone releasing hormone (LH-RH), leuprorelin acetate. At the Department of Urology of Gunma University Hospital, TAP-144-SR (3M) was injected once subcutaneously into 10 prostatic cancer patients who had had no treatment in the past to investigate safety, serum testosterone levels, drug concentrations and efficacy. In safety, no problematic adverse reactions occurred, and the drug was well tolerated. Serum testosterone levels elevated temporarily up to 2 days after injection and then were reduced rapidly. The levels were reduced below the castration level (100 ng/dl) after 3 weeks and then remained reduced up to 12 weeks. Serum TAP-144 levels including metabolite M-I, elevated to maximal plasma concentration up to 3 hours after injection and then were maintained at about 0.2 ng/ml between 1 week and 12 weeks after injection. With respect to the anti-tumor effects, the response rate according to "criteria of prostate cancer" at 12 weeks after injection was 100% (stable response cases) and the ratio of PSA normalization at 12 weeks was 90%. These results showed that an injection of TAP-144-SR (3M) was well tolerated in prostate cancer patients having no prior treatment and inhibited serum testosterone persisting for at least 12 weeks so that TAP-144-SR (3M) was concluded to be safe and clinically effective for prostate cancer patients.
Koiso
Kenkichi
K
Senpo Tokyo Takanawa Hospital.
Yamanaka
Hidetoshi
H
Ito
Kazuto
K
Yoshinaka
Ryoji
R
Uchida
Satoshi
S
Yokokawa
Kiyoshi
K
D000368:Aged; D018931:Antineoplastic Agents, Hormonal / Q000008:administration & dosage* / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations; D007987:Gonadotropin-Releasing Hormone / Q000819:agonists*; D006801:Humans; D007279:Injections, Subcutaneous; D016729:Leuprolide / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008297:Male; D008875:Middle Aged; D011471:Prostatic Neoplasms / Q000097:blood / Q000188:drug therapy*; D013739:Testosterone / Q000097:blood; D013997:Time Factors; D016896:Treatment Outcome
D018931:Antineoplastic Agents, Hormonal; D003692:Delayed-Action Preparations; D007987:Gonadotropin-Releasing Hormone; D013739:Testosterone; D016729:Leuprolide