OR12-07 Disease Control in Patients With Acromegaly Switching From Injected Somatostatin Receptor Ligands to Once-Daily Oral Paltusotine: Interim Results of the PATHFNDR-1 Open-Label Extension

Συγγραφείς: Biller, Beverly M K, Casagrande, Alessandra, Strasburger, Christian J, Bidlingmaier, Martin, Snyder, Peter J, Adriana Guitelman, Mirtha, Luiz Boguszewski, Cesar, Buchfelder, Michael, Shimon, Ilan, Raverot, Gerald, Toth, Miklos, Mezősi, Emese, Doknic, Mirjana, Hu, Beibei, Clemmons, David R, James Trainer, Peter, Struthers, R Scott, Krasner, Alan, Gadelha, Monica

Πηγή: J Endocr Soc

Θεματικοί όροι: Abstract

Σύνδεσμος πρόσβασης: https://pmc.ncbi.nlm.nih.gov/articles/PMC12545234/
https://doi.org/10.1210/jendso/bvaf149.1474

MON-069 Once-daily Oral Paltusotine In The Treatment Of Patients With Biochemically Uncontrolled Acromegaly: Interim Results Of The PATHFNDR-2 Open-label Extension

Συγγραφείς: Gadelha, Monica, Casagrande, Alessandra, Elenkova, Atanaska, Boguszewski, Cesar L, Jallad, Raquel S, Hu, Beibei, Hubina, Erika, Fazeli, Pouneh K, Fleseriu, Maria, Snyder, Peter J, Strasburger, Christian J, Bidlingmaier, Martin, Zhao, Yining, Soares, Beatriz, Trainer, Peter J, Struthers, R Scott, Krasner, Alan, Biller, Beverly M K

Πηγή: J Endocr Soc

Θεματικοί όροι: Abstract

Discovery of CRN04894: A Novel Potent Selective MC2R Antagonist

Συγγραφείς: Kim, Sun Hee, Han, Sangdon, Zhao, Jian, Wang, Shimiao, Kusnetzow, Ana Karin, Reinhart, Greg, Fowler, Melissa A., Markison, Stacy, Johns, Michael, Luo, Rosa, Struthers, R. Scott, Zhu, Yunfei, Betz, Stephen F.

Πηγή: ACS Medicinal Chemistry Letters. 15(4):478-485

Διαθεσιμότητα: https://pubs.acs.org/doi/10.1021/acsmedchemlett.3c00514

Oral paltusotine, a nonpeptide selective somatostatin receptor 2 agonist: Mass balance, absolute bioavailability and metabolism in healthy participants

Συγγραφείς: Luo, Rosa, Madan, Ajay, Ferrara‐Cook, Christine T., Dalvie, Deepak, Goulet, Lance, Struthers, R. Scott, Krasner, Alan S.

Πηγή: British Journal of Clinical Pharmacology ; volume 91, issue 7, page 2070-2079 ; ISSN 0306-5251 1365-2125

Διαθεσιμότητα: https://doi.org/10.1002/bcp.70020
https://bpspubs.onlinelibrary.wiley.com/doi/pdf/10.1002/bcp.70020

12537 Once Daily Oral Atumelnant (CRN04894) Induces Rapid And Profound Reductions Of Androstenedione And 17-Hydroxyprogesterone In Participants With Classical Congenital Adrenal Hyperplasia: Initial Results From A 12-Week, Phase 2, Open-Label Study

Συγγραφείς: Joseph Auchus, Richard, James Trainer, Peter, Jean Lucas, Kathryn, Bruera, Dario, Marko, Jamie, Ayala, Alejandro, Wu, Yang, Ferrara-Cook, Christine T, De La Torre, Eduardo, Krasner, Alan, Lagast, Hjalmar, Luo, Rosa, Bachega, Tania A S S, Struthers, R Scott, Betz, Stephen F, Srirangalingam, Umasuthan

Πηγή: J Endocr Soc

Θεματικοί όροι: Abstract

9330 Atumelnant (crn04894) Induces Rapid And Sustained Reductions In Serum And Urine Cortisol In Patients With Acth-Dependent Cushing Syndrome During A Phase 1b/2a, Single Center, 10-day, Inpatient, Open-Label Study

Συγγραφείς: Elenius, H, McGlotten, R, Moore, C, Omotosho, Y B, Ayala, A, Wu, Y, Trainer, P J, Struthers, R S, Krasner, A, Betz, S F, Nieman, L K

Πηγή: J Endocr Soc

Θεματικοί όροι: Abstract

8404 Use of the Acromegaly Symptom Diary (ASD) in a Phase 3, Placebo-Controlled Study of Once-Daily, Oral Paltusotine in Patients With Acromegaly Switched From Injected Octreotide or Lanreotide

Συγγραφείς: Gadelha, Monica Roberto, Casagrande, Alessandra, Strasburger, Christian Joseph, Bidlingmaier, Martin, Snyder, Peter J, Guitelman, Mirtha Adriana, Boguszewski, Cesar Luiz, Buchfelder, Michael, Shimon, Ilan, Raverot, Gerald, Toth, Miklos, Mezosi, Emese, Doknic, Mirjana, Fan, Xiaolin, Clemmons, David, Keeley, Michael, Trainer, Peter James, Scott Struthers, R, Krasner, Alan, Biller, Beverly M K

Πηγή: J Endocr Soc

Θεματικοί όροι: Abstract

Discovery of Paltusotine (CRN00808), a Potent, Selective, and Orally Bioavailable Non-peptide SST2 Agonist

Συγγραφείς: Zhao, Jian, Wang, Shimiao, Markison, Stacy, Kim, Sun Hee, Han, Sangdon, Chen, Mi, Kusnetzow, Ana Karin, Rico-Bautista, Elizabeth, Johns, Michael, Luo, Rosa, Struthers, R. Scott, Madan, Ajay, Zhu, Yunfei, Betz, Stephen F.

Πηγή: ACS Medicinal Chemistry Letters. 14(1):66-74

Διαθεσιμότητα: https://pubs.acs.org/doi/10.1021/acsmedchemlett.2c00431

Paltusotine, a novel oral once-daily nonpeptide SST2 receptor agonist, suppresses GH and IGF-1 in healthy volunteers

Συγγραφείς: Madan, Ajay^{Aff1, Aff3, IDs1110202101201z_cor1}, Markison, Stacy^Aff1, Betz, Stephen F.^Aff1, Krasner, Alan^Aff1, Luo, Rosa^Aff1, Jochelson, Theresa^Aff1, Lickliter, Jason^Aff2, Struthers, R. Scott^Aff1

Πηγή: Pituitary: The official publication of the Pituitary Society and the Growth Hormone Research Society. 25(2):328-339

SAT628 Effect Of Hepatic Impairment On The Pharmacokinetics, Safety, And Tolerability Of Oral Paltusotine, A Non-peptide, Selective Somatostatin Receptor Subtype 2 Agonist

Συγγραφείς: Luo, Rosa, Casagrande, Alessandra, Oun, Sonic, Wang, Yang, Scott Struthers, R, Krasner, Alan

Πηγή: J Endocr Soc

Θεματικοί όροι: 03 medical and health sciences, 0302 clinical medicine, Neuroendocrinology & Pituitary, 16. Peace & justice, 3. Good health

Allosteric and Orthosteric Binding Modes of Two Nonpeptide Human Gonadotropin-Releasing Hormone Receptor Antagonists

Συγγραφείς: Sullivan, Susan K., Brown, Michael S., Gao, Yinghong, Loweth, Colin J., Lio, Francisco M., Crowe, Paul D., Struthers, R. Scott, Betz, Stephen F.

Πηγή: Biochemistry. 45(51):15327-15337

Διαθεσιμότητα: https://pubs.acs.org/doi/10.1021/bi0617097

Determination of the Binding Mode of Thienopyrimidinedione Antagonists to the Human Gonadotropin Releasing Hormone Receptor Using Structure−Activity Relationships, Site-Directed Mutagenesis, and Homology Modeling

Συγγραφείς: Betz, Stephen F., Lio, Francisco M., Gao, Yinghong, Reinhart, Greg J., Guo, Zhiqiang, Mesleh, Michael F., Zhu, Yun-Fei, Struthers, R. Scott

Πηγή: Journal of Medicinal Chemistry. 49(21):6170-6176

Διαθεσιμότητα: https://pubs.acs.org/doi/10.1021/jm060580w

Overlapping, Nonidentical Binding Sites of Different Classes of Nonpeptide Antagonists for the Human Gonadotropin-Releasing Hormone Receptor

Συγγραφείς: Betz, Stephen F., Reinhart, Greg J., Lio, Francisco M., Chen, Struthers, R. Scott

Πηγή: Journal of Medicinal Chemistry. 49(2):637-647

Διαθεσιμότητα: https://pubs.acs.org/doi/10.1021/jm0506928

3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a Potent and Orally Active Antagonist of the Human Gonadotropin-Releasing Hormone Receptor. Design, Synthesis, and in Vitro and in Vivo Characterization

Συγγραφείς: Tucci, Fabio C., Zhu, Yun-Fei, Struthers, R. Scott, Guo, Zhiqiang, Gross, Timothy D., Rowbottom, Martin W., Acevedo, Oscar, Gao, Yinghong, Saunders, John, Xie, Qiu, Reinhart, Greg J., Liu, Xin-Jun, Ling, Nicholas, Bonneville, Anne K. L., Chen, Takung, Bozigian, Haig, Chen

Πηγή: Journal of Medicinal Chemistry. 48(4):1169-1178

Διαθεσιμότητα: https://pubs.acs.org/doi/10.1021/jm049218c

Determinants of High-Affinity Binding and Receptor Activation in the N-Terminus of CCL-19 (MIP-3β)

Συγγραφείς: Ott, T. R., Lio, F. M., Olshefski, D., Liu, X.-J., Struthers, R. S., Ling, N.

Πηγή: Biochemistry. 43(12):3670-3678

Διαθεσιμότητα: https://pubs.acs.org/doi/10.1021/bi035895h

Synthesis and Structure−Activity Relationships of 1-Arylmethyl-5-aryl-6-methyluracils as Potent Gonadotropin-Releasing Hormone Receptor Antagonists

Συγγραφείς: Guo, Zhiqiang, Zhu, Yun-Fei, Gross, Timothy D., Tucci, Fabio C., Gao, Yinghong, Moorjani, Manisha, Connors, Patrick J., Rowbottom, Martin W., Chen, Yongsheng, Struthers, R. Scott, Xie, Qiu, Saunders, John, Reinhart, Greg, Chen, Ta Kung, Bonneville, Anne L. Killam, Chen

Πηγή: Journal of Medicinal Chemistry. 47(5):1259-1271

Διαθεσιμότητα: https://pubs.acs.org/doi/10.1021/jm030472z

Consensus Bioactive Conformation of Cyclic GnRH Antagonists Defined by NMR and Molecular Modeling †

Συγγραφείς: Koerber, Steven C., Rizo, Josep, Struthers, R. Scott, Rivier, Jean E.

Πηγή: Journal of Medicinal Chemistry. 43(5):819-828

Διαθεσιμότητα: https://pubs.acs.org/doi/10.1021/jm990118u

Design of Monocyclic (1−3) and Dicyclic (1−3/4−10) Gonadotropin Releasing Hormone (GnRH) Antagonists †

Συγγραφείς: Rivier, Jean E., Porter, John, Cervini, Laura A., Lahrichi, Sabine L., Kirby, Dean A., Struthers, R. Scott, Koerber, Steven C., Rivier, Catherine L.

Πηγή: Journal of Medicinal Chemistry. 43(5):797-806

Διαθεσιμότητα: https://pubs.acs.org/doi/10.1021/jm9901172

Design of Potent Dicyclic (1−5/4−10) Gonadotropin Releasing Hormone (GnRH) Antagonists †

Συγγραφείς: Rivier, Jean E., Jiang, Guangcheng, Struthers, R. Scott, Koerber, Steven C., Porter, John, Cervini, Laura A., Kirby, Dean A., Craig, A. Grey, Rivier, Catherine L.

Πηγή: Journal of Medicinal Chemistry. 43(5):807-818

Διαθεσιμότητα: https://pubs.acs.org/doi/10.1021/jm990116+

Design of Potent Dicyclic (4−10/5−8) Gonadotropin Releasing Hormone (GnRH) Antagonists

Συγγραφείς: Rivier, Jean E., Struthers, R. Scott, Porter, John, Lahrichi, Sabine L., Jiang, Guangcheng, Cervini, Laura A., Ibea, Michel, Kirby, Dean A., Koerber, Steven C., Rivier, Catherine L.

Πηγή: Journal of Medicinal Chemistry. 43(5):784-796

Διαθεσιμότητα: https://pubs.acs.org/doi/10.1021/jm990115h