LHRH and Its Analogs: Contraceptive and Therapeutic Applications Part 2

606 Pages·1987·27.578 MB·English

by  J. J. Nestor Jr (auth.), B. H. Vickery, J. J. Nestor Jr. (eds.)

LURU
and Its Analogs
Contraceptive and Therapeutic Applications
Part 2
LHRH
and Its Analogs
contraceptive and Therapeutic Applications
Part
2
Edited by
B. H. Vickery and J. J. Nestor Jr.
MTP PRESS LIMITED
~.
~ a member of the KLUWER ACADEMIC PUBLISHERS GROUP
LANCASTER I BOSTON I THE HAGUE I DORDRECHT
Published in the UK and Europe by
MTP Press Limited
Falcon House
Lancaster, England
British Library CataloguiDg in Publication Data
LHRH and its analogs : contraceptive and
therapeutic applications
Part 2
1. Generative organs -- Diseases -
Chemotherapy 2. Luteinizing honnone
releasing hormone -- Therapeutic use
I. Vickery, B.H. II. Nestor, J.J.
615 I .766 RC877
ISBN-13: 978-94-010-7949-5 e-ISBN-13: 978-94-009-3229-6
DOl: 10.1007/978-94-009-3229-6
Published in the USA by
MTP Press
A division of Kluwer Academic Publishers
101 Philip Drive
Norwell, MA 02061, USA
Copyright 1987 MTP Press Limited
Softcover reprint of the hardcover 1st edition 1987
All rights reserved. No part of this publication may be reproduced,
stored in a retrieval system, or transmitted in any form or by any
means, electronic, mechanical, photocopying, recording or
otherwise, without prior permission from the publishers.
Contents
PART 2
TABLE OF CONTENTS
Foreword xiii
List of Contributolt'S xv
Introduction
J. J. Nestor, Jr. and B. H. Vickery xix
SECTION 1 CHEMISTRY
1. Development of LHRH antagonists
J. J. Nestor, Jr. 3
2. LHRH antagonists with low histamine releasing activity
R. W. Roeske, N. C. Chaturvedi, T. Hrinyo-Pavlina
and M. Kowalczuk 17
3. Specificity of design to achieve antagonists of LHRH of
increasing effectiveness in therapeutic activity
K. Folkers, C. Bowers, P.-F. L. Tang, D.-M. Feng,
T. Okamoto, Y. Zhang and A. Ljungqvist 25
4. Biosynthesis of LHRH
K. Nikolics and P. H. Seeburg 37
5. Phylogenetic diversity of LHRH
J. A. King and R. P. Millar 53
SECTION 2 MECHANISMS OF ACTION OF HYPOTHALAMIC
LHRH AND ANALOGS
6. Molecular mechanism of LHRH action in the gonadotrope
C. A. McArdle and P. M. Conn 77
7. Mediation of the preovulatory LH surge: LHRH
pulsatility and opioid modulation
A. L. Barkan and J. C. Marshall 101
v
PART 2 TABLE OF CONTENTS
SECTION 3 EXTRA-HYPOTHALAMIC LHRH-LIKE MATERIALS
8. LHRH binding sites in human tissues
T. A. Bramley 123
9. LHRH and "LHRH-like" factors in the male
reproductive tract
M. P. Hedger, D. M. Robertson and D. M. de Kretser 141
10. Placental LHRH-like activity
T. M. Siler-Khodr 161
SECTION 4 PHARMACOLOGY OF LHRH ANTAGONISTS
11. In vitro histamine release with LHRH analogs
M. J. Karten, W. A. Hook, R. P. Siraganian,
D. H. Coy, K. Folkers, J. E. Rivier and
R. W. Roeske 179
12. Anaphylactoid properties of LHRH analogs
A . Phillips, D. W. Hahn, C . Bishop , R. J. Capetola
and J. L. McGuire 191
13. Reproductive physiology and general pharmacology
of LHRH antagonists
B. H. Vickery 201
14. Suppression of plasma gonadotropins, testosterone
and sperm production in adult male monkeys by a
potent inhibitory analog of LHRH
W. J. Bremner, L. A. Adams and R. A. Steiner 217
15. LHRH antagonists and female reproductive function
H. M. Fraser 227
SECTION 5 BASIC CLINICAL STUDIES
16. LHRH antagonists in normal men
S. N. Pavlou, G. B. Wakefield and W. J. Kovacs 245
17. Clinical investigations of the contraceptive and
therapeutic potential of nafarelin
S. E. Monroe, J. L. Andreyko and R. B. Jaffe 257
18. LHRH agonists and antagonists: therapeutic
possibilities for premenstrual syndrome
R. L. Reid and S. S. C. Yen 279
19. Early clinical studies with LHRH antagonists in women
Z. M. van der Spuy, L. Pillay, F. Hardie,
M. van der Watt, T. de Chalain, H. Kaplan,
R. Roeske and R. P. Millar 293
vi
PART 2 TABLE OF CONTENTS
20. Profertility uses of LHRH agonist analogues
H. S. Jacobs, R. Porter, A. Eshel and I. Craft 303
SECTION 6 CLINICAL TRIALS
21. Ovulation induction with pulsatile LHRH
S. J. Ory 323
22. Treatment of endometriosis by nasal administration
of nafarelin
M. R. Henzl and S. E. Monroe 337
23. Effects of nafarelin in precocious puberty
J. L. Kirkland and T. H. Lin 349
24. Pharmacokinetics, metabolism and clinical studies
with buserelin
J, Sandow and W. von Rechenberg 363
25. Trials with leuprolide
M. B. Garnick, A. Lipton, H. A. Harvey,
D. T. Max, J. A. Smith and L. M. Glode 383
26. Zoladex studies in prostatic and breast cancer
R. J. Donnelly and R. A. V. Milsted 397
27. Intermittent LHRH agonist sequentially combined
with a progestogen as antiovulatory contraception
A. Lemay and N. Faure 411
28. LHRH agonists and male contraception
S, Bhasin, B, S. Steiner and R, S. Swerdloff 427
SECTION '1 GONADAL PROTECTIVE PROSPECTS WITH LHRH
ANALOGS
29. Interactions between an LHRH analogue and cancer
chemotherapeutic agents at the testicular level
in dogs
J. C. Goodpasture and B. H. Vickery 443
30, Is it possible to conserve the fertility of patients
with Hodgkin's disease treated with cytotoxic
chemotherapy?
J. Waxman 461
SECTION 8 DIAGNOSTIC APPLICATIONS
31. Predicting predisposition to osteoporosis: GnRH
antagonist for acute estrogen deficiency
G. D. Hodgen, D. Kenigsberg and R. Abbasi 473
vii
PART 2 TABLE OF CONTENTS
SECTION 9 APPLICATIONS IN ANIMALS
32. The use of LHRH analogs in aquaculture
L. W. Crim, R. E. Peter and G. van der Kraak 489
33. Uses of LHRH and its analogs in cattle
H. A. Garverick and J. S. Stevenson 499
34. Clinical uses of LHRH analogs in dogs
B. H. Vickery, G. I. McRae and J. C. Goodpasture 517
SECTION 10 FORMULATION AND METABOLISM
35. Intra-nasal administration of LHRH and its analogs
B. H. Vickery 547
36. The controlled delivery of polypeptides including
LHRH analogs
C. G. Pitt 557
37. Pharmacokinetics and metabolism of LHRH analogs
R. L. Chan and C. A. Nerenberg 577
EPilogue
B. H. Vickery and J. J. Nestor, Jr. 595
Subject index 605
viii
Contents
PAR.T 1
TABLE OF CONTENTS'"
List of Contributors xi
Preface
A. Corbin xix
Introduction
J. J. Nestor, Jr. and B. H. Vickery xxi
A retrospective: LHRH and its
analogs: the first decade
A. V. SchaUy xxvii
SECTION I CHEMISTRY AND BASIC REPRODUCTIVE
PROPERTIES
1. Development of agonistic LHRH analogs
J. J. Nestor, Jr. 3
2. LHRH analogs as antiovulatory agents
J. Rivier, C. Rivier, M. Perrin, J. Porter and
W. W. Vale 11
3. LHRH agonists and antagonists containing very
hydrophobic amino acids
J. J. Nestor, Jr., T. L. Ho, R. Tahilramani,
B. L. Horner, R. A. Simpson, G. H. Jones,
G. 1. McRae and B. H. Vickery 23
4. Pharmacological regulation of pituitary LHRH receptors
R. N. Clayton 35
SECTION II REPRODUCTIVE PHYSIOLOGY AND
PHARMACOLOGY IN LABORATORY ANIMALS
5. Biological assays utilized to characterize LHRH and
its analogs
D. W. Hahn, J. L. McGuire, W. Vale and J. Rivier 49
6. Male contraceptive potential of nafarelin acetate
assessed in the dog
B. H. Vickery and G. 1. McRae 61
*Published separately
ix
PART 1 TABLE OF CONTENTS
7. Male fertility control with an LHRH agonist:
primate studies
F. Bint Akhtar, E. J. Wickings and E. Nieschlag 77
8. LHRH agonists for control of female fertility:
primate studies
B. H. Vickery and G. I. McRae 91
9. LHRH antagonists in rhesus and cynomolgus monkeys
R. Asch, J. P. Balmaceda and M. Borghi 107
10. LHRH antagonists in females
M. Nekom and D. H. Coy 125
11. Biological evaluation of a highly potent LHRH
antagonist
G.!. McRae, B. H. Vickery, J. J. Nestor, Jr.,
W. J. Bremner and T. M. Badger 137
12. LHRH antagonists for male contraception
D. Heber and R. S. Swerdloff 153
SECTION III EXTRAHYPOPHYSIAL PARAMETERS
13. Direct antigonadal actions of LHRH
P. B. C. Jones and A. J. W. Hsueh 163
14. Direct gonadal stimumtion with LHRH
H. M. Fraser, R. M. Sharpe and R. M. Popkin 181
15. Antisteroidal actions of LHRH agonists
K. Sundaram and C. W. Bardin 197
SECTION IV CONTRACEPTION IN WOMEN
16. LHRH agonists for female contraception
S. J. Nillius and C. Bergquist 207
17. Postcoital contraception with intranasal buserelin
A. Lemay, N. Faure, F. Labrie and
A. T. A. Fazekas 219
18. Antifertility by discontinuous treatment with
buserelin in women
W. Hardt, T. Genz and M. Schmidt-Gollwitzer 235
19. Risks and benefits of LHRH agonists as antifertility
agents
M. Schmidt-Gollwitzer, W. Hardt and
K. Schmidt-Gollwitzer 243
x
PART 1 TABLE OF CONTENTS
SECTION V CONTRACEPTION IN MAN
20. Effects of nafarelin acetate in men
D. Heber, R. S. Swerdloff and M. Henzl 257
21. Antifertility effects of an LHRH agonist in men
G. C. Doelle, R. M. Evans, A. N. Alexander and
D. Rabin 271
SECTION VI HUMAN THERAPEUTIC APPLICATIONS
22. LHRH therapy for hypo gonadotropic hypo gonadal men
A. Hoffman and W. F. Crowley, Jr. 285
23. Correction of infertility with LHRH agonists
in the male
J. Happ 299
24. LHRH analog therapy of precocious puberty
F. Comite, G. B. Cutler, Jr. and D. L. Loriaux 315
25. LHRH analogs for human mammary carcinoma
H. A. Harvey, A. Lipton and D. T. Max 329
26. Buserelin therapy for prostatic carcinoma
N. Faure, A. Lemay, G. Tolis, F. Labrie
A. Belanger and A. T. A. Fazekas 337
27. Leuprolide therapy for prostatic carcinoma
R. J. Santen, B. Warner, L. M. Demers, M. Dufau
and J. A. Smith, Jr. 351
SECTION VII DIAGNOSTIC APPLICATIONS OF LHRH
28. Diagnostic uses of LHRH
Z. Laron, R. Prager-Lewin and Z. Dickerman 367
SECTION VIII APPLICATIONS IN ANIMALS
29. Actions of LHRH and its analogs in lower vertebrates
L. W. Crim 377
30. LHRH and analogs in relation to livestock
B. D. Schanbacher 385
SECTION IX METABOLIC PARAMETERS
31. Enzymatic degradation of LHRH and analogs
G. Flouret, M. A. Stettler-Stevenson,
F. A. Carone and D. R. Peterson 397
xi