HORMONAL EFFECTS, TOLERABILITY, AND PRELIMINARY KINETICS IN MEN OF MK-906, A 5-ALPHA-REDUCTASE INHIBITOR

被引:28
|
作者
DESCHEPPER, PJ
IMPERATOMCGINLEY, J
VANHECKEN, A
DELEPELEIRE, I
BUNTINX, A
CARLIN, J
GRESSI, MH
STONER, E
机构
[1] Department of Pharmacology and Clinical Pharmacology, University of Leuven, School of Medicine, Leuven
[2] Cornell University Medical College, New York, NY
[3] Merck Sharp and Dohme Research Laboratories, Rahway, NJ
关键词
STEROIDS; 5-ALPHA-REDUCTASE INHIBITOR; PHARMACODYNAMICS; DIHYDROTESTOSTERONE; TESTOSTERONE; HUMAN; PHARMACOKINETICS; FINASTERIDE;
D O I
10.1016/0039-128X(91)90003-E
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The hormonal effects following the acute (single dose) administration of a 4-azasteroid inhibitor of 5-alpha-reductase (MK-906) were evaluated in 10 healthy male volunteers. Marked suppression of serum dihydrotestosterone (DHT) was observed after the administration of single doses as low as 12.5 mg. The mean percent decrease in DHT at 24 hours in the group treated with a single 25-mg dose was 56% +/- 10% compared with the baseline. The suppression of plasma DHT levels continued for up to 72 hours. This study demonstrates that administration of single oral doses (12.5 to 400 mg) of MK-906 results in a significant decrease in the conversion of testosterone to DHT.
引用
收藏
页码:469 / 471
页数:3
相关论文
共 50 条
  • [1] EFFECT OF MK-906, A SPECIFIC 5-ALPHA-REDUCTASE INHIBITOR, ON SERUM ANDROGENS AND ANDROGEN CONJUGATES IN NORMAL MEN
    RITTMASTER, RS
    STONER, E
    THOMPSON, DL
    NANCE, D
    LASSETER, KC
    [J]. JOURNAL OF ANDROLOGY, 1989, 10 (04): : 259 - 262
  • [2] EFFECTS OF FINASTERIDE (MK-906), A 5-ALPHA-REDUCTASE INHIBITOR, ON CIRCULATING ANDROGENS IN MALE-VOLUNTEERS
    GORMLEY, GJ
    STONER, E
    RITTMASTER, RS
    GREGG, H
    THOMPSON, DL
    LASSETER, KC
    VLASSES, PH
    STEIN, EA
    [J]. JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM, 1990, 70 (04): : 1136 - 1141
  • [3] EFFECTS OF LONG-TERM TREATMENT WITH FINASTERIDE (MK-906), A 5-ALPHA-REDUCTASE INHIBITOR, ON CIRCULATING LH, FSH, PROLACTIN AND ESTRADIOL
    MATZKIN, H
    CHEN, J
    LEWYSHON, O
    AYALON, D
    BRAF, Z
    [J]. HORMONE AND METABOLIC RESEARCH, 1992, 24 (10) : 498 - 499
  • [4] HORMONAL EFFECTS OF TUROSTERIDE, A 5-ALPHA-REDUCTASE INHIBITOR, IN THE RAT
    DISALLE, E
    GIUDICI, D
    BRIATICO, G
    ORNATI, G
    PANZERI, A
    [J]. JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, 1993, 46 (05): : 549 - 555
  • [5] EFFECT OF CASTRATION, DES, FLUTAMIDE, AND THE 5-ALPHA-REDUCTASE INHIBITOR, MK-906, ON THE GROWTH OF THE DUNNING RAT PROSTATIC-CARCINOMA, R-3327
    BROOKS, JR
    BERMAN, C
    NGUYEN, H
    PRAHALADA, S
    PRIMKA, RL
    RASMUSSON, GH
    SLATER, EE
    [J]. PROSTATE, 1991, 18 (03): : 215 - 227
  • [6] HORMONAL EFFECTS OF A 5-ALPHA-REDUCTASE INHIBITOR (FINASTERIDE) ON HORMONAL LEVELS IN NORMAL MEN AND IN PATIENTS WITH BENIGN PROSTATIC HYPERPLASIA
    VERMEULEN, A
    GIAGULLI, VA
    DESCHEPPER, P
    BUNTINX, A
    [J]. EUROPEAN UROLOGY, 1991, 20 : 82 - 86
  • [7] CLINICAL AND HORMONAL EFFECTS OF THE 5-ALPHA-REDUCTASE INHIBITOR FINASTERIDE IN IDIOPATHIC HIRSUTISM
    MOGHETTI, P
    CASTELLO, R
    MAGNANI, CM
    TOSI, F
    NEGRI, C
    ARMANINI, D
    BELLOTTI, G
    MUGGEO, M
    [J]. JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM, 1994, 79 (04): : 1115 - 1121
  • [8] PHARMACODYNAMICS AND TOLERABILITY OF L-654,066, A STEROID 5-ALPHA-REDUCTASE INHIBITOR, IN MEN
    DEPRE, M
    MEETER, C
    VANHECKEN, A
    LASKIN, OL
    BUNTINX, A
    DESCHEPPER, PJ
    [J]. CLINICAL PHARMACOLOGY & THERAPEUTICS, 1992, 52 (04) : 409 - 412
  • [9] EFFECT OF COMBINATION TREATMENT WITH ZANOTERONE (WIN-49596), A STEROIDAL ANDROGEN RECEPTOR ANTAGONIST, AND FINASTERIDE (MK-906), A STEROIDAL 5-ALPHA-REDUCTASE INHIBITOR, ON THE PROSTATE AND TESTES OF BEAGLE DOGS
    JUNIEWICZ, PE
    HOEKSTRA, SJ
    LEMP, BM
    BARBOLT, TA
    DEVIN, JA
    GAUTHIER, E
    FRENETTE, G
    DUBE, JY
    TREMBLAY, RR
    [J]. ENDOCRINOLOGY, 1993, 133 (02) : 904 - 913
  • [10] HORMONAL EFFECTS OF AN ORALLY ACTIVE 4-AZASTEROID INHIBITOR OF 5-ALPHA-REDUCTASE IN HUMANS
    VERMEULEN, A
    GIAGULLI, VA
    DESCHEPPER, P
    BUNTINX, A
    STONER, E
    [J]. PROSTATE, 1989, 14 (01): : 45 - 53