Norprolac (quinagolide) / Ferring - LARVOL DELTA

Circulating prolactin levels and the effect of dopaminergic agonists in systemic lupus erythematosus: a systematic review and meta-analysis. (PubMed, Sci Rep) - "In addition, treatment with the dopaminergic agonists bromocriptine and quinagolide reduced SLE disease activity in small studies and may be a beneficial adjuvant therapy for the disease if larger trials confirm these findings. This review was registered in PROSPERO (CRD42021237156)."

Clinical • Journal • Retrospective data • Review • Immunology • Inflammatory Arthritis • Lupus • Systemic Lupus Erythematosus • PRL

Effect of prolactin concentration during the dry period on the subsequent milk production of dairy cows. (PubMed, J Dairy Sci) - "In this experiment, quinagolide was used to inhibit PRL secretion during the dry period...Lowering the PRL level during short dry period restored milk production to the level normally observed after a conventional dry period, which suggests that higher PRL levels during short dry period are the cause of the lower milk production after a short dry period. Ultimately, strategies to lower blood PRL level may help the adoption of short dry period."

Journal • PRL • PRLR • SOCS3

Editorial: Insights in hyperprolactinemia. (PubMed, Front Endocrinol (Lausanne)) - No abstract available

Journal • Polycystic Ovary Syndrome

Streamlined Stereoselective Entry to (-)-Quinagolide and to 3-Substituted Octahydrobenzo[g]-Quinolines. (PubMed, J Org Chem) - "The key steps involved are a copper-catalyzed regioselective arylation of (S)-epichlorohydrin with 1,6-dimethoxynaphthalene and a diastereoselective trans-reduction of a cyclic enamine intermediate. The possibility to use both enantiomers of epichlorohydrin and the diastereodivergency found in the reduction process paves the way for a general preparation also in the nonracemic form of chiral trans-fused 3-substituted octahydrobenzo[g]quinolines that are privileged structures in medicinal chemistry."

Journal

Development of an asymmetric formal synthesis of (-)-quinagolide via enzymatic resolution and stereoselective iminium ion reduction. (PubMed, Org Biomol Chem) - "A diastereoselective borohydride reduction in combination with an efficient deacylative enzymatic resolution of its β-aminoester precursor are the key steps for a stereoselective installation of the three chiral centres present in the (3S,4aS,10aR)-eutomer of the medicinal drug quinagolide. The obtained data paves the way for an easy and practical attainment of chiral 3-substituted octahydrobenzo[g]quinolines that are privileged structures in medicinal chemistry."

Journal

Research advances in drug therapy of endometriosis. (PubMed, Front Pharmacol) - "This paper investigated Genetic changes, estrogen-dependent inflammation induction, progesterone resistance, imbalance in proliferation and apoptosis, angiogenesis, lymphangiogenesis and neurogenesis, and tissue remodeling in its pathogenesis; and explored the pharmacological mechanisms, constitutive relationships, and application prospects of each compound in the text...In clinical trials, Quinagolide showed no statistical difference with the placebo group; the results of phase II clinical trial of the IL-33 antibody have not been announced yet; clinical trial stage III of vilaprisan was suspended due to drug toxicity...The results of a clinical study of Linzagolix in patients with moderate to severe endometriosis-related pain have not been disclosed yet. Letrozole improved the fertility of patients with mild endometriosis. For endometriosis patients with infertility, oral GnRH antagonists and aromatase inhibitors are promising drugs, especially Elagolix and Letrozole."

Journal • Review • Endometriosis • Gynecology • Infertility • Inflammation • Musculoskeletal Pain • Pain • Sexual Disorders • Women's Health • IL33

Macroprolactinoma with secondary resistance to dopamine agonists: a case report and review of the literature. (PubMed, J Med Case Rep) - "Surgery can facilitate disease control in patients with prolactinomas that develop secondary resistance to dopamine agonists. Malignant prolactinoma is an important differential diagnosis in this group of patients, especially when serum prolactin remains markedly elevated despite resolution or stability of the primary pituitary lesion, suggesting a metastatic source of prolactin secretion."

Journal • Review • Oncology • PRL

The efficacy and safety of quinagolide in hyperprolactinemia treatment: A systematic review and meta-analysis. (PubMed, Front Endocrinol (Lausanne)) - "Three dopamine agonists [bromocriptine, cabergoline, and quinagolide (CV)] have been used for hyperprolactinemia treatment for decades. Hence, this drug could be considered an alternative first-line or rescue treatment in treating hyperprolactinemia in the future. https://www.crd.york.ac.uk/PROSPERO, identifier CRD42022347750."

Retrospective data • Review • Oncology

State of the art, new treatment strategies, and emerging drugs for non-hormonal treatment of endometriosis: a systematic review of randomized control trials. (PubMed, Gynecol Endocrinol) - "Randomized control trials showed promising results with dopamine agonists (cabergoline, quinagolide, and bromocriptine), and the immunomodulatory JNK inhibitor bentamapimod. Agents that have not been represented in randomized control trials or have failed to demonstrate efficacy include statins and TNF-α inhibitors. Although there are substantial improvements in non-hormonal therapy options, majority of the currently available treatment options are supressive rather than curative and do not present a final solution for patients. Future research priorities should be to identify novel target therapies and to evalute the effects of available drugs through different routes of administration."

Journal • Review • Endometriosis • Gynecology • Immune Modulation • Inflammation • Musculoskeletal Pain • Pain • Women's Health

Impulse control disorders in hyperprolactinemic patients on dopamine agonist therapy. (PubMed, Rev Endocr Metab Disord) - "The widespread use of DAs, including bromocriptine, cabergoline and (in some countries) quinagolide, has led to the emergence and recognition of impulse control disorders (ICDs) that may occur in association with DA therapy.Such ICDs include pathological gambling, compulsive shopping, hypersexuality and punding (the performance of repetitive tasks), among others. However, the role of psychopharmacotherapy in hyperprolactinemic patients with ICDs remains incompletely characterized.Patient counseling regarding the risk of ICDs occurring in association with DA therapy, early detection and prompt intervention may mitigate potential harms associated with ICDs. Additional studies are needed to fully characterize risk factors, underlying mechanisms and identify effective therapies for ICDs in patients with hyperprolactinemia receiving DAs."

Journal • Review • CNS Disorders • Depression • Psychiatry

Quinagolide Treatment Reduces Invasive and Angiogenic Properties of Endometrial Mesenchymal Stromal Cells. (PubMed, Int J Mol Sci) - "Of interest, several effects were more prominent on ectopic E-MSCs with respect to eutopic lines. Together with the reported effects on endometrial and endothelial cells, the observed inhibition of E-MSCs may increase the rationale for quinagolide in endometriosis treatment."

Journal • Endometriosis • Gynecology • ER

Comparison of the Effectiveness of Various Medicines in the Prevention of Ovarian Hyperstimulation Syndrome: A Network Meta-Analysis of Randomized Controlled Trials. (PubMed, Front Endocrinol (Lausanne)) - "We investigated the following drugs in our study: aspirin, albumin, metformin, calcium, cabergoline, quinagolide, letrozole, hydroxyethyl starch (HES), and glucocorticoids. These drugs were safe and did not affect clinical pregnancy, miscarriage, or live birth rates. Calcium, HES, and cabergoline could effectively and safely prevent moderate-to-severe OHSS, with calcium as the most effective intervention."

Retrospective data • Review

Formal Synthesis of (-)-Quinagolide: Diastereoselective Ring Expansion via a Bicyclic Aziridinium Ion Strategy to Access the Octahydrobenzo[g]quinoline Architecture. (PubMed, J Org Chem) - "The diastereoselective formal synthesis of (-)-quinagolide, a D receptor agonist, has been achieved. The synthesis started from l-pyroglutamic acid and relied on utilization of (a) a stereospecific catalytic hydrogenation and diastereoselective Horner-Emmons-Michael cascade to obtain functionalized prolinate, (b) a Lewis acid mediated Pummerer cyclization to construct a tricyclic fused ring system, and (c) a diastereoselective ring expansion via a bicyclic aziridinium intermediate to access the required 3-substituted piperidine scaffold."

Journal

Efficacy and safety in the treatment of hyperprolactinemia: A systematic review and network meta-analysis. (PubMed, J Clin Pharm Ther) - "This is the first network meta-analysis that evaluated the efficacy and safety of dopaminergic agonists in the treatment of hyperprolactinemia. The results of this review revealed that these drugs have similar efficacy, but cabergoline has a better safety profile."

Clinical • Journal • Retrospective data • Review • Infertility • Pain • Sexual Disorders • Women's Health

Dopamine agonists for preventing ovarian hyperstimulation syndrome. (PubMed, Cochrane Database Syst Rev) - "Dopamine agonists probably reduce the incidence of moderate or severe OHSS compared to placebo/no intervention, while we are uncertain of the effect on adverse events and pregnancy outcomes (live birth, clinical pregnancy, miscarriage). Dopamine agonists plus co-intervention may decrease moderate or severe OHSS rates compared to co-intervention only, but we are uncertain whether dopamine agonists affect pregnancy outcomes. When compared to other active interventions, we are uncertain of the effects of dopamine agonists on moderate or severe OHSS and pregnancy outcomes."

Journal • Review • Cardiovascular • Gynecology • Venous Thromboembolism

QLARITY: Quinagolide Vaginal Ring on Lesion Reduction Assessed by MRI in Women With Endometriosis/Adenomyosis (clinicaltrials.gov) - P2; N=65; Active, not recruiting; Sponsor: Ferring Pharmaceuticals; Recruiting ➔ Active, not recruiting; Trial completion date: May 2021 ➔ Aug 2021; Trial primary completion date: Apr 2021 ➔ Jul 2021

Clinical • Enrollment closed • Trial completion date • Trial primary completion date • Endometriosis • Gynecology

Use of dopamine agonists to target angiogenesis in women with endometriosis. (PubMed, Hum Reprod) - "In experimental models of endometriosis, DAs (bromocriptine, cabergoline, quinagolide) downregulate proangiogenic and upregulate antiangiogenic pathways in inflammatory, endothelial and endometrial cells, blocking cellular proliferation and reducing lesion size...Moreover, a 20-fold downregulation of Serpin-1, the gene that encodes for plasminogen activator inhibitor 1 (PAI-1), has been observed after DAs treatment...Thus, the data support the use of DAs in the medical management of endometriosis to reduce lesion size and pain while maintaining ovulation. A combined approach of DAs and pentoxifylline is perhaps a smart way of targeting the disease from a completely different angle than current medical treatments."

Clinical • Journal • Endometriosis • Gynecology • Immunology • Inflammation • Pain

RAQUEL: Randomized Trial Assessing Quinagolide Vaginal Ring for Endometriosis-related Pain (clinicaltrials.gov) - P2; N=280; Recruiting; Sponsor: Ferring Pharmaceuticals; Trial primary completion date: Mar 2023 ➔ Jul 2023

Clinical • Trial primary completion date • Endometriosis • Gynecology • Pain • IGF1

Direct Synthesis of Unprotected 2-Azidoamines from Alkenes via an Iron-Catalyzed Difunctionalization Reaction. (PubMed, J Am Chem Soc) - "Facile derivatizations of the azidoamine group demonstrate the versatility of this masked diamine motif in chemoselective, orthogonal transformations. Applications of the methodology in the concise synthesis of RO 20-1724 as well as in the formal total syntheses of both (±)-hamacanthin B and (±)-quinagolide further demonstrate the broad synthetic potential of this highly functional-group-tolerant reaction."

Journal

RAQUEL: Randomized Trial Assessing Quinagolide Vaginal Ring for Endometriosis-related Pain (clinicaltrials.gov) - P2; N=280; Recruiting; Sponsor: Ferring Pharmaceuticals; Trial completion date: Apr 2022 ➔ Aug 2023; Trial primary completion date: Nov 2021 ➔ Mar 2023

Clinical • Trial completion date • Trial primary completion date • Endometriosis • Gynecology • Pain

RAQUEL: Randomized Trial Assessing Quinagolide Vaginal Ring for Endometriosis-related Pain (clinicaltrials.gov) - P2; N=280; Recruiting; Sponsor: Ferring Pharmaceuticals; Suspended ➔ Recruiting

Clinical • Enrollment open • Endometriosis • Gynecology • Pain • IGF1

New therapeutic approaches for endometriosis besides hormonal therapy. (PubMed, Chin Med J (Engl)) - "Clinical data about most of the non-hormonal agents are not sufficient to support them as options for replacement therapy for endometriosis. In spite of this, a few drugs like pentoxifylline showed strong potential for real clinical application."

Journal • Endometriosis • Gynecology • Pain

CURRENT MEDICAL STRATEGIES IN THE PREVENTION OF OVARIAN HYPERSTIMULATION SYNDROME. (PubMed, Acta Clin Croat) - "Among various GnRH agonists, buserelin 0.5 mg, triptorelin 0.2 mg and leuprolide acetate (0.5-4 mg) have been mostly utilized. Among currently available dopamine agonists, cabergoline, quinagolide and bromocriptine are the most common drugs that should be used for prevention of both early and late OHSS. Mild stimulation protocols offer attractive option in OHSS prevention with satisfactory pregnancy rates."

Journal • Review • Biosimilar • Long-acting Reversible Contraceptives

QLARITY: Quinagolide Vaginal Ring on Lesion Reduction Assessed by MRI in Women With Endometriosis/Adenomyosis (clinicaltrials.gov) - P2; N=72; Recruiting; Sponsor: Ferring Pharmaceuticals; Suspended ➔ Recruiting

Clinical • Enrollment open • Endometriosis • Gynecology • Uterine Leiomyoma

Effect of the concentration of circulating prolactin on dairy cows' responsiveness to domperidone injection. (PubMed, J Dairy Sci) - "...After 1 pre-experimental week (d -7 to -1), 18 Holstein cows in mid to late lactation were injected intramuscularly twice daily with either 0.5 mg of quinagolide (QN) or 2 mL of water (control) for 2 wk (d 1 to 14; treatment period)...On d 35, milking did not induce a significant release of PRL above the baseline for both treatments. In conclusion, the results of this experiment support the contention that the mammary gland's responsiveness to PRL is modulated by the previous level of the hormone."

Journal • Biosimilar