Back to products
Approved anticancer agents
Anticancer agents in trials
in preclinical trials
Anticancer molecular libraries
Other drug agents
Bio-reagents and biochemicals
MedKoo product information:
Deacription of Quinagolide: Quinagolide (Norprolac) is a selective, D2 receptor
agonist that is used for the treatment of elevated levels of prolactin.
Quinagolide (Norprolac) was approved in European Community, but not in
USA as of December, 2011. Quinagolide (Norprolac) is a selective, D2 receptor
agonist (also called dopamine receptor stimulant) that is used for the
treatment of elevated levels of prolactin, and Quinagolide prevents the
production of a chemical called prolactin. Prolactin is involved in many
processes within the body, such as milk production after childbirth and
altering levels of hormones involved with controlling the menstrual
cycle and fertility. Quinagolide is therefore helpful in reducing
prolactin levels to reduce milk production for certain medical reasons
and to treat some types of infertility, breast problems and menstrual
Current developer: Ferring
MedKoo Code#: 202390
(quinagolide free base); 94424-50-7 (quinagolide HCl);
Chemical Formula: C20H34ClN3O3S
Molecular Weight: 432.02
Elemental Analysis: C, 55.60; H, 7.93; Cl, 8.21; N,
9.73; O, 11.11; S, 7.42.
Quinagolide (free base)
Chemical Formula: C20H33N3O3S
Exact Mass: 395.22426
Molecular Weight: 395.56
Elemental Analysis: C, 60.73; H, 8.41; N, 10.62; O,
12.13; S, 8.11
Availability and price:
Quinagolide HCl is available soon
For quotation, order and questions, please send email to
firstname.lastname@example.org. A representative
will respond your email shortly. We offer big discount for orders of bulk quantities.
Quality control data:
Product will be shipped with
supporting analytical data.
Highlight of recent study using quinagolide
1. Quinagolide on endometriotic lesions in
patients with endometriosis-associated hyperprolactinemia.
Quinagolide induced a 69.5% reduction in the size of the lesions, with
35% vanishing completely. Histologic analysis showed tissue
degeneration, which was supported by down-regulation of VEGF/VEGFR2,
three proangiogenic cytokines (CCL2, RUNX1, and AGGF1) and plasminogen
activator inhibitor (PAI) 1, a potent inhibitor of fibrinolysis in the
L2 lesions. CONCLUSION(S): By interfering with
angiogenesis, enhancing fibrinolysis, and reducing inflammation,
quinagolide reduces or eliminates peritoneal endometriotic lesions in
women with endometriosis. [source:
Steril. 2011 Mar 1;95(3):882-888.e1.]
2. Quinagolide in prevention of early ovarian
hyperstimulation syndrome in IVF patients: a randomized, double-blind,
placebo-controlled trial. Quinagolide appears to prevent moderate/severe
early OHSS while not affecting treatment outcome. The effect is more
marked in patients who did not achieve a clinical pregnancy. Quinagolide
administered in high doses without dose-titration is associated with
poor tolerability. ClinicalTrials.gov Identifier: NCT00329693. [source:
Hum Reprod. 2010
3. Quinagolide--a valuable treatment option
for hyperprolactinaemia. Quinagolide may
improve patient compliance to treatment owing to its reduced side effect
profile, simple and rapid titration over just 7 days, once-daily dosing
regimen and easy to use starter pack (available in some countries).
Quinagolide offers an additional benefit for patients wishing to become
pregnant, as it can be used until the point of confirmation of
pregnancy. Therefore, as a well tolerated and effective therapy, with a
simple dosing regimen, quinagolide should be considered as a first-line
therapy in the treatment of hyperprolactinaemia. [source:
Eur J Endocrinol. 2006 Feb;154(2):187-95.]
PD and PK properties of quinagolide
1. Pharmacodynamic properties of Quinagolide
Pharmacotherapeutic group: prolactin inhibitors (ATC
code G02C B04).
Quinagolide, the active ingredient of NORPROLAC, is a selective dopamine
D2-receptor agonist not belonging to the chemical classes of ergot or
ergoline compounds. Owing to its dopaminergic action, the drug exerts a
strong inhibitory effect on the secretion of the anterior pituitary
hormone prolactin, but does not reduce normal levels of other pituitary
hormones. In some patients the reduction of prolactin secretion may be
accompanied by short-lasting, small increases in plasma growth hormone
levels, the clinical significance of which is unknown.
As a specific inhibitor of prolactin secretion with a prolonged duration
of action, NORPROLAC has been shown to be effective and suitable for
once-a-day oral treatment of patients presenting with
hyperprolactinaemia and its clinical manifestations such as
galactorrhoea, oligomenorrhoea, amenorrhoea, infertility and reduced
2. Pharmacokinetic properties of Quinagolide
After oral administration of radiolabelled drug,
quinagolide is rapidly and well absorbed. Plasma concentration values
obtained by a non-selective radio-immunoassay (RIA), measuring
quinagolide together with some of its metabolites, were close to the
limit of quantification and gave no reliable information.
The apparent volume of distribution of quinagolide after single oral
administration of radiolabelled compound was calculated to be approx.
100L. For the parent drug, a terminal half-life of 11.5 hours has been
calculated under single dose conditions, and of 17 hours at steady
Quinagolide is extensively metabolised during its first pass. Studies
performed with 3H-labelled quinagolide revealed that more than 95% of
the drug is excreted as metabolites. About equal amounts of total
radioactivity are found in faeces and urine.
In blood, quinagolide and its N-desethyl analogue are the biologically
active but minor components. Their inactive sulphate or glucuronide
conjugates represent the major circulating metabolites. In urine, the
main metabolites are the glucuronide and sulphate conjugates of
quinagolide and the N-desethyl, N,N-didesethyl analogues. In the faeces
the unconjugated forms of the three components were found.
The protein binding of quinagolide is approximately 90% and is
The results, obtained in pharmacodynamic studies, indicate that with the
recommended therapeutic dosage a clinically significant prolactin-lowering
effect occurs within 2 hours after ingestion, reaches a maximum of 4 to
6 hours and is maintained for about 24 hours.
A definite dose-response relationship could be established for the
duration, but not for the magnitude of the prolactin-lowering effect
which, with a single oral dose of 50 micrograms was close to maximum.
Higher doses did not result in a considerably greater effect but
prolonged its duration.
1: Broekhof R, Gosselink MJ, Pijl H, Giltay EJ. The
effect of aripiprazole and quinagolide, a dopamine agonist, in a patient
with symptomatic pituitary prolactinoma and chronic psychosis. Gen Hosp
Psychiatry. 2011 Aug 25. [Epub ahead of print] PubMed PMID: 21872335.
2: Lacasse P, Lollivier V, Bruckmaier RM, Boisclair YR, Wagner GF,
Boutinaud M. Effect of the prolactin-release inhibitor quinagolide on
lactating dairy cows. J Dairy Sci. 2011 Mar;94(3):1302-9. PubMed PMID:
3: Gómez R, Abad A, Delgado F, Tamarit S, Simón C, Pellicer A. Effects
of hyperprolactinemia treatment with the dopamine agonist quinagolide on
endometriotic lesions in patients with endometriosis-associated
hyperprolactinemia. Fertil Steril. 2011 Mar 1;95(3):882-8.e1. Epub 2010
Nov 5. PubMed PMID: 21055747.
4: Lakatos G, Szücs N, Kender Z, Czirják S, Rácz K. [Macroprolactinemia
associated with pituitary macroadenoma: treatment with quinagolide]. Orv
Hetil. 2010 Jun 27;151(26):1072-5. Hungarian. PubMed PMID: 20558354.
5: Busso C, Fernández-Sánchez M, García-Velasco JA, Landeras J,
Ballesteros A, Muńoz E, González S, Simón C, Arce JC, Pellicer A. The
non-ergot derived dopamine agonist quinagolide in prevention of early
ovarian hyperstimulation syndrome in IVF patients: a randomized,
double-blind, placebo-controlled trial. Hum Reprod. 2010
Apr;25(4):995-1004. Epub 2010 Feb 6. PubMed PMID: 20139430; PubMed
Central PMCID: PMC2839910.
6: Vinkers DJ, van der Wee NJ. A case of mania after long-term use of
quinagolide. Gen Hosp Psychiatry. 2007 Sep-Oct;29(5):464. PubMed PMID:
7: Hrycek A, Pochopień-Kenig G, Scieszka J. Selected acute phase
proteins and interleukin-6 in systemic lupus erythematosus patients
treated with low doses of quinagolide. Autoimmunity. 2007
May;40(3):217-22. PubMed PMID: 17453721.
8: Hrycek A, Kusmierz D, Dybała T, Swiatkowska L. Expression of
messenger RNA for transforming growth factor-beta1 and for transforming
growth factor-beta receptors in peripheral blood of systemic lupus
erythematosus patients treated with low doses of quinagolide.
Autoimmunity. 2007 Feb;40(1):23-30. PubMed PMID: 17364494.
9: Barlier A, Jaquet P. Quinagolide--a valuable treatment option for
hyperprolactinaemia. Eur J Endocrinol. 2006 Feb;154(2):187-95. Review.
PubMed PMID: 16452531.
10: Hair WM, Wu FC, Lincoln GA. An investigation of the effectiveness of
testosterone implants in combination with the prolactin inhibitor
quinagolide in the suppression of spermatogenesis in men. Hum Reprod.
2003 Apr;18(4):749-55. PubMed PMID: 12660266.
11: Hrycek A, Kokocińska D, Kośmider J, Konieczny B.
Tissue-polypeptide-specific antigen in SLE patients treated with low
doses of quinagolide. Lupus. 2003;12(2):149-52. PubMed PMID: 12630763.
12: Ilkko E, Tikkakoski T, Salmela P, Pyhtinen J, Kurunlahti M. MR
imaging of pituitary adenomas treated with the prolactin inhibitor
quinagolide. Acta Radiol. 2002 Mar;43(2):125-9. PubMed PMID: 12010287.
13: Mostafa AA, Bebawy LI, Refaat HH. Spectrophotometric determination
of clobetasol propionate, halobetasol propionate, quinagolide
hydrochloride, through charge transfer complexation. J Pharm Biomed
Anal. 2002 Mar 1;27(6):889-99. PubMed PMID: 11836053.
14: Schultz PN, Ginsberg L, McCutcheon IE, Samaan N, Leavens M, Gagel
RF. Quinagolide in the management of prolactinoma. Pituitary. 2000
Dec;3(4):239-49. PubMed PMID: 11788012.
15: De Luis DA, Lahera M, Botella JI, Valero MA, Varela C. [Efficacy of
quinagolide in the treatment of a patient with hypophyseal resistance to
thyroid hormones]. An Med Interna. 2001 May;18(5):259-61. Spanish.
PubMed PMID: 11496561.
16: Hrycek A, Cieślik P, Tustanowski J, Nowak S, Jedynak P. Selected
serum cytokines in systemic lupus erythematosus treated with quinagolide.
Lupus. 2001;10(6):424-30. PubMed PMID: 11434578.
17: Ferone D, Pivonello R, Lastoria S, Faggiano A, Del Basso de Caro ML,
Cappabianca P, Lombardi G, Colao A. In vivo and in vitro effects of
octreotide, quinagolide and cabergoline in four hyperprolactinaemic
acromegalics: correlation with somatostatin and dopamine D2 receptor
scintigraphy. Clin Endocrinol (Oxf). 2001 Apr;54(4):469-77. PubMed PMID:
18: Rohmer V, Freneau E, Morange I, Simonetta C. Efficacy of quinagolide
in resistance to dopamine agonists: results of a multicenter study. Club
de l'Hypophyse. Ann Endocrinol (Paris). 2000 Nov;61(5):411-7. PubMed
19: Nobels FR, de Herder WW, van den Brink WM, Kwekkeboom DJ, Hofland
LJ, Zuyderwijk J, de Jong FH, Lamberts SW. Long-term treatment with the
dopamine agonist quinagolide of patients with clinically non-functioning
pituitary adenoma. Eur J Endocrinol. 2000 Nov;143(5):615-21. PubMed
20: De Luis DA, Becerra A, Lahera M, Botella JI, Valero, Varela C. A
randomized cross-over study comparing cabergoline and quinagolide in the
treatment of hyperprolactinemic patients. J Endocrinol Invest. 2000
Jul-Aug;23(7):428-34. PubMed PMID: 11005266.
21: Koloszár S, Keresztúri A, Kovács L. [Treatment of hyperprolactinemic
anovulation with the dopamin-agonist quinagolide]. Orv Hetil. 2000 Jul
16;141(29):1621-3. Hungarian. PubMed PMID: 10962898.
22: Di Sarno A, Landi ML, Marzullo P, Di Somma C, Pivonello R, Cerbone
G, Lombardi G, Colao A. The effect of quinagolide and cabergoline, two
selective dopamine receptor type 2 agonists, in the treatment of
prolactinomas. Clin Endocrinol (Oxf). 2000 Jul;53(1):53-60. PubMed PMID:
23: Colao A, Ferone D, Lastoria S, Cerbone G, Di Sarno A, Di Somma C,
Lucci R, Lombardi G. Hormone levels and tumour size response to
quinagolide and cabergoline in patients with prolactin-secreting and
clinically non-functioning pituitary adenomas: predictive value of
pituitary scintigraphy with 123I-methoxybenzamide. Clin Endocrinol (Oxf).
2000 Apr;52(4):437-45. PubMed PMID: 10762286.
24: Webster J. Cabergoline and quinagolide therapy for prolactinomas.
Clin Endocrinol (Oxf). 2000 Nov;53(5):549-50. PubMed PMID: 11106914.
25: Eijsbouts A, van den Hoogen F, Laan RF, Hermus RM, Sweep FC, van de
Putte L. Treatment of rheumatoid arthritis with the dopamine agonist
quinagolide. J Rheumatol. 1999 Oct;26(10):2284-5. PubMed PMID: 10529161.
26: Ioannidou-Mouzaka L, Niagassas M, Galanos A, Kalovidouris A. Pilot
study on the treatment of cyclical mastodynia with Quinagolide. Eur J
Gynaecol Oncol. 1999;20(2):117-21. PubMed PMID: 10376428.
27: Ferone D, Lastoria S, Colao A, Varrella P, Cerbone G, Acampa W,
Merola B, Salvatore M, Lombardi G. Correlation of scintigraphic results
using 123I-methoxybenzamide with hormone levels and tumor size response
to quinagolide in patients with pituitary adenomas. J Clin Endocrinol
Metab. 1998 Jan;83(1):248-52. PubMed PMID: 9435450.
28: Colao A, Lombardi G. Prolactinomas apparently resistant to
quinagolide respond to cabergoline therapy. J Clin Endocrinol Metab.
1997 Aug;82(8):2756. PubMed PMID: 9253368.
29: Delgrange E, Donckier J. Prolactinomas apparently resistant to
quinagolide respond to cabergoline therapy. J Clin Endocrinol Metab.
1997 Aug;82(8):2755-6. PubMed PMID: 9253367.
30: Guido R, Valenti S, Foppiani L, De Martini D, Cossu M, Giusti M.
Prolactin decrease and shift to a normal-like isoform profile during
treatment with quinagolide in a patient affected by an invasive
prolactinoma. J Endocrinol Invest. 1997 May;20(5):289-93. PubMed PMID:
31: Tabarin A, Catargi B. [Treatment of macroprolactinomas with
quinagolide (Norprolac)]. Ann Endocrinol (Paris). 1997;58(2):87-94.
Review. French. PubMed PMID: 9239226.
32: Jaquet P. [Quinagolide and macroprolactinomas a progress?]. Ann
Endocrinol (Paris). 1997;58(2):83-5. Review. French. PubMed PMID:
33: Morange I, Barlier A, Pellegrini I, Brue T, Enjalbert A, Jaquet P.
Prolactinomas resistant to bromocriptine: long-term efficacy of
quinagolide and outcome of pregnancy. Eur J Endocrinol. 1996
Oct;135(4):413-20. PubMed PMID: 8921822.
34: Bodmer CW, Atkin SL, Savage MW, Masson EA, White MC. Effects of
quinagolide (CV 205-502), a selective D2-agonist, on vascular reactivity
in patients with a prolactin-secreting adenoma. Clin Endocrinol (Oxf).
1995 Jul;43(1):49-53. PubMed PMID: 7641411.
35: Vilar L, Burke CW. Quinagolide efficacy and tolerability in
hyperprolactinaemic patients who are resistant to or intolerant of
bromocriptine. Clin Endocrinol (Oxf). 1994 Dec;41(6):821-6. PubMed PMID:
36: Lévy L, Alvaro V, Dubray C, Joubert D. Ca(2+)-dependent protein
kinase C isoforms in rat pituitary hyperplasia: effect of in vivo
treatment with quinagolide. Eur J Pharmacol. 1994 Aug 16;268(3):327-34.
PubMed PMID: 7528679.
37: Giusti M, Porcella E, Carraro A, Cuttica M, Valenti S, Giordano G. A
cross-over study with the two novel dopaminergic drugs cabergoline and
quinagolide in hyperprolactinemic patients. J Endocrinol Invest. 1994
Jan;17(1):51-7. PubMed PMID: 7911813.
38: Trouillas J, Chevallier P, Claustrat B, Hooghe-Peters E, Dubray C,
Rousset B, Girod C. Inhibitory effects of the dopamine agonists
quinagolide (CV 205-502) and bromocriptine on prolactin secretion and
growth of SMtTW pituitary tumors in the rat. Endocrinology. 1994
Jan;134(1):401-10. PubMed PMID: 7903933.
39: Nickelsen T, Jungmann E, Althoff P, Schumm-Draeger PM, Usadel KH.
Treatment of macroprolactinoma with the new potent non-ergot D2-dopamine
agonist quinagolide and effects on prolactin levels, pituitary function,
an the renin-aldosterone system. Results of a clinical long-term study.
Arzneimittelforschung. 1993 Apr;43(4):421-5. PubMed PMID: 8098604.
40: Verhelst JA, Froud AL, Touzel R, Wass JA, Besser GM, Grossman AB.
Acute and long-term effects of once-daily oral bromocriptine and a new
long-acting non-ergot dopamine agonist, quinagolide, in the treatment of
hyperprolactinemia: a double-blind study. Acta Endocrinol (Copenh). 1991
Oct;125(4):385-91. PubMed PMID: 1683503.
(Keyword; CAS#; MedKoo code#)