| ID Source | ID |
|---|---|
| PubMed CID | 16132393 |
| MeSH ID | M0028836 |
| Synonym |
|---|
| teriparatide rdna |
| ly-333334 |
| ly333334 |
| pth (1-34) |
| OGBMKVWORPGQRR-UMXFMPSGSA-N |
| Class | Description |
|---|---|
| polypeptide | A peptide containing ten or more amino acid residues. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Parathyroid hormone/parathyroid hormone-related peptide receptor | Homo sapiens (human) | IC50 (µMol) | 0.0001 | 0.0001 | 0.0001 | 0.0001 | AID1381232 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Parathyroid hormone/parathyroid hormone-related peptide receptor | Homo sapiens (human) | EC50 (µMol) | 0.0013 | 0.0003 | 0.0013 | 0.0025 | AID1381233; AID482428; AID482479 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Parathyroid hormone/parathyroid hormone-related peptide receptor | Homo sapiens (human) | EC20 (µMol) | 0.0002 | 0.0002 | 0.0002 | 0.0002 | AID1381233 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| parathyroid hormone receptor activity | Parathyroid hormone/parathyroid hormone-related peptide receptor | Homo sapiens (human) |
| protein binding | Parathyroid hormone/parathyroid hormone-related peptide receptor | Homo sapiens (human) |
| peptide hormone binding | Parathyroid hormone/parathyroid hormone-related peptide receptor | Homo sapiens (human) |
| protein homodimerization activity | Parathyroid hormone/parathyroid hormone-related peptide receptor | Homo sapiens (human) |
| G protein-coupled peptide receptor activity | Parathyroid hormone/parathyroid hormone-related peptide receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| nucleus | Parathyroid hormone/parathyroid hormone-related peptide receptor | Homo sapiens (human) |
| cytoplasm | Parathyroid hormone/parathyroid hormone-related peptide receptor | Homo sapiens (human) |
| plasma membrane | Parathyroid hormone/parathyroid hormone-related peptide receptor | Homo sapiens (human) |
| basolateral plasma membrane | Parathyroid hormone/parathyroid hormone-related peptide receptor | Homo sapiens (human) |
| apical plasma membrane | Parathyroid hormone/parathyroid hormone-related peptide receptor | Homo sapiens (human) |
| receptor complex | Parathyroid hormone/parathyroid hormone-related peptide receptor | Homo sapiens (human) |
| plasma membrane | Parathyroid hormone/parathyroid hormone-related peptide receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID372215 | Volume of distribution in human | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Antagonists of the calcium receptor I. Amino alcohol-based parathyroid hormone secretagogues. |
| AID1381258 | Half life in Sprague-Dawley rat at 5 ug/kg, sc | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14 | Development of a Novel Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist (CH5447240), a Potent and Orally Available Small Molecule for Treatment of Hypoparathyroidism. |
| AID456241 | Ex vivo calvaria formation in neonatal mouse assessed as increase in total bone area at 0.001 uM after 7 days relative to control | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Modulation of Wnt signaling through inhibition of secreted frizzled-related protein I (sFRP-1) with N-substituted piperidinyl diphenylsulfonyl sulfonamides: part II. |
| AID1569249 | Osteo-blastogenic activity in mouse MC3T3-E1 cells assessed as stimulation of ALP activity at 1 uM supplemented with fresh medium every 3 to 4 days and measured after 14 days relative to control | |||
| AID482428 | Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP production | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11 | Emerging targets in osteoporosis disease modification. |
| AID1381255 | In vivo agonist activity at PTHR1 in Crl:CD(SD) rat TPTX model assessed as increase in serum calcium levels at 9 nmol/kg, sc administered as single dose measured after 24 hrs by o-cresolphthalein complexone method | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14 | Development of a Novel Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist (CH5447240), a Potent and Orally Available Small Molecule for Treatment of Hypoparathyroidism. |
| AID371999 | Tmax in human | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Antagonists of the calcium receptor I. Amino alcohol-based parathyroid hormone secretagogues. |
| AID1381232 | Displacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysis | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14 | Development of a Novel Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist (CH5447240), a Potent and Orally Available Small Molecule for Treatment of Hypoparathyroidism. |
| AID456243 | Ex vivo calvaria formation in neonatal mouse assessed as increase in osteoblast formation at 0.001 uM after 7 days relative to control | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1 | Modulation of Wnt signaling through inhibition of secreted frizzled-related protein I (sFRP-1) with N-substituted piperidinyl diphenylsulfonyl sulfonamides: part II. |
| AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID1381257 | Tmax in Sprague-Dawley rat at 5 ug/kg, sc | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14 | Development of a Novel Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist (CH5447240), a Potent and Orally Available Small Molecule for Treatment of Hypoparathyroidism. |
| AID1381256 | In vivo agonist activity at PTHR1 in Crl:CD(SD) rat TPTX model assessed as decrease in serum phosphorus levels 9 nmol/kg, sc administered as single dose measured after 24 hrs by xanthine oxidase method | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14 | Development of a Novel Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist (CH5447240), a Potent and Orally Available Small Molecule for Treatment of Hypoparathyroidism. |
| AID1381233 | Agonist activity at human PTHR1 expressed in HKRKB7 cells assessed as accumulation of intracellular cAMP after 20 mins by enzyme immunoassay | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14 | Development of a Novel Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist (CH5447240), a Potent and Orally Available Small Molecule for Treatment of Hypoparathyroidism. |
| AID482479 | Agonist activity at PTH1R overexpressed in HEK293 cells assessed as intracellular cAMP mobilization | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11 | Emerging targets in osteoporosis disease modification. |
| AID372001 | Clearance in men | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Antagonists of the calcium receptor I. Amino alcohol-based parathyroid hormone secretagogues. |
| AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID372000 | Clearance in women | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Antagonists of the calcium receptor I. Amino alcohol-based parathyroid hormone secretagogues. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (16.67) | 29.6817 |
| 2010's | 5 (83.33) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 2 (33.33%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 4 (66.67%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| Påskyndar PTH läkningen av Konservativt Behandlade Humerusfrakturer? [NCT01105832] | Phase 4 | 40 participants (Actual) | Interventional | 2010-04-30 | Completed | ||
| Comparison of the Effects of Teriparatide With Those of Alendronate Sodium on Lumbar Spine Bone Mineral Density in Glucocorticoid-Induced Osteoporosis [NCT00051558] | Phase 3 | 428 participants (Actual) | Interventional | 2002-11-30 | Completed | ||
| Evaluating Teriparatide as a Chondroregenerative Therapy in Human Osteoarthritis [NCT03072147] | Phase 2 | 76 participants (Actual) | Interventional | 2017-05-01 | Completed | ||
| A Phase I, Partially Blinded, Randomized, Placebo Controlled, Active Comparator Study to Explore the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics in Post-menopausal Women After Daily Oral Doses of PTH134 [NCT01224717] | Phase 1 | 104 participants (Actual) | Interventional | 2010-09-30 | Completed | ||
| The Use of Teriparatide as an Adjunctive Therapy for the Treatment of Jones Fractures [NCT01173081] | Phase 4 | 38 participants (Anticipated) | Interventional | 2010-07-31 | Recruiting | ||
| Examination How the Administration Period of Teriparatide Affects Bone Metabolism and Bone Mineral Density Prior to Denosumab Therapy [NCT03702140] | Phase 2 | 90 participants (Anticipated) | Interventional | 2018-10-09 | Recruiting | ||
| Treatment of Osteogenesis Imperfecta With Parathyroid Hormone and Zoledronic Acid [NCT03735537] | Phase 4 | 380 participants (Anticipated) | Interventional | 2016-11-01 | Recruiting | ||
| [NCT02156960] | Phase 4 | 100 participants (Anticipated) | Interventional | 2014-05-31 | Recruiting | ||
| Teriparatide (Forsteo) Treatment in Postmenopausal Women: Mechanism of Action. A Two-year Open-label Single-arm Study of Teriparatide in Secondary Care [NCT01293292] | Phase 4 | 19 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
| A Study to Assess the Effectiveness of Teriparatide (FORTEO) for Increasing Bone Mass and Improving Bone Strength in Adults Affected With Osteogenesis Imperfecta (OI) [NCT00131469] | Phase 4 | 79 participants (Actual) | Interventional | 2005-06-30 | Completed | ||
| Two-dose, Positive Drug Control, Multicentre, Randomized, Double-blind Study of Recombinant Human Parathyroid Hormone for Injection(rhPTH)(1-34) Once a Week to Treat Postmenopausal Osteoporosis Women for the Evaluation the Pharmacokinetics and Safety and [NCT03720886] | Phase 1/Phase 2 | 148 participants (Anticipated) | Interventional | 2018-10-01 | Active, not recruiting | ||
| A Three Stage, Study to Assess the Safety, Pharmacokinetics and Pharmacodynamics of Oral PTH (1-34) in Healthy Subjects [NCT02202603] | Phase 1 | 42 participants (Actual) | Interventional | 2011-07-31 | Completed | ||
| Prospective,Non-interventional Study Investigating Possible Correlation Between Adherence to Postmenopausal and Steroid Induced Osteoporosis Treatment and Physicians' Perception Regarding Osteoporosis Medication [NCT02472782] | 851 participants (Actual) | Observational [Patient Registry] | 2015-05-31 | Completed | |||
| [NCT02223416] | Phase 1 | 0 participants | Interventional | Completed | |||
| Teriparatide for Fracture Repair in Humans: A Prospective, Randomized, Double-blind Placebo-controlled Pilot Study in Female and Male Patients With Proximal Humerus Fracture: The TERAFRAP Study [NCT02091492] | Phase 3 | 0 participants (Actual) | Interventional | 2014-06-30 | Withdrawn(stopped due to no participants) | ||
| Förbättrar PTH Postero-lateral fusionsläkning Vid Ryggkirurgi? [NCT02090244] | Phase 4 | 34 participants (Actual) | Interventional | 2012-08-31 | Completed | ||
| Effect of Teriparatide on Fracture Healing in Patients With Incomplete Atypical Femur Fractures: a Randomized Controlled Trial [NCT01896011] | Phase 3 | 34 participants (Actual) | Interventional | 2013-07-31 | Completed | ||
| Effect of 24 Months of Teriparatide Therapy on Bone Microarchitecture and Bone Volume in Men and Women With Osteoporosis [NCT01155232] | 100 participants (Anticipated) | Observational | 2004-11-30 | Recruiting | |||
| A One-year Partial Double-blinded, Randomized, Multi-center, Multi-national Study to Assess the Effects of Combination Therapy of Annual Zoledronic Acid (5 mg) and Daily Subcutaneous Teriparatide (2mcrg) on Postmenopausal Women With Severe Osteoporosis [NCT00439244] | Phase 3 | 412 participants (Actual) | Interventional | 2006-12-31 | Completed | ||
| Effect and Cost Comparation of Different Treatment Strategies for Osteoporotic Vertebral Fractures (OVF): Teriparatide Injection and Percutaneous Vertebroplasty (PVP) [NCT03692143] | 90 participants (Anticipated) | Observational | 2017-01-01 | Active, not recruiting | |||
| The Use of Nuclear Scintigraphy to Evaluate the Anabolic Effects of Teriparatide on the Skeleton in Postmenopausal Women With Osteoporosis [NCT00259298] | Phase 4 | 12 participants (Actual) | Interventional | 2005-11-30 | Completed | ||
| Efficacy of Teriparatide Treatment in Patients With New Forms of Inherited Low-Turnover Osteoporosis [NCT01360424] | Phase 4 | 6 participants (Actual) | Interventional | 2011-05-31 | Completed | ||
| MicroRNAs Levels in Women With Postmenopausal Osteoporosis Under Antiresorptive or Osteoanabolic Treatment [NCT03472846] | Phase 4 | 26 participants (Actual) | Interventional | 2017-03-01 | Completed | ||
| Early Effects of PTH on the Proximal Femur [NCT01309399] | 40 participants (Actual) | Interventional | 2010-08-31 | Completed | |||
| Study on the Effect of 24 Months of Teriparatide Therapy on Bone Microarchitecture and Bone Volume in Postmenopausal Women With Osteoporosis [NCT01155245] | 60 participants (Anticipated) | Observational | 2008-06-30 | Active, not recruiting | |||
| A Six-month Phase 2 Study of Oral hPTH(1-34) (EBP05) in Postmenopausal Women With Low Bone Mass [NCT04003467] | Phase 2 | 161 participants (Actual) | Interventional | 2019-06-30 | Completed | ||
| A Multiple-Dose Study to Evaluate Skin Irritation and Sensitization of Teriparatide Administered Transdermally in Healthy Postmenopausal Women [NCT01250145] | Phase 1 | 251 participants (Actual) | Interventional | 2010-11-30 | Completed | ||
| A Phase 2 Study for Transdermal Application of Teriparatide [NCT01011556] | Phase 2 | 233 participants (Actual) | Interventional | 2009-11-30 | Completed | ||
| Mechanisms Underlying the Bone Modeling Effects of Combined Anabolic/Antiresorptive Administration [NCT04026256] | Phase 4 | 37 participants (Actual) | Interventional | 2019-09-02 | Completed | ||
| A Randomised, Placebo-controlled, Multi-dose Phase 2 Study to Determine the Efficacy, Safety and Tolerability of AMG 785 in the Treatment of Postmenopausal Women With Low Bone Mineral Density [NCT00896532] | Phase 2 | 419 participants (Actual) | Interventional | 2009-06-03 | Completed | ||
| An Open-label Crossover Study to Determine the Patient Preference Between ZP-PTH Patches and Forteo Pens After Daily Treatment for 14 Days in Women 55-85 Years of Age [NCT02478879] | Phase 1 | 24 participants (Anticipated) | Interventional | 2015-06-30 | Completed | ||
| Management Strategies by an Orthopedic Department to Improve the Evaluation and Treatment of Osteoporosis. [NCT02239523] | 200 participants (Actual) | Interventional | 2017-02-21 | Completed | |||
| The Treatment of Osteoporosis Using a Combination of Teriparatide (Forteo) and Denosumab [NCT02130973] | Phase 4 | 60 participants (Anticipated) | Interventional | 2013-08-31 | Active, not recruiting | ||
| Pharmacokinetic and PHarmacodynamic Analysis and Evaluation of Teriparatide (PTH 1-34) Between Sexes [NCT04921124] | Phase 3 | 30 participants (Actual) | Interventional | 2021-05-24 | Completed | ||
| Efficacy of Sequential Therapies After Osteoanabolic Treatment in Postmenopausal Women With Severe Osteoporosis: the Sequential Treatment After Romosozumab and Teriparatide (START) Study [NCT06164795] | 150 participants (Anticipated) | Observational | 2023-11-25 | Recruiting | |||
| The Effect of Teriparatide on the Early Postoperative Hypocalcemia After Parathyroidectomy in Dialysis Patients: a Pilot, Randomized Trial [NCT04750460] | Phase 3 | 20 participants (Actual) | Interventional | 2021-03-01 | Completed | ||
| Teriparatide for the Treatment of Idiopathic Osteoporosis in Premenopausal Women [NCT00697463] | Phase 2/Phase 3 | 22 participants (Actual) | Interventional | 2008-08-20 | Completed | ||
| Comparison of the Effects of Teriparatide With Those of Risedronate on Lumbar Spine BMD (Bone Mineral Density) in Men and Postmenopausal Women With Low Bone Mass and a Recent Pertrochanteric Hip Fracture [NCT00887354] | Phase 4 | 224 participants (Actual) | Interventional | 2009-04-30 | Completed | ||
| A Randomized Crossover TrIal to Compare Recombinant Human rhPTH(1-34) to the ASsociation Alfacalcidol/Hydrochlorothiazide in the Treatment of Severe Primary Hypoparathyroidism [NCT02824718] | Phase 2 | 16 participants (Actual) | Interventional | 2017-06-06 | Completed | ||
| A Randomized, Parallel-Group, Phase 2 Dose-finding Study to Evaluate the Effects of BA058 in the Treatment of Postmenopausal Women With Osteoporosis [NCT00542425] | Phase 2 | 222 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
| A Phase 2, 24-Week, Multicenter, Randomized, Parallel-Group, Dose-Ranging Study To Evaluate The Effect Of Teriparatide Nasal Spray On Bone Mineral Density In Postmenopausal Women With Low Bone Mineral Density [NCT00624481] | Phase 2 | 350 participants (Anticipated) | Interventional | 2008-03-31 | Withdrawn | ||
| Use of Teriparatide to Accelerate Fracture Healing [NCT00594906] | 10 participants (Actual) | Interventional | 2008-01-31 | Terminated(stopped due to The study was terminated due to poor enrollment.) | |||
| The Effect of Teriparatide Compared With Risedronate on Back Pain in Postmenopausal Women With Osteoporotic Vertebral Fractures [NCT00343252] | Phase 3 | 712 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
| A Dose Ranging Study of the Effects of Macroflux® PTH Compared With Macroflux® Placebo and FORTEO® in Postmenopausal Women With Osteoporosis [NCT00489918] | Phase 2 | 165 participants (Actual) | Interventional | 2007-06-30 | Completed | ||
| [NCT01063504] | Phase 2 | 60 participants (Anticipated) | Interventional | 2010-02-28 | Completed | ||
| A Pilot Study to Assess the Safety and Efficacy of Oral PTH (1-34) in the Treatment of Hypoparathyroidism [NCT02152228] | Phase 2 | 20 participants (Actual) | Interventional | 2014-07-31 | Completed | ||
| An Italian Observational Study to Evaluate Fracture Outcomes, Compliance to Treatment, Back Pain, Health-related Quality of Life in Patients With Severe Osteoporosis Treated According to Common Clinical Practice [NCT00696644] | 794 participants (Actual) | Observational | 2008-06-30 | Completed | |||
| An Observational Study to Assess Back Pain in Patients With Severe Osteoporosis Treated With Teriparatide Versus Antiresorptives [NCT00761332] | 650 participants (Actual) | Observational | 2008-02-29 | Completed | |||
| Clinical and Molecular Characterization of Suspected Partial 25-hydroxyvitamin D-1-alpha-hydroxylase Deficiency [NCT00754442] | 20 participants (Actual) | Interventional | 2007-02-28 | Completed | |||
| A Phase 1b, Open-label, Partially Randomised Study to Assess Safety and Compare Pharmacokinetics of New Oral hPTH(1-34) Tablet Formulations vs. Oral EBP05 Tablets and Subcutaneous Forteo® Injection in Healthy Male Subjects [NCT05965167] | Phase 1/Phase 2 | 45 participants (Anticipated) | Interventional | 2023-05-11 | Active, not recruiting | ||
| Effect of PTH(1-34) Treatment on Fracture Healing in Vivo [NCT00741182] | Phase 2 | 0 participants (Actual) | Interventional | 2008-10-31 | Withdrawn | ||
| Comparison of Teriparatide and Calcitonin in the Treatment of Men and Postmenopausal Women With Osteoporosis [NCT00414973] | Phase 3 | 364 participants (Actual) | Interventional | 2006-12-31 | Completed | ||
| Cyclic Versus Daily Teriparatide on Bone Mass [NCT00668941] | Phase 2 | 140 participants (Anticipated) | Interventional | 2005-09-30 | Active, not recruiting | ||
| Effects of LY333334 in the Treatment of Postmenopausal Women With Osteoporosis [NCT00670501] | Phase 3 | 1,637 participants (Actual) | Interventional | 1996-08-31 | Completed | ||
| Comparison of 3 Month PTHrP(1-36) and PTH(1-34) on Post-Menopausal Osteoporosis [NCT00853723] | Phase 2 | 105 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
| A Double-Masked, Randomized, Two-Treatment Cross-over Study Comparing the Pharmacokinetics of PF708 and Forteo Administered by Subcutaneous Injection in Healthy Adult Subjects [NCT02656810] | Phase 1 | 70 participants (Actual) | Interventional | 2015-12-31 | Completed | ||
| Bone Microarchitecture and Implant Stabilization in Atrophic Jaws Reconstructed With Bone Grafts Treated With Teriparatide [NCT06061354] | Phase 4 | 42 participants (Anticipated) | Interventional | 2023-08-23 | Recruiting | ||
| Skeletal Histomorphometry in Patients on Teriparatide or Zoledronic Acid Therapy [NCT00927186] | Phase 4 | 69 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
| Osteocalcin in Bone Metabolism and Aging: Effect of Vitamin K Supplementation on Circulating Levels of Osteocalcin, on Glucose and Energy Metabolism and on Muscle Mass and Function [NCT04669782] | 123 participants (Anticipated) | Interventional | 2020-11-24 | Recruiting | |||
| Effect of PTH Combined With Weight-Bearing on Bone Density and Bone Architecture in People With Spinal Cord Injury [NCT00826228] | Phase 4 | 12 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
| Efficacy and Safety of Teriparatide 20 Micrograms in the Treatment of Postmenopausal Women With Osteoporosis [NCT00532207] | Phase 3 | 50 participants (Actual) | Interventional | 2003-11-30 | Completed | ||
| Treatment of Adynamic Bone Disorder With Parathyroid Hormone in Patients With Chronic Kidney Disease [NCT04522622] | Phase 4 | 66 participants (Anticipated) | Interventional | 2021-12-15 | Recruiting | ||
| Efficacy and Safety of LY333334 in Japanese Patients With Osteoporosis [NCT00433160] | Phase 3 | 207 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
| Comparison of the Effects of Teriparatide With Those of Risedronate on Lumbar Spine vBMD in Glucocorticoid-Induced Osteoporosis in Men [NCT00503399] | Phase 3 | 92 participants (Actual) | Interventional | 2007-07-31 | Completed | ||
| A Single-centre, Open-label, Five-way Crossover Study in Healthy Female Participants to Assess the Pharmacokinetics of Nasally Administered Formulations of Teriparatide Compared to a Subcutaneous Injection. [NCT01913834] | Phase 1 | 7 participants (Anticipated) | Interventional | 2013-09-30 | Not yet recruiting | ||
| Comparación de la Eficacia y Seguridad clínicas de Osteofortil Respecto de Forteo [NCT01945788] | Phase 4 | 110 participants (Anticipated) | Interventional | 2013-06-30 | Active, not recruiting | ||
| Novel Combination Therapy for Osteoporosis in Men [NCT03994172] | Phase 4 | 48 participants (Anticipated) | Interventional | 2019-07-01 | Recruiting | ||
| The Role of Myokines in Postmenopausal Osteoporosis [NCT04206618] | 220 participants (Actual) | Observational | 2019-06-01 | Completed | |||
| NMR Imaging and Stereological Analysis of Trabecular Bone in Female Subjects 60 and Older at Risk of Fracture Receiving Either Zoledronic Acid or Teriparatide [NCT01153425] | Phase 4 | 33 participants (Actual) | Interventional | 2008-07-31 | Completed | ||
| Bone Properties in Hypoparathyroidism: Effects of PTH [NCT00473265] | Phase 2/Phase 3 | 68 participants (Actual) | Interventional | 2004-05-31 | Completed | ||
| Study CR9108963: A 12-month, Randomized, Double-blind, Parallel-group, Placebo and Active-controlled Dose-range Finding Study of the Efficacy and Safety of SB-751689 in Post-menopausal Women With Osteoporosis [NCT00471237] | Phase 2 | 564 participants (Actual) | Interventional | 2007-05-14 | Terminated(stopped due to Terminated for futility by sponsor after a pre-planned interim review of data) | ||
| A Parallel Group Study to Evaluate the Effect of Six Weeks of Treatment With Nasal Spray (NS) ZT-034, Compared to Subcutaneous (SC) Forteo and Placebo, on Bone Formation, as Assessed by Stimulation of Serum P1NP Levels in Postmenopausal Women With Low Bon [NCT01604057] | Phase 2 | 130 participants (Actual) | Interventional | 2011-11-30 | Active, not recruiting | ||
| B3D-MC-GHDF: Community Experience of Subjects With Osteoporosis Using the Forteo B Pen to Self Administer Once Daily Teriparatide Therapy [NCT00577863] | Phase 3 | 200 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
| PTH and Vibration in OSteoporosis (PaVOS) Study [NCT02563353] | 35 participants (Actual) | Interventional | 2015-11-30 | Completed | |||
| A Phase Ib Study to Assess the Safety, Pharmacokinetics and Pharmacodynamics of Oral PTH (1-34) Formulations in Healthy Subjects [NCT02571140] | Phase 1 | 30 participants (Actual) | Interventional | 2013-10-31 | Completed | ||
| Enhancing Osteoporosis Therapy: Can We Open the Anabolic Window? [NCT01166958] | Phase 4 | 26 participants (Actual) | Interventional | 2010-09-30 | Completed | ||
| Direct Assessment of Non-Vertebral Fractures in Community Experience (DANCE) [NCT01078805] | 4,167 participants (Actual) | Observational | 2003-08-31 | Completed | |||
| Comparison of Teriparatide and Calcitonin in the Treatment of Postmenopausal Women With Osteoporosis [NCT00542984] | Phase 3 | 70 participants (Actual) | Interventional | 2003-08-31 | Completed | ||
| Comparison of Teriparatide and Calcitonin in the Treatment of Postmenopausal Women With Osteoporosis [NCT00543023] | Phase 3 | 104 participants (Actual) | Interventional | 2003-06-30 | Completed | ||
| Comparison of Teriparatide and Calcitonin in the Treatment of Postmenopausal Women With Osteoporosis [NCT00543218] | Phase 3 | 63 participants (Actual) | Interventional | 2002-12-31 | Completed | ||
| Compliance With and Acceptance of Teriparatide Pen Injection in Severely Osteoporotic Patients [CATS] [NCT00191802] | Phase 3 | 120 participants | Interventional | 2003-09-30 | Completed | ||
| TUHRS Study - Teriparatide Use in Hip Replaced Subjects A Pilot Study on the Use of Teriparatide in Severe Osteoporotic Women With Hip Fracture and Submitted to Hip Replacement [NCT00191321] | Phase 3 | 60 participants | Interventional | 2004-07-31 | Completed | ||
| Assessment of Dose Response of LY333334 in Japanese Postmenopausal Women With Osteoporosis [NCT00191867] | Phase 2 | 160 participants | Interventional | 2005-02-28 | Completed | ||
| Second Study of the Effect of Teriparatide on Femoral Neck Fracture Healing [NCT01473602] | Phase 3 | 39 participants (Actual) | Interventional | 2012-01-31 | Completed | ||
| Study of Teriparatide in Stress Fracture Healing [NCT04196855] | Phase 3 | 136 participants (Anticipated) | Interventional | 2019-12-23 | Recruiting | ||
| A Phase I Study to Evaluate the Pharmacokinetics of Parathyroid Hormone (1-34) Administered Orally Via RaniPill™ Capsule [NCT05164614] | Phase 1 | 50 participants (Actual) | Interventional | 2022-02-21 | Completed | ||
| The Effects of Teriparatide on Bone Microarchitecture as Determined by High Resolution Magnetic Resonance Imaging and Digital Topological Analysis [NCT00557310] | Phase 4 | 35 participants (Actual) | Interventional | 2007-11-30 | Completed | ||
| [NCT00446589] | Phase 4 | 19 participants (Actual) | Interventional | 2006-07-31 | Terminated(stopped due to due to financial problems) | ||
| A Double Blind, Randomized, Repeat Dose Parallel Group Study of Recombinant Human Parathyroid Hormone Analog Tablets, or Placebo Tablets, Compared to Open Label Forsteo® in Postmenopausal Women With Osteoporosis [NCT01321723] | Phase 2 | 97 participants (Actual) | Interventional | 2011-02-28 | Completed | ||
| Bone Marker Changes In One Month Treatment With TERIPARATIDE (LY333334) Injections (rDNA Origin) in Men and Postmenopausal Women With Severe Osteoporosis [NCT00532545] | Phase 4 | 45 participants (Actual) | Interventional | 2003-04-30 | Completed | ||
| A Multicenter, Randomized, Parallel Study to Assess the Clinical Efficacy, Safety, and Tolerability of ViaDerm-hPTH (1-34) in Comparison to Subcutaneous Injection of Forteo in Postmenopausal Women With Osteoporosis [NCT00535860] | Phase 2 | 104 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
| Fracture Recovery for Returning to Duty (Teriparatide STRONG) [NCT04589819] | Phase 4 | 183 participants (Anticipated) | Interventional | 2022-12-08 | Enrolling by invitation | ||
| Differential Effects of Teriparatide and Strontium Ranelate on Bone Remodeling and Formation in Postmenopausal Women With Osteoporosis [NCT00239629] | Phase 4 | 73 participants | Interventional | 2005-09-30 | Completed | ||
| The Effects of Therapy With Teriparatide (Recombinant Parathyroid Hormone (1-34) on Vascular Compliance and Osteoprotegerin/RANKL [NCT00347737] | 0 participants (Actual) | Interventional | 2006-06-30 | Withdrawn | |||
| To Study the Efficacy of Teriparatide in Improving Remodeling of Foot Bones in Chronic Charcot Neuroarthropathy in Patients With Diabetes Mellitus. [NCT02023411] | Phase 2 | 20 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
| A Randomized, Double-blind, Placebo-Controlled, Comparative Multicenter Phase 3 Study to Evaluate the Safety and Efficacy of BA058 (Abaloparatide) for Injection for Prevention of Fracture in Ambulatory Postmenopausal Women With Severe Osteoporosis and at [NCT01343004] | Phase 3 | 2,463 participants (Actual) | Interventional | 2011-04-30 | Completed | ||
| Effects of Teriparatide on Distal Radius Fracture Healing [NCT00190944] | Phase 2 | 105 participants | Interventional | 2004-12-31 | Completed | ||
| A Feasibility Study to Explore the Difference in Healing Time Between Teriparatide Treatment and Standard Care on Weber B Ankle Fractures in Older People [NCT02955056] | Phase 4 | 10 participants (Anticipated) | Interventional | 2016-10-31 | Recruiting | ||
| Phase IV Study Teriparatide and Antiresorptive Combination Treatment Subsequent to 9 Months of Teriparatide Monotherapy [NCT01535027] | Phase 4 | 125 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
| Effects of Teriparatide in Postmenopausal Women With Osteoporosis Previously Treated With Alendronate or Raloxifene [NCT00079924] | Phase 4 | 200 participants | Interventional | 2004-11-30 | Completed | ||
| Sequential Use of Teriparatide and Raloxifene HCl in the Treatment of Postmenopausal Women With Osteoporosis [NCT00035256] | Phase 4 | 330 participants | Interventional | 2001-10-31 | Completed | ||
| PTH Once Weekly Research (POWR) [NCT00065637] | Phase 3 | 50 participants | Interventional | 2003-12-31 | Completed | ||
| A Phase II Study of Parathyroid Hormone Following Myeloablative Sequential Unrelated Cord Blood Transplantation [NCT00393380] | Phase 2 | 13 participants (Actual) | Interventional | 2006-09-30 | Terminated(stopped due to Study stopped because of toxicity concerns.) | ||
| [NCT00046137] | Phase 3 | 0 participants | Interventional | Completed | |||
| Comparison of a 2-Year Therapy of Teriparatide Alone and Its Sequential Use for 1 Year, With or Without Raloxifene HCl, in the Treatment of Severe Postmenopausal Osteoporosis [NCT00191425] | Phase 4 | 810 participants | Interventional | 2002-08-31 | Completed | ||
| Bone Effects of Subcutaneous Teriparatide Following Discontinuation of Alendronate Treatment in Postmenopausal Women With Osteoporosis [NCT00191893] | Phase 3 | 66 participants | Interventional | 2003-09-30 | Completed | ||
| Teriparatide for Joint Erosions in Rheumatoid Arthritis: The TERA Trial [NCT01400516] | Phase 4 | 26 participants (Actual) | Interventional | 2011-08-31 | Completed | ||
| Effect of Teriparatide, Vibration and the Combination on Bone Mass and Bone Architecture in Chronic Spinal Cord Injury [NCT01225055] | Phase 2 | 60 participants (Actual) | Interventional | 2010-10-31 | Completed | ||
| Acute Effect of Teriparatide With Bisphosphonate or Denosumab on Bone Resorption [NCT01750086] | Phase 4 | 27 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
| Treatment of Atraumatic Bone Marrow Edema With Denosumab and Teriparatide vs Placebo [NCT01734824] | Phase 4 | 90 participants (Anticipated) | Interventional | 2012-05-31 | Suspended(stopped due to no patients randomized) | ||
| To Compare Efficacy of Weekly Versus Daily Teriparatide in the Management of Postmenopausal Osteoporosis [NCT01760798] | 20 participants (Anticipated) | Interventional | 2012-01-31 | Recruiting | |||
| A Study to Assess the Effects on Serum Calcium When Teriparatide is Used With Active Vitamin D in Osteoporosis Patients [NCT01430104] | Phase 4 | 30 participants (Actual) | Interventional | 2011-08-31 | Completed | ||
| Assessment of the Efficacy of Forteo (Teriparatide) in Patients Undergoing Posterolateral Lumbar Spinal Fusion [NCT01292252] | Phase 4 | 36 participants (Actual) | Interventional | 2011-08-31 | Completed | ||
| Combination Risedronate - Parathyroid Hormone Trial in Male Osteoporosis [NCT01611571] | Phase 3 | 31 participants (Actual) | Interventional | 2003-12-31 | Completed | ||
| Replication of the VERO Osteoporosis Trial in Healthcare Claims Data [NCT04879420] | 12,757 participants (Actual) | Observational | 2020-10-29 | Completed | |||
| A Retrospective, Observational Cohort Study Evaluating the Effectiveness and Cardiovascular Safety of Abaloparatide in Postmenopausal Women New to Anabolic Therapies [NCT04974723] | 16,000 participants (Anticipated) | Observational | 2021-07-01 | Active, not recruiting | |||
| The Effect of Weekly Injection of Teriparatide on the Healing of Distal Radius Fracture in a Double-blind, Randomized Controlled Clinical Trial [NCT04473989] | Phase 2 | 80 participants (Anticipated) | Interventional | 2021-06-01 | Not yet recruiting | ||
| A Phase II Study of Short-Term Use of Teriparatide (Forteo) in the Treatment of Patients With Postoperative Hypocalcemia [NCT00623974] | Phase 2 | 7 participants (Actual) | Interventional | 2008-05-31 | Terminated(stopped due to Terminated due to slow accrual.) | ||
| Bone Formation-Resorption Coupling and Osteoporosis [NCT00000400] | Phase 2 | 176 participants (Actual) | Interventional | 1999-08-31 | Completed | ||
| Efficacy of Wharton's Jelly-derived Mesenchymal Stem Cells in Combination With Parathyroid Hormone for Vertebral Compression Fracture [NCT05018637] | Phase 2 | 30 participants (Anticipated) | Interventional | 2020-09-01 | Enrolling by invitation | ||
| Renal Osteodystrophy: A Fresh Approach [NCT02440581] | 141 participants (Actual) | Interventional | 2015-07-01 | Completed | |||
| Study of the Key Techniques of Prevention and Treatment of Osteoporotic Refracture [NCT05866029] | 2,310 participants (Anticipated) | Interventional | 2023-06-02 | Not yet recruiting | |||
| PTH(1-34) and Pelvic Fracture Healing - a Randomized Controlled Trial [NCT02972424] | Phase 2 | 35 participants (Actual) | Interventional | 2017-05-01 | Completed | ||
| Pilot Study of Teriparatide for Postsurgical Hypoparathyroidism [NCT01171690] | Phase 2 | 5 participants (Actual) | Interventional | 2010-11-30 | Terminated(stopped due to Funding problems) | ||
| Effect of 1 Month Preoperative Teriparatide Use on the Insertional Torque of Pedicle Screws for Lumbar Fusion Surgery [NCT03770338] | 192 participants (Anticipated) | Interventional | 2019-03-01 | Recruiting | |||
| Cyclical vs Daily Continuous PTH in Combination With Alendronate vs Alendronate Alone [NCT00005006] | Phase 2 | 140 participants (Actual) | Interventional | 1987-09-30 | Completed | ||
| A Pilot Methodology Study To Evaluate Changes In Bone Quality Parameters Following Therapy With Recombinant Human Parathyroid Hormone, PTH (Forteo) [NCT00365924] | 20 participants (Actual) | Interventional | 2006-12-31 | Completed | |||
| Effect of Teriparatide on Femoral Neck Fracture Healing [NCT01473589] | Phase 3 | 122 participants (Actual) | Interventional | 2012-02-29 | Completed | ||
| Teriparatide Compared With Alendronate on Spine Bone Mineral Density in Postmenopausal Women With Osteoporosis [NCT02416271] | Phase 4 | 203 participants (Actual) | Interventional | 2001-04-30 | Completed | ||
| Novel Precision Medicine Approach to Treatment of Osteoporosis Based on Bone Turnover [NCT05151484] | Phase 4 | 60 participants (Anticipated) | Interventional | 2022-03-21 | Recruiting | ||
| Randomized Controlled Trial of Teriparatide for the Treatment of Idiopathic Osteoporosis in Premenopausal Women [NCT01440803] | Phase 2 | 41 participants (Actual) | Interventional | 2012-08-02 | Completed | ||
| An Open-label, Randomized, Teriparatide-controlled Study to Evaluate the Effect of Treatment With Romosozumab in Postmenopausal Women With Osteoporosis Previously Treated With Bisphosphonate Therapy [NCT01796301] | Phase 3 | 436 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
| Stem Cell Recruitment in Osteoporosis Therapy [NCT01656629] | 55 participants (Actual) | Interventional | 2012-08-31 | Terminated(stopped due to Inability to analyze collected samples due to no funds.) | |||
| Denosumab and Teriparatide Study (DATA-HD and DATA-EX) [NCT02176382] | Phase 4 | 76 participants (Actual) | Interventional | 2014-08-31 | Completed | ||
| Fracture (FX) Improvement With Teriparatide: FiX-IT Study [NCT01705587] | Phase 4 | 13 participants (Actual) | Interventional | 2012-12-31 | Completed | ||
| The Effect of Treatment With Teriparatide and Zoledronic Acid in Patients With Osteogenesis Imperfecta [NCT01679080] | Phase 2 | 9 participants (Actual) | Interventional | 2012-11-30 | Terminated(stopped due to Eli Lilly has withdrawn support to the study of teriparatide and placebo pens. The study was not able to continue as a randomized study without the supply of placebo pens.) | ||
| Anabolism Versus Antiresorption: A Quadruple Labeling Histomorphometry Study to Compare the Mechanism of Action of Teriparatide and Denosumab in Postmenopausal Women With Osteoporosis [NCT01753856] | Phase 4 | 69 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
| The Role of PTH in Low Bone Mass in Anorexia Nervosa [NCT00759772] | Phase 2 | 23 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
| The Denosumab And Teriparatide Administration Study (DATA) [NCT00926380] | Phase 2 | 94 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
| The Impact of Parathyroid Hormone (PTH) on Craniofacial Osseous Regeneration in Bone [NCT01279187] | Phase 2 | 27 participants (Actual) | Interventional | 2011-02-28 | Terminated(stopped due to Study was terminated due to patient complications unrelated to study drugs) | ||
| 12 Month Open-Label Extension Study of the Effect of Teriparatide on Bone in People With Chronic SCI [NCT02025179] | Phase 2 | 25 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
| A Randomized Study Comparing the Effects of PF708 and Forteo in Patients With Osteoporosis [NCT03002428] | Phase 3 | 181 participants (Actual) | Interventional | 2016-12-31 | Completed | ||
| A Randomized, Open, Self-crossover, Single-dose Clinical Study to Compare Pharmacokinetic of Teriparatide Injection (SAL001) and the Original Drug FORSTEO in Healthy Chinese Adult Volunteers [NCT04747392] | Phase 1 | 64 participants (Actual) | Interventional | 2020-08-19 | Completed | ||
| A Phase III, Randomized, Double Blind, Placebo Controlled Study to Evaluate the Effect of Teriparatide on Bone Union in Unstable Intertrochanteric Fracture Patients Treated With Proximal Femoral Nail Antirotation (PFNA) [NCT03133195] | Phase 3 | 60 participants (Anticipated) | Interventional | 2017-05-17 | Recruiting | ||
| The Relationship Between the Residual Renal Function and Osteoporosis Treatment [NCT02304887] | 1,000 participants (Anticipated) | Observational | 2006-01-31 | Recruiting | |||
| Teriparatide and Risedronate in the Treatment of Patients With Severe Postmenopausal Osteoporosis: Comparative Effects on Vertebral Fractures [NCT01709110] | Phase 4 | 1,366 participants (Actual) | Interventional | 2012-10-31 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||
change from baseline at endpoint in bone mineral density of the lumbar spine as assessed by dual energy X-ray absorptiometry (DXA) (NCT00051558)
Timeframe: 18 month endpoint
| Intervention | grams per square centimeters (Least Squares Mean) |
|---|---|
| Teriparatide | 0.059 |
| Alendronate | 0.028 |
change from baseline at endpoint in bone mineral density of the lumbar spine as assessed by dual energy X-ray absorptiometry (DXA) (NCT00051558)
Timeframe: 18 month endpoint
| Intervention | grams per square centimeters (Least Squares Mean) |
|---|---|
| Teriparatide | 0.056 |
| Alendronate | 0.023 |
Clinical vertebral fracture was defined as a radiographically confirmed fracture that was associated with symptoms such as back pain. (NCT00051558)
Timeframe: 36 months
| Intervention | participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Any Fracture | Nonvertebral Fracture | Vertebral Fracture | Clinical Vertebral Fracture | Nonvertebral Fragility Fracture | Severity-Radiographic Vertebral Fracture: Mild | Severity-Radiographic Vertebral Fracture: Moderate | Severity-Radiographic Vertebral Fracture: Severe | |
| Alendronate | 27 | 15 | 13 | 4 | 5 | 7 | 2 | 4 |
| Teriparatide | 19 | 16 | 3 | 0 | 9 | 1 | 2 | 0 |
change from baseline in bone mineral density of the femoral neck as assessed by dual energy X-ray absorptiometry (DXA) (NCT00051558)
Timeframe: 18, 24, 36 months, and 18 and 36 month endpoints
| Intervention | grams per square centimeters (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Change, baseline to 36 month endpoint(N=185,N=177) | Change from baseline at 36 months(N=120,N=113) | Change from baseline at 24 months(N=135,N=131) | Change, baseline to 18 month endpoint(N=185,N=176) | Change from baseline at 18 months (N=156,N=145) | |
| Alendronate | 0.017 | 0.021 | 0.015 | 0.014 | 0.017 |
| Teriparatide | 0.033 | 0.041 | 0.030 | 0.024 | 0.028 |
change from baseline in bone mineral density of the lumbar spine as assessed by dual energy X-ray absorptiometry (DXA) (NCT00051558)
Timeframe: 24 and 36 months and Endpoint at 36 months
| Intervention | grams per square centimeters (Least Squares Mean) | ||
|---|---|---|---|
| Change, baseline to 36 month endpoint(N=198,N=195) | Change from baseline at 36 months (N=123, N=112) | Change from baseline at 24 months (N=136, N=131) | |
| Alendronate | 0.034 | 0.044 | 0.043 |
| Teriparatide | 0.073 | 0.090 | 0.081 |
change from baseline in bone mineral density of the total hip as assessed by dual energy X-ray absorptiometry (DXA) (NCT00051558)
Timeframe: 18, 24, 36 months, and 18 and 36 month endpoints
| Intervention | grams per square centimeters (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Change, baseline to 36 month endpoint(N=185,N=177) | Change from baseline at 36 months(N=120,N=113) | Change from baseline at 24 months(N=135,N=131) | Change, baseline to 18 month endpoint(N=185,N=176) | Change from baseline at 18 months (N=156,N=144) | |
| Alendronate | 0.017 | 0.020 | 0.018 | 0.017 | 0.018 |
| Teriparatide | 0.032 | 0.037 | 0.034 | 0.026 | 0.027 |
(NCT00051558)
Timeframe: 1, 6, 18, and 36 months
| Intervention | percent (Mean) | |||
|---|---|---|---|---|
| Percent change from baseline at Month 1(N=65,N=78) | Percent change from baseline at Month 6(N=66,N=76) | Percent change from baseline at Month18(N=54,N=65) | Percent change from baseline at Month36(N=44,N=49) | |
| Alendronate | 0.5 | -7.2 | -4.1 | 20.6 |
| Teriparatide | 35.0 | 52.3 | 34.4 | 44.7 |
(NCT00051558)
Timeframe: 1, 6, 18, and 36 months
| Intervention | percent (Mean) | |||
|---|---|---|---|---|
| Percent change from baseline at Month1(N=94,N=100) | Percent change from baseline at Month 6(N=84,N=88) | Percent change from baseline at Month18(N=77,N=77) | Percent change from baseline at Month36(N=56,N=58) | |
| Alendronate | -5.2 | -33.6 | -25.0 | -19.6 |
| Teriparatide | 147.1 | 120.0 | 108.9 | 62.1 |
(NCT00051558)
Timeframe: 1, 6, 18, and 36 months
| Intervention | percent (Mean) | |||
|---|---|---|---|---|
| Percent change from baseline at Month 1(N=66,N=78) | Percent change from baseline at Month 6(N=67,N=76) | Percent change from baseline at Month18(N=55,N=65) | Percent change from baseline at Month36(N=45,N=49) | |
| Alendronate | -8.8 | -22.3 | -21.3 | -15.4 |
| Teriparatide | 48.2 | 10.5 | 5.1 | -1.3 |
(NCT00051558)
Timeframe: 1, 6, 18, and 36 months
| Intervention | percent (Mean) | |||
|---|---|---|---|---|
| Percent change from baseline at Month 1(N=98,N=99) | Percent change from baseline at Month 6(N=86,N=85) | Percent change from baseline at Month18(N=77,N=76) | Percent change from baseline at Month36(N=59,N=57) | |
| Alendronate | -14.8 | -43.2 | -35.8 | -20.2 |
| Teriparatide | 107.0 | 130.8 | 86.3 | 61.7 |
(NCT00051558)
Timeframe: 1, 6, 18, and 36 months
| Intervention | percent (Mean) | |||
|---|---|---|---|---|
| Percent change from baseline at Month 1(N=70,N=79) | Percent change from baseline at Month 6(N=66,N=75) | Percent change from baseline at Month18(N=64,N=71) | Percent change from baseline at Month36(N=49,N=48) | |
| Alendronate | -38.6 | -42.4 | -47.5 | -16.2 |
| Teriparatide | 29.0 | 66.8 | 29.1 | 30.7 |
change from baseline in bone mineral density of the femoral neck as assessed by dual energy X-ray absorptiometry (DXA) (NCT00051558)
Timeframe: 12, 18, 24, and 36 months
| Intervention | grams per square centimeters (Least Squares Mean) | |||
|---|---|---|---|---|
| Change from baseline at Month 36 (N=120,N=113) | Change from baseline at Month 24 (N=135,N=131) | Change from baseline at Month 18 (N=156,N=145) | Change from baseline at Month 12 (N=167,N=158) | |
| Alendronate | 0.021 | 0.015 | 0.017 | 0.012 |
| Teriparatide | 0.041 | 0.030 | 0.028 | 0.026 |
change from baseline in bone mineral density of the lumbar spine as assessed by dual energy X-ray absorptiometry (DXA) (NCT00051558)
Timeframe: 3, 6, 12, and 18 months
| Intervention | grams per square centimeters (Least Squares Mean) | |||
|---|---|---|---|---|
| Change from baseline at Month 18 (N=127,N=119) | Change from baseline at Month 12 (N=139,N=129) | Change from baseline at Month 6 (N=147,N=139) | Change from baseline at Month 3 (N=149,N=150) | |
| Alendronate | 0.027 | 0.024 | 0.015 | 0.012 |
| Teriparatide | 0.062 | 0.052 | 0.031 | 0.017 |
change from baseline in bone mineral density of the lumbar spine as assessed by dual energy X-ray absorptiometry (DXA) (NCT00051558)
Timeframe: 3, 6, 12, 18, 24, 36 months
| Intervention | grams per square centimeters (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Change from baseline at Month 36 (N=123,N=112) | Change from baseline at Month 24 (N=136,N=131) | Change from baseline at Month 18 (N=156,N=148) | Change from baseline at Month 12 (N=170,N=159) | Change from baseline at Month 6 (N=178,N=173) | Change from baseline at Month 3 (N=183,N=184) | |
| Alendronate | 0.044 | 0.043 | 0.031 | 0.028 | 0.018 | 0.012 |
| Teriparatide | 0.090 | 0.081 | 0.066 | 0.054 | 0.034 | 0.019 |
change from baseline in bone mineral density of the total hip as assessed by dual energy X-ray absorptiometry (DXA) (NCT00051558)
Timeframe: 12, 18, 24, and 36 months
| Intervention | grams per square centimeters (Least Squares Mean) | |||
|---|---|---|---|---|
| Change from baseline at 36 Months (N=120, N=113) | Change from baseline at 24 Months (N=135, N=131) | Change from baseline at 18 Months (N=156, N=145) | Change from baseline at 12 Months (N=167, N=158) | |
| Alendronate | 0.020 | 0.018 | 0.018 | 0.014 |
| Teriparatide | 0.037 | 0.034 | 0.027 | 0.022 |
bone density by dual energy xray absorptiometry (NCT00131469)
Timeframe: baseline and 18 months
| Intervention | percentage of change in g/cm2 (Mean) |
|---|---|
| Teriparatide (FORTEO) | 6.1 |
| Placebo | 2.8 |
bone density by dual energy xray absorptiometry (NCT00131469)
Timeframe: baseline and 18 months
| Intervention | percentage of change in g/cm2 (Mean) |
|---|---|
| Teriparatide (FORTEO) | 2.6 |
| Placebo | -2.4 |
Skeletal plasma clearance is defined as the volume of plasma cleared of tracer (99m Tc-MDP) by the skeleton per unit time (milliliter/minute). Kbone is the rate constant representing plasma clearance of tracer to bone. The Patlak plot method was used to evaluate whole skeleton 99mTc-MDP skeletal plasma clearance (Kbone). (NCT00259298)
Timeframe: baseline, 18 months
| Intervention | percentage of change of plasma clearance (Median) |
|---|---|
| Teriparatide | 33.75 |
Changes in focal uptake (localized, defined areas of uptake) were visually scored and compared to baseline or other post-baseline assessments. Changes were rated on a scale from 0-4: 0=no clinically significant focal areas of skeletal uptake; 1=focal areas affecting <1% of skeleton; 2=focal areas affecting >=5% of skeleton; 3=focal areas affecting >=20% of skeleton; 4=focal areas affecting >=50% of skeleton. (NCT00259298)
Timeframe: Baseline, 3 months, 18 months, 24 months
| Intervention | units on a scale (Mean) | ||||
|---|---|---|---|---|---|
| focal change, baseline to 3 months, n=10 | focal change, baseline to 18 months, n=10 | focal change, baseline to 24 months, n=9 | focal change, 3 months to 18 months, n=10 | focal change, 18 months to 24 months, n=9 | |
| Teriparatide | 0.1 | 0.1 | 0 | 0 | 0 |
Skeletal plasma clearance is defined as the volume of plasma cleared of tracer (99m Tc-MDP) by the skeleton per unit time (milliliter/minute). Kbone is the rate constant representing plasma clearance of tracer to bone. The Patlak plot method was used to evaluate whole skeleton 99mTc-MDP skeletal plasma clearance (Kbone) and to derive regional values for the skull, mandible, spine, pelvis, and upper and lower extremities. (NCT00259298)
Timeframe: Baseline, 3 months, 18 months, 24 months
| Intervention | percentage of change of plasma clearance (Median) | |||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Whole skeleton, baseline to 3 months, n=10 | Whole skeleton, baseline to 24 months, n=9 | Whole skeleton, 3 months to 18 months, n=10 | Whole skeleton, 18 months to 24 months, n=9 | Skull, baseline to 3 months, n=8 | Skull, baseline to 18 months, n=8 | Skull, baseline to 24 months, n=7 | Skull, 3 months to 18 months, n=8 | Skull, 18 months to 24 months, n=7 | Mandible, baseline to 3 months, n=8 | Mandible, baseline to 18 months, n=8 | Mandible, baseline to 24 months, n=7 | Mandible, 3 months to 18 months, n=8 | Mandible, 18 months to 24 months, n=7 | Spine, baseline to 3 months, n=10 | Spine, baseline to 18 months, n=10 | Spine, baseline to 24 months, n=9 | Spine, 3 months to 18 months, n=10 | Spine, 18 months to 24 months, n=9 | Pelvis, baseline to 3 months, n=10 | Pelvis, baseline to 18 months, n=10 | Pelvis, baseline to 24 months, n=9 | Pelvis, 3 months to 18 months, n=10 | Pelvis, 18 months to 24 months, n=9 | Upper extremities, baseline to 3 months, n=10 | Upper extremities, baseline to 18 months, n=10 | Upper extremities, baseline to 24 months, n=9 | Upper extremities, 3 months to 18 months, n=10 | Upper extremities, 18 months to 24 months, n=9 | Lower extremities, baseline to 3 months, n=10 | Lower extremities, baseline to 18 months, n=10 | Lower extremities, baseline to 24 months, n=9 | Lower extremities, 3 months to 18 months, n=10 | Lower extremities, 18 months to 24 months, n=9 | |
| Teriparatide | 25.02 | 3.52 | 10.44 | -22.20 | 72.25 | 128.44 | 21.20 | 31.01 | -37.87 | 65.94 | 60.99 | 21.05 | 4.55 | -17.39 | 17.31 | 33.81 | 16.94 | 14.10 | -9.42 | 20.26 | 8.36 | -5.58 | -3.29 | -13.81 | 42.52 | 95.49 | 62.76 | 45.84 | -19.35 | 20.98 | 34.88 | 7.07 | 12.72 | -20.72 |
Skeletal uptake describes the percent uptake of radionuclide tracer by the skeleton when compared to baseline or other post-baseline measures. Skeletal uptake is defined as percentage of uptake of 99mTc-MDP 4 hours after injection. This value differs from skeletal plasma clearance measurements because it only quantifies the amount of 99mTc-MDP taken up by bone without consideration of concentration of tracer in the plasma. (NCT00259298)
Timeframe: Baseline, 3 months, 18 months, 24 months
| Intervention | percentage of change of skeletal uptake (Median) | ||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| whole skeleton, baseline to 3 months, n=10 | whole skeleton, baseline to 18 months, n=10 | whole skeleton, baseline to 24 months, n=9 | whole skeleton, 3 months to 18 months, n=10 | whole skeleton, 18 months to 24 months, n=9 | skull, baseline to 3 months, n=8 | skull, baseline to 18 months, n=8 | skull, baseline to 24 months, n=7 | skull, 3 months to 18 months, n=8 | skull, 18 months to 24 months, n=7 | mandible, baseline to 3 months, n=8 | mandible, baseline to 18 months, n=8 | mandible, baseline to 24 months, n=7 | mandible, 3 months to 18 months, n=8 | mandible, 18 to 24 months, n=7 | spine, baseline to 3 months, n=10 | spine, baseline to 18 months, n=10 | spine, baseline to 24 months, n=9 | spine, 3 months to 18 months, n=10 | spine, 18 months to 24 months, n=9 | pelvis, baseline to 3 months, n=10 | pelvis, baseline to 18 months, n=10 | pelvis, baseline to 24 months, n=9 | pelvis, 3 months to 18 months, n=10 | pelvis, 18 months to 24 months, n=9 | upper extremities, baseline to 3 months, n=10 | upper extremities, baseline to 18 months, n=10 | upper extremities, baseline to 24 months, n=9 | upper extremities, 3 months to 18 months, n=10 | upper extremities, 18 months to 24 months, n=9 | lower extremities, baseline to 3 months, n=10 | lower extremities, baseline to 18 months, n=10 | lower extremities, baseline to 24 months, n=9 | lower extremities, 3 months to 18 months, n=10 | lower extremities, 18 months to 24 months, n=9 | |
| Teriparatide | 15.63 | 26.12 | 5.68 | 3.99 | -14.54 | 68.27 | 120.85 | 26.87 | 23.63 | -34.36 | 52.20 | 62.91 | 23.08 | 3.85 | -6.25 | 12.15 | 17.77 | 17.68 | 13.36 | -0.19 | 14.26 | -1.21 | -1.48 | -3.70 | -5.23 | 31.59 | 76.58 | 57.82 | 48.58 | -10.13 | 9.25 | 23.98 | 0.86 | 7.58 | -16.99 |
Changes in diffuse uptake were determined by comparing diffuse uptake to baseline or other post-baseline observations. Diffuse uptake indicates response to therapy (during active treatment, increased diffuse uptake was expected; after the 6-month withdrawal period, decreased diffuse uptake was expected). Qualitative visual scoring of changes in the bone scan images were performed jointly by 3 reviewers who classified changes in the whole skeleton into 4 groups as follows: possible decreased response, no response, possible response, and definite response. (NCT00259298)
Timeframe: baseline, 3 months, 18 months, 24 months
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| 3 months, no response | 3 months, possible response | 3 months, definite response | 18 months, no response | 18 months, possible response | 18 months, definite response | 24 months, possible response | 24 months, no response | 24 months, definite response | ||
| Teriparatide | 2 | 2 | 6 | 1 | 1 | 8 | 1 | 6 | 1 | 1 |
Time to first occurrence of >=30% pain reduction in average back pain from baseline to 18 months. Average back pain is assessed using an 11-point numeric rating scale, an ordinal scale ranging from 0 (no pain) to 10 (worst possible pain), to rate the average back pain experienced in the preceding 24 hours and is evaluated daily in the week prior to each scheduled study visit. The results are reported as the number of participants reporting at least a 30% reduction in the severity of average back pain up to time (t) in days. (NCT00343252)
Timeframe: Baseline through 18 Months
| Intervention | participants (Number) |
|---|---|
| Teriparatide | 260 |
| Risedronate | 242 |
Time to first occurrence of >= 30% pain reduction in worst back pain from baseline to 12 months. Worst back pain is assessed using an 11-point numeric rating scale, an ordinal scale ranging from 0 (no pain) to 10 (worst possible pain), to rate the worst back pain experienced in the preceding 24 hours and is evaluated daily in the week prior to each scheduled study visit. The results are reported as the number of participants reporting at least a 30% reduction in the severity of worst back pain up to time (t) in days. (NCT00343252)
Timeframe: Days 0, 60, 120, 180, 240, 300, 360, 420, 480, 540, and 600
| Intervention | participants (Number) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Day 0 | Day 60 | Day 120 | Day 180 | Day 240 | Day 300 | Day 360 | Day 420 | Day 480 | Day 540 | Day 600 | |
| Risedronate | 0 | 74 | 145 | 181 | 193 | 206 | 209 | 220 | 220 | 220 | 220 |
| Teriparatide | 0 | 70 | 151 | 195 | 206 | 224 | 226 | 233 | 233 | 233 | 233 |
Time to first occurrence of >= 30% pain reduction in worst back pain from baseline to 18 months. Worst back pain is assessed using an 11-point numeric rating scale, an ordinal scale ranging from 0 (no pain) to 10 (worst possible pain), to rate the worst back pain experienced in the preceding 24 hours and is evaluated daily in the week prior to each scheduled study visit. The results are reported as the number of participants reporting at least a 30% reduction in the severity of worst back pain up to time (t) in days. (NCT00343252)
Timeframe: Baseline through 18 Months
| Intervention | participants (Number) |
|---|---|
| Teriparatide | 248 |
| Risedronate | 234 |
QUALEFFO is an osteoporosis-specific health instrument developed specifically for participants with vertebral deformities used to evaluate the effect of back pain and treatment on quality of life. The QUALEFFO questionnaire includes 41 items in 5 domains: pain, physical function, social function, general health perception, and mental function. The total score is calculated according to the scoring algorithm developed by the International Osteoporosis Foundation. Total scores are reported from 0 to 100, with lower scores corresponding to better quality of life. (NCT00343252)
Timeframe: Baseline, 6 Months
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Teriparatide | -2.80 |
| Risedronate | -2.63 |
Roland-Morris Disability Questionnaire (RMDQ-24) is completed by the participant and measures the degree of disability due to back pain. The questionnaire consists of 24 statements and the participant is instructed to put a mark next to each appropriate statement. The number of statements marked are added up by the clinician and a total score is given. The total score ranges from 0 (no disability) to 24 (severe disability). (NCT00343252)
Timeframe: Baseline, 12 Months
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Teriparatide | -2.09 |
| Risedronate | -2.12 |
Roland-Morris Disability Questionnaire (RMDQ-24) is completed by the participant and measures the degree of disability due to back pain. The questionnaire consists of 24 statements and the participant is instructed to put a mark next to each appropriate statement. The number of statements marked are added up by the clinician and a total score is given. The total score ranges from 0 (no disability) to 24 (severe disability). (NCT00343252)
Timeframe: Baseline, 6 Months
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Teriparatide | -1.58 |
| Risedronate | -1.77 |
Roland-Morris Disability Questionnaire (RMDQ-24) is completed by the participant and measures the degree of disability due to back pain. The questionnaire consists of 24 statements and the participant is instructed to put a mark next to each appropriate statement. The number of statements marked are added up by the clinician and a total score is given. The total score ranges from 0 (no disability) to 24 (severe disability). (NCT00343252)
Timeframe: Baseline, 3 Months
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Teriparatide | -1.42 |
| Risedronate | -1.41 |
Roland-Morris Disability Questionnaire (RMDQ-24) is completed by the participant and measures the degree of disability due to back pain. The questionnaire consists of 24 statements and the participant is instructed to put a mark next to each appropriate statement. The number of statements marked are added up by the clinician and a total score is given. The total score ranges from 0 (no disability) to 24 (severe disability). Pooled site, baseline glucocorticoid usage status (yes/no) and baseline score were controlled for. (NCT00343252)
Timeframe: Baseline, 18 Months
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Teriparatide | -3.21 |
| Risedronate | -3.19 |
QUALEFFO is an osteoporosis-specific health instrument developed specifically for participants with vertebral deformities used to evaluate the effect of back pain and treatment on quality of life. The QUALEFFO questionnaire includes 41 items in 5 domains: pain, physical function, social function, general health perception, and mental function. The total score is calculated according to the scoring algorithm developed by the International Osteoporosis Foundation. Total scores are reported from 0 to 100, with lower scores corresponding to better quality of life. (NCT00343252)
Timeframe: Baseline, 18 Months
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Teriparatide | -5.67 |
| Risedronate | -5.17 |
QUALEFFO is an osteoporosis-specific health instrument developed specifically for participants with vertebral deformities used to evaluate the effect of back pain and treatment on quality of life. The QUALEFFO questionnaire includes 41 items in 5 domains: pain, physical function, social function, general health perception, and mental function. The total score is calculated according to the scoring algorithm developed by the International Osteoporosis Foundation. Total scores are reported from 0 to 100, with lower scores corresponding to better quality of life. (NCT00343252)
Timeframe: Baseline, 12 Months
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Teriparatide | -5.74 |
| Risedronate | -5.27 |
Time to first occurrence of >=30% pain reduction in average back pain from baseline to 6 months. Average back pain is assessed using an 11-point numeric rating scale, an ordinal scale ranging from 0 (no pain) to 10 (worst possible pain), to rate the average back pain experienced in the preceding 24 hours and is evaluated daily in the week prior to each scheduled study visit. The results are reported as the number of participants reporting at least a 30% reduction in the severity of average back pain up to time (t) in days. (NCT00343252)
Timeframe: Days 0, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300
| Intervention | participants (Number) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Day 0 | Day 30 | Day 60 | Day 90 | Day 120 | Day 150 | Day 180 | Day 210 | Day 240 | Day 270 | Day 300 | |
| Risedronate | 0 | 33 | 86 | 130 | 162 | 178 | 200 | 210 | 211 | 211 | 211 |
| Teriparatide | 0 | 40 | 91 | 136 | 175 | 199 | 212 | 221 | 221 | 221 | 221 |
Time to first occurrence of >= 30% pain reduction in average back pain from baseline to 12 months. Average back pain is assessed using an 11-point numeric rating scale, an ordinal scale ranging from 0 (no pain) to 10 (worst possible pain), to rate the average back pain experienced in the preceding 24 hours and is evaluated daily in the week prior to each scheduled study visit. The results are reported as the number of participants reporting at least a 30% reduction in the severity of average back pain up to time (t) in days. (NCT00343252)
Timeframe: Days 0, 60, 120, 180, 240, 300, 360, 420, 480, 540, and 600
| Intervention | participants (Number) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Day 0 | Day 60 | Day 120 | Day 180 | Day 240 | Day 300 | Day 360 | Day 420 | Day 480 | Day 540 | Day 600 | |
| Risedronate | 0 | 86 | 162 | 200 | 211 | 220 | 226 | 238 | 238 | 238 | 238 |
| Teriparatide | 0 | 91 | 175 | 212 | 221 | 234 | 238 | 246 | 246 | 246 | 246 |
Time to first occurrence of >= 30% pain reduction in worst back pain from baseline to 6 months. Worst back pain is assessed using an 11-point numeric rating scale, an ordinal scale ranging from 0 (no pain) to 10 (worst possible pain), to rate the worst back pain experienced in the preceding 24 hours and is evaluated daily in the week prior to each scheduled study visit. The results are reported as the number of participants reporting at least a 30% reduction in the severity of worst back pain up to time (t) in days. (NCT00343252)
Timeframe: Days 0, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300
| Intervention | participants (Number) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Day 0 | Day 30 | Day 60 | Day 90 | Day 120 | Day 150 | Day 180 | Day 210 | Day 240 | Day 270 | Day 300 | |
| Risedronate | 0 | 22 | 74 | 111 | 145 | 164 | 181 | 192 | 193 | 193 | 193 |
| Teriparatide | 0 | 26 | 70 | 110 | 151 | 175 | 195 | 206 | 206 | 206 | 206 |
Safety is assessed via serious adverse events and all other non-serious adverse events and the data are located in the Reported Adverse Events Section. (NCT00343252)
Timeframe: Baseline through 18 Months
| Intervention | participants (Number) | |
|---|---|---|
| Serious Adverse Events | Adverse Events | |
| Risedronate | 66 | 273 |
| Teriparatide | 55 | 277 |
Safety was assessed via serious adverse events and all other non-serious adverse events and the data are located in the Reported Adverse Events Section. (NCT00343252)
Timeframe: Baseline through 12 Months
| Intervention | participants (Number) | |
|---|---|---|
| Serious Adverse Events | Adverse Events | |
| Risedronate | 50 | 266 |
| Teriparatide | 39 | 269 |
24-hour worst back pain severity scores recorded daily on an 11-point numeric rating scale, an ordinal scale ranging from 0 (no pain) to 10 (worst possible pain). The 11-point scale is used for assessment of worst back pain in the preceding 24 hours and is evaluated daily in the week prior to each scheduled study visit. Responders are defined as participants with at least a 30% reduction in the severity of worst back pain from baseline to the 6-month last observation carried forward (LOCF) endpoint. (NCT00343252)
Timeframe: 6 Months
| Intervention | participants (Number) | |
|---|---|---|
| Responder to Treatment | Non-Responder to Treatment | |
| Risedronate | 193 | 143 |
| Teriparatide | 206 | 142 |
24-hour worst back pain severity scores recorded daily on an 11-point numeric rating scale, an ordinal scale ranging from 0 (no pain) to 10 (worst possible pain). The 11-point scale is used for assessment of worst back pain in the preceding 24 hours and is evaluated daily in the week prior to each scheduled study visit. Responders are defined as participants with at least a 30% reduction in the severity of worst back pain from baseline to the 18-month last observation carried forward (LOCF) endpoint. (NCT00343252)
Timeframe: 18 Months
| Intervention | participants (Number) | |
|---|---|---|
| Responder | Non-Responder | |
| Risedronate | 234 | 115 |
| Teriparatide | 248 | 112 |
24-hour worst back pain severity scores recorded daily on an 11-point numeric rating scale, an ordinal scale ranging from 0 (no pain) to 10 (worst possible pain). The 11-point scale is used for assessment of worst back pain in the preceding 24 hours and is evaluated daily in the week prior to each scheduled study visit. Responders are defined as participants with at least a 30% reduction in the severity of worst back pain from baseline to the 12-month last observation carried forward (LOCF) endpoint. (NCT00343252)
Timeframe: 12 Months
| Intervention | participants (Number) | |
|---|---|---|
| Responder to Treatment | Non-Responder to Treatment | |
| Risedronate | 220 | 116 |
| Teriparatide | 233 | 115 |
24-hour average back pain severity scores recorded daily on an 11-point numeric rating scale, an ordinal scale ranging from 0 (no pain) to 10 (worst possible pain). The 11-point scale is used for assessment of average back pain in the preceding 24 hours and is evaluated daily in the week prior to each scheduled study visit. Responders are defined as participants with at least a 30% reduction in the severity of average back pain from baseline to the 6-month last observation carried forward (LOCF) endpoint. (NCT00343252)
Timeframe: 6 Months
| Intervention | participants (Number) | |
|---|---|---|
| Responder to Treatment | Non-Responder to Treatment | |
| Risedronate | 211 | 125 |
| Teriparatide | 221 | 126 |
24-hour average back pain severity scores recorded daily on an 11-point numeric rating scale, an ordinal scale ranging from 0 (no pain) to 10 (worst possible pain). The 11-point scale is used for assessment of average back pain in the preceding 24 hours and is evaluated daily in the week prior to each scheduled study visit. Responders are defined as participants with at least a 30% reduction in the severity of average back pain from baseline to the 18-month last observation carried forward (LOCF) endpoint. (NCT00343252)
Timeframe: 18 Months
| Intervention | participants (Number) | |
|---|---|---|
| Responder | Non-responder | |
| Risedronate | 242 | 107 |
| Teriparatide | 260 | 100 |
24-hour average back pain severity scores recorded daily on an 11-point numeric rating scale, an ordinal scale ranging from 0 (no pain) to 10 (worst possible pain). The 11-point scale is used for assessment of average back pain in the preceding 24 hours and is evaluated daily in the week prior to each scheduled study visit. Responders are defined as participants with at least a 30% reduction in the severity of average back pain from baseline to the 12-month last observation carried forward (LOCF) endpoint. (NCT00343252)
Timeframe: 12 Months
| Intervention | participants (Number) | |
|---|---|---|
| Responder to Treatment | Non-Responder to Treatment | |
| Risedronate | 238 | 98 |
| Teriparatide | 246 | 101 |
Median time to neutrophil engraftment (defined as an absolute neutrophil count [ANC] greater than 500) (NCT00393380)
Timeframe: Statistic is calculated at Day 42 but ANC counts are measured daily up through discharge.
| Intervention | days (Median) |
|---|---|
| Parathyroid Hormone (Teriparatide) | 30 |
Disease-free survival (NCT00393380)
Timeframe: Measured at 1 year
| Intervention | percentage of participants (Number) |
|---|---|
| Parathyroid Hormone (Teriparatide) | 38.5 |
Cumulative Incidence of Relapse (NCT00393380)
Timeframe: Measured at 2 years
| Intervention | percentage of participants (Number) |
|---|---|
| Parathyroid Hormone (Teriparatide) | 15.4 |
Cumulative Incidence of Acute GVHD Grades II-IV at day 100 (NCT00393380)
Timeframe: Measured at Day 100
| Intervention | percentage of participants (Number) |
|---|---|
| Parathyroid Hormone (Teriparatide) | 38.5 |
100-day transplant-related mortality (NCT00393380)
Timeframe: Measured at Day 100
| Intervention | participants (Number) |
|---|---|
| Parathyroid Hormone (Teriparatide) | 4 |
Platelet engraftment (greater than 20,000) (NCT00393380)
Timeframe: Measured at Day 180
| Intervention | percentage of participants (Number) |
|---|---|
| Parathyroid Hormone (Teriparatide) | 46.2 |
Cumulative Incidence of Chronic GVHD (NCT00393380)
Timeframe: Measured at 2 years
| Intervention | percentage of participants (Number) |
|---|---|
| Parathyroid Hormone (Teriparatide) | 38.5 |
Overall Survival (NCT00393380)
Timeframe: Measured at 2 years
| Intervention | percentage of participants (Number) |
|---|---|
| Parathyroid Hormone (Teriparatide) | 38.5 |
Lumbar spine bone mineral density (milligrams per square centimeter) was measured by dual energy X-ray absorptiometry (DXA). Change = Endpoint minus baseline. (NCT00414973)
Timeframe: Baseline to 24 weeks
| Intervention | percentage change in lumbar spine BMD (Least Squares Mean) |
|---|---|
| Teriparatide - Males | 6.01 |
| Calcitonin - Males | 3.38 |
Lumbar spine bone mineral density (milligrams per square centimeter) was measured by dual energy X-ray absorptiometry (DXA). Change = Endpoint minus baseline. (NCT00414973)
Timeframe: Baseline to 24 weeks
| Intervention | percentage change in lumbar spine BMD (Least Squares Mean) |
|---|---|
| Teriparatide - Females | 6.04 |
| Calcitonin - Females | 1.65 |
Total hip bone mineral density (milligrams per square centimeter) was measured by dual energy X-ray absorptiometry (DXA). Change = Endpoint minus baseline. (NCT00414973)
Timeframe: Baseline to 24 weeks
| Intervention | percentage change in total hip BMD (Least Squares Mean) |
|---|---|
| Teriparatide - Males | 0.37 |
| Calcitonin - Males | 1.34 |
Total hip bone mineral density (milligrams per square centimeter) was measured by dual energy X-ray absorptiometry (DXA). Change = Endpoint minus baseline. (NCT00414973)
Timeframe: Baseline to 24 weeks
| Intervention | percentage change in total hip BMD (Least Squares Mean) |
|---|---|
| Teriparatide - Females | -0.53 |
| Calcitonin - Females | -0.62 |
Measures of serum osteocalcin (nanograms per milliliter). Change = Endpoint minus baseline. (NCT00414973)
Timeframe: Baseline to 12 weeks and 24 weeks
| Intervention | percentage change in osteocalcin (Median) | |
|---|---|---|
| Week 12 Percentage Change (n=21, n=11) | Week 24 Percentage Change (n=21, n=11) | |
| Calcitonin - Males | 4.35 | -17.65 |
| Teriparatide - Males | 107.27 | 79.26 |
Measures of serum osteocalcin (nanograms per milliliter). Change = Endpoint minus baseline. (NCT00414973)
Timeframe: Baseline to 12 weeks and 24 weeks
| Intervention | percentage change in osteocalcin (Median) | |
|---|---|---|
| Week 12 Percentage Change (n=202, n=102) | Week 24 Percentage Change (n=191, n=97) | |
| Calcitonin - Females | -7.67 | -10.58 |
| Teriparatide - Females | 113.87 | 137.45 |
Percent change in serum bone-specific alkaline phosphatase (BAP) from baseline to the individual visits and last measurement point. (NCT00433160)
Timeframe: Baseline, 76 Weeks, 104 Weeks
| Intervention | percent change in BAP (Mean) | |
|---|---|---|
| Percent Change to Week 76; n=113, n=55 | Percent Change to Week 104; n=92, n=47 | |
| Placebo | 15.71 | 16.45 |
| Teriparatide | 17.49 | -1.52 |
Number of vertebral fractures observed from Visit 1 (study entry) through Visit 19 (Week 52). All new or worsened vertebral fractures were defined as a deterioration of at least one grade in a semiquantitative score by X-ray assessment. Number of subjects with fractures and number of fractured vertebra(e) were counted. (NCT00433160)
Timeframe: Baseline through 52 weeks
| Intervention | number of fractures (Number) | |
|---|---|---|
| New Fractures (n=5, n=4) | Worsening Fractures (n=2, n=0) | |
| Placebo | 5 | 0 |
| Teriparatide | 7 | 3 |
Percent change in serum bone-specific alkaline phosphatase (BAP) from baseline to the individual visits and last measurement point. (NCT00433160)
Timeframe: Baseline to Weeks 4, 12, 24, 52
| Intervention | percent change in BAP (Mean) | ||||
|---|---|---|---|---|---|
| Percent Change to Week 4 (n=135, n=66) | Percent Change to Week 12 (n=131, n=62) | Percent Change to Week 24 (n=127, n=60) | Percent Change to Week 52 (n=120, n=59) | Percent Change to Last Measurement (n=136, n=66) | |
| Placebo | -9.63 | -16.97 | -28.46 | -32.24 | -28.34 |
| Teriparatide | 3.74 | 3.23 | -4.60 | -17.69 | -17.32 |
"Vertebral and nonvertebral fractures assessed by the investigator or subinvestigator after starting the study treatment. Traumatic fractures were those caused by falling from above standing height or a high velocity (car) accident. Fractures were assessed to be fragility if they occurred without trauma." (NCT00433160)
Timeframe: Baseline through 52 Weeks
| Intervention | number of fractures (Number) | |||
|---|---|---|---|---|
| Vertebral Fracture - Fragility | Vertebral Fracture - Traumatic | Non-Vertebra Fracture - Fragility | Non-Vertebra Fracture - Traumatic | |
| Placebo | 1 | 0 | 1 | 3 |
| Teriparatide | 0 | 0 | 1 | 2 |
Severity of back pain at 76 weeks and 104 weeks. Back pain was measured on a scale of 1 (none) to 4 (severe). (NCT00433160)
Timeframe: Baseline, 76 Weeks, 104 Weeks
| Intervention | participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Week 76: 1- None | Week 76: 2- Mild | Week 76: 3- Moderate | Week 76: 4- Severe | Week 104: 1- None | Week 104: 2- Mild | Week 104: 3- Moderate | Week 104: 4- Severe | |
| Placebo | 38 | 13 | 4 | 0 | 32 | 13 | 2 | 0 |
| Teriparatide | 78 | 31 | 4 | 0 | 66 | 23 | 3 | 0 |
Severity of back pain at baseline, individual visits and the last measurement point. Back pain was measured on a scale of 1 (none) to 4 (severe). (NCT00433160)
Timeframe: Baseline, Weeks 12, 24, 36, 52
| Intervention | participants (Number) | |||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline: 1 - None | Baseline: 2 - Mild | Baseline: 3 - Moderate | Baseline: 4 - Severe | Week 12: 1 - None | Week 12: 2 - Mild | Week 12: 3 - Moderate | Week 12: 4 - Severe | Week 24: 1 - None | Week 24: 2 - Mild | Week 24: 3 - Moderate | Week 24: 4 - Severe | Week 36: 1 - None | Week 36: 2 - Mild | Week 36: 3 - Moderate | Week 36: 4 - Severe | Week 52: 1 - None | Week 52: 2 - Mild | Week 52: 3 - Moderate | Week 52: 4 - Severe | Last Measurement: 1 - None | Last Measurement: 2 - Mild | Last Measurement: 3 - Moderate | Last Measurement: 4 - Severe | |
| Placebo | 36 | 26 | 4 | 1 | 41 | 18 | 5 | 0 | 42 | 15 | 4 | 0 | 42 | 15 | 4 | 0 | 42 | 12 | 5 | 1 | 44 | 14 | 5 | 1 |
| Teriparatide | 77 | 47 | 12 | 0 | 79 | 44 | 8 | 0 | 87 | 34 | 6 | 0 | 82 | 36 | 5 | 0 | 84 | 32 | 5 | 0 | 90 | 36 | 5 | 0 |
Number of vertebral fractures observed from Visit 1 (study entry) through 104 weeks. All new or worsened vertebral fractures were defined as a deterioration of at least one grade in a semiquantitative score by X-ray assessment. Number of subjects with fractures and number of fractured vertebra(e) were counted. (NCT00433160)
Timeframe: Baseline through 104 Weeks
| Intervention | number of fractures (Number) | |
|---|---|---|
| New Fractures at 104 Weeks (n=5, n=6) | Worsening Fractures at 104 Weeks (n=2, n=2) | |
| Placebo | 7 | 3 |
| Teriparatide | 7 | 3 |
Percent change in bone mineral density (BMD) at lumbar spine (L2-L4) from baseline to the last measurement point. (NCT00433160)
Timeframe: Baseline, 76 Weeks, 104 Weeks
| Intervention | percent change in BMD (Mean) | |
|---|---|---|
| Percent Change to Week 76; n=113, n=55 | Percent Change to Week 104; n=92, n=47 | |
| Placebo | 6.39 | 9.11 |
| Teriparatide | 11.93 | 13.42 |
Percent change in bone mineral density (BMD) at lumbar spine (L2-L4) from baseline to the last measurement point. (NCT00433160)
Timeframe: Baseline to 52 weeks
| Intervention | percent change in BMD (Mean) |
|---|---|
| Percent Change to Last Measurement Point | |
| Placebo | 0.04 |
| Teriparatide | 9.82 |
Percent change in bone mineral density (BMD) at total hip from baseline to the last measurement point. (NCT00433160)
Timeframe: Baseline, 76 Weeks, 104 Weeks
| Intervention | percent change in BMD (Mean) | |
|---|---|---|
| Percent Change to Week 76; n=112, n=54 | Percent Change to Week 104; n=91, n=46 | |
| Placebo | 1.64 | 2.46 |
| Teriparatide | 3.02 | 3.67 |
Percent change in bone mineral density (BMD) at total hip from baseline to the last measurement point. (NCT00433160)
Timeframe: Baseline to 52 Weeks
| Intervention | percent change in BMD (Mean) |
|---|---|
| Percent Change to Last Measurement Point | |
| Placebo | -0.22 |
| Teriparatide | 2.66 |
Percent change in bone mineral density at lumbar spine (L1-L4) from baseline to the last measurement point. (NCT00433160)
Timeframe: Baseline, 76 Weeks, 104 Weeks
| Intervention | percent change in BMD (Mean) | |
|---|---|---|
| Percent Change to Week 76; n=113, n=55 | Percent Change to Week 104; n=92, n=47 | |
| Placebo | 6.63 | 9.46 |
| Teriparatide | 12.24 | 14.01 |
Percent change in bone mineral density at lumbar spine (L1-L4) from baseline to the last measurement point. (NCT00433160)
Timeframe: Baseline to 52 Weeks
| Intervention | percent change in BMD (Mean) |
|---|---|
| Percent Change to Last Measurement Point | |
| Placebo | 0.11 |
| Teriparatide | 10.23 |
Percent change in bone mineral density at femoral neck from baseline to the last measurement point. (NCT00433160)
Timeframe: Baseline, 76 Weeks, 104 Weeks
| Intervention | percent change in BMD (Mean) | |
|---|---|---|
| Percent Change to Week 76; n=112, n=54 | Percent Change to Week 104; n=91, n=46 | |
| Placebo | 1.17 | 2.19 |
| Teriparatide | 2.68 | 3.26 |
Percent change in bone mineral density at femoral neck from baseline to the last measurement point. (NCT00433160)
Timeframe: Baseline to 52 Weeks
| Intervention | percent change in BMD (Mean) |
|---|---|
| Percent Change to Last Measurement Point | |
| Placebo | 0.46 |
| Teriparatide | 2.24 |
Percent change in serum type I collagen crosslinked C-telepeptide (CTX) from baseline to the individual visits and last measurement point. (NCT00433160)
Timeframe: Baseline, 76 Weeks, 104 Weeks
| Intervention | percent change in CTX (Mean) | |
|---|---|---|
| Percent Change to Week 76; n=104, n=53 | Percent Change to Week 104; n=85, n=45 | |
| Placebo | 86.98 | 72.84 |
| Teriparatide | 85.85 | 54.39 |
Percent change in serum type I collagen crosslinked C-telopeptide (CTX) from baseline to the individual visits and last measurement point. (NCT00433160)
Timeframe: Baseline to Weeks 4, 12, 24, 52
| Intervention | percent change in CTX (Mean) | ||||
|---|---|---|---|---|---|
| Percent Change to Week 4 (n=124, n=63) | Percent Change to Week 12 (n=121, n=61) | Percent Change to Week 24 (n=119, n=59) | Percent Change to Week 52 (n=113, n=58) | Percent Change to Last Measurement (n=126, n=65) | |
| Placebo | -2.05 | -3.56 | 4.39 | 13.50 | 11.64 |
| Teriparatide | 2.78 | 46.52 | 82.27 | 84.81 | 79.41 |
Percent change in serum procollagen I N-terminal propeptide (PINP) from baseline to the individual visits and last measurement point. (NCT00433160)
Timeframe: Baseline, 76 Weeks, 104 Weeks
| Intervention | percent change in PINP (Mean) | |
|---|---|---|
| Percent change to Week 76; n=113, n=55 | Percent change to Week 104; n=92, n=47 | |
| Placebo | 97.28 | 134.89 |
| Teriparatide | 115.45 | 74.71 |
Percent change in serum procollagen I N-terminal propeptide (PINP) from baseline to the individual visits and last measurement point. (NCT00433160)
Timeframe: Baseline to Weeks 4, 12, 24, and 52
| Intervention | percent change in PINP (Mean) | ||||
|---|---|---|---|---|---|
| Percent Change to Week 4 (n=136, n=66) | Percent Change to Week 12 (n=131, n=64) | Percent Change to Week 24 (n=127, n=61) | Percent Change to Week 52 (n=121, n=60) | Percent Change to Last Measurement (n=136,n=66) | |
| Placebo | -9.58 | -16.89 | -19.10 | -14.18 | -13.82 |
| Teriparatide | 90.67 | 89.58 | 114.12 | 116.11 | 111.74 |
"Vertebral and nonvertebral fractures assessed by the investigator or subinvestigator after starting the study treatment. Traumatic fractures were those caused by falling from above standing height or a high velocity (car) accident. Fractures were assessed to be fragility if they occurred without trauma." (NCT00433160)
Timeframe: Baseline Through 104 Weeks
| Intervention | number of fractures (Number) | |||
|---|---|---|---|---|
| Vertebral Fracture - Fragility - 104 Weeks | Vertebral Fracture - Traumatic - 104 Weeks | Non-Vertebra Fracture - Fragility - 104 Weeks | Non-Vertebra Fracture - Traumatic - 104 Weeks | |
| Placebo | 1 | 0 | 1 | 4 |
| Teriparatide | 0 | 0 | 1 | 3 |
BMD measurements of the lumbar spine (L1-L4) by Dual X-ray absorptiometry (DXA) were performed on all patients at screening, and Weeks 13, 26, and 52 (or early termination). Every attempt was made to obtain the BMD measurements at the scheduled visit. If this was not possible, a BMD measurement ± 7 days from the scheduled visit was obtained. For the Final DXA at Week 52, the window was 10 - 15 days prior to the final study visit. BMD scans were acquired locally and all results sent to a central reader for evaluation. (NCT00439244)
Timeframe: Baseline through Week 52
| Intervention | Percent change (Least Squares Mean) |
|---|---|
| Zoledronic Acid Plus Teriparatide | 7.51 |
| Zoledronic Acid | 4.37 |
| Placebo Zoledronic Acid Plus Teriparatide | 7.05 |
BMD measurements of the total hip by Dual X-ray absorptiometry (DXA) were performed on all patients at screening, and Weeks 13, 26, and 52 (or early termination). Every attempt was made to obtain the BMD measurements at the scheduled visit. If this was not possible, a BMD measurement ± 7 days from the scheduled visit was obtained. For the final DXA at Week 52, the window was 10 - 15 days prior to the final study visit. BMD scans were acquired locally and all results sent to a central reader for evaluation. (NCT00439244)
Timeframe: Baseline through Week 13, Week 26 and Week 52
| Intervention | Percent Change (Least Squares Mean) | ||
|---|---|---|---|
| At Week 13 (n= 127, 133, 133) | At Week 26 (n= 128, 130, 133) | At Week 52 (n= 123, 129, 129) | |
| Placebo Zoledronic Acid Plus Teriparatide | 0.75 | 0.89 | 1.10 |
| Zoledronic Acid | 1.53 | 1.73 | 2.16 |
| Zoledronic Acid Plus Teriparatide | 2.54 | 2.31 | 2.33 |
Specialized tests for markers of bone formation such as β-CTx were performed at Baseline, and Weeks 4, 8, 26, 39, and 52. The amount of serum β-CTx was determined by the central laboratory. (NCT00439244)
Timeframe: At Baseline, Week 4, Week 8, Week 26, Week 39 and Week 52
| Intervention | ng/mL (Mean) | |||||
|---|---|---|---|---|---|---|
| At Baseline (n= 126, 129, 121) | At Week 4 (n= 109, 110, 104) | At Week 8 (n= 106, 107, 98) | At Week 26 (n= 116, 119, 114) | At Week 39 (n= 110, 115, 110) | At Week 52 (n= 110, 113, 112) | |
| Placebo Zoledronic Acid Plus Teriparatide | 0.46 | 0.45 | 0.60 | 0.90 | 0.89 | 0.83 |
| Zoledronic Acid | 0.44 | 0.05 | 0.07 | 0.12 | 0.15 | 0.17 |
| Zoledronic Acid Plus Teriparatide | 0.45 | 0.05 | 0.09 | 0.43 | 0.57 | 0.64 |
Specialized tests for markers of bone formation such as n-terminal propeptide of type I collagen (P1NP) were performed at Baseline, and Weeks 4, 8, 26, 39, and 52. The amount of serum P1NP was determined by the central laboratory. (NCT00439244)
Timeframe: At Baseline, Week 4, Week 8, Week 26, Week 39 and Week 52
| Intervention | ng/mL (Mean) | |||||
|---|---|---|---|---|---|---|
| At Baseline (n= 126, 129, 121) | At Week 4 (n= 109, 110, 104) | At Week 8 (n= 106, 107, 98) | At Week 26 (n= 116, 119, 114) | At Week 39 (n= 110, 115, 110) | At Week 52 (n= 110, 113, 112) | |
| Placebo Zoledronic Acid Plus Teriparatide | 55.69 | 93.63 | 99.27 | 156.97 | 153.92 | 137.53 |
| Zoledronic Acid | 53.64 | 39.57 | 21.68 | 18.32 | 20.69 | 23.49 |
| Zoledronic Acid Plus Teriparatide | 52.72 | 61.74 | 39.91 | 65.26 | 97.00 | 112.87 |
BMD measurements of the lumbar spine (L1-L4) by Dual X-ray absorptiometry (DXA) were performed on all patients at screening, and Weeks 13, 26, and 52 (or early termination). Every attempt was made to obtain the BMD measurements at the scheduled visit. If this was not possible, a BMD measurement ± 7 days from the scheduled visit was obtained. For the Final DXA at Week 52, the window was 10 - 15 days prior to the final study visit. BMD scans were acquired locally and all results sent to a central reader for evaluation. (NCT00439244)
Timeframe: Baseline through Week 13 and Week 26
| Intervention | Percent Change (Least Squares Mean) | |
|---|---|---|
| At Week 13 (n= 127, 131, 131) | At Week 26 (n= 128, 130, 132) | |
| Placebo Zoledronic Acid Plus Teriparatide | 2.88 | 4.45 |
| Zoledronic Acid | 2.97 | 3.87 |
| Zoledronic Acid Plus Teriparatide | 4.65 | 6.31 |
Blood samples were collected at Baseline (Day 0), Week 4, Month 3, 6, and 12 for measurement of CTX1. (NCT00471237)
Timeframe: Baseline (Day 0), Week 4, Month 3, 6, and 12
| Intervention | nanogram per litre (ng/L) (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Baseline | Week 4 | Month 3 | Month 6 | Month 12 | |
| Placebo | 625.2 | 530.7 | 523.5 | 517.6 | 525.1 |
Blood samples were collected at Baseline (Day 0), Week 4, Month 3, 6, and 12 for measurement of CTX1. (NCT00471237)
Timeframe: Baseline (Day 0), Week 4, Month 3, 6, and 12
| Intervention | nanogram per litre (ng/L) (Least Squares Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Baseline | Baseline, Placebo contrast | Week 4 | Week 4, Placebo contrast | Month 3 | Month 3, Placebo contrast | Month 6 | Month 6, Placebo contrast | Month 12 | Month 12, Placebo contrast | |
| Alendronate, 70 mg, Capsule, OW | 630.4 | 1.01 | 288.0 | 0.54 | 257.1 | 0.49 | 235.9 | 0.46 | 158.3 | 0.30 |
| Ronacaleret, 100 mg Tablet, OD | 635.3 | 1.02 | 515.2 | 0.97 | 598.5 | 1.14 | 648.2 | 1.25 | 695.2 | 1.32 |
| Ronacaleret, 200 mg Tablet, OD | 632.0 | 1.01 | 525.4 | 0.99 | 688.9 | 1.32 | 777.1 | 1.50 | 806.1 | 1.54 |
| Ronacaleret, 300 mg Tablet, OD | 587.9 | 0.94 | 506.1 | 0.95 | 723.2 | 1.38 | 859.6 | 1.66 | 852.8 | 1.62 |
| Ronacaleret, 400 mg Tablet, OD | 645.5 | 1.03 | 529.2 | 1.00 | 818.9 | 1.56 | 964.3 | 1.86 | 991.9 | 1.89 |
| Teriparatide, 20 mcg, SC Injection, OD | 564.0 | 0.90 | 576.1 | 1.09 | 864.1 | 1.65 | 1112 | 2.15 | 1071 | 2.04 |
Full 12-lead ECGs pre-dose at screening and visits 6, 8, 11, 12 and 14 were recorded. Participants rested supine or seated for at least 10 minutes before each reading. All ECGs were transmitted to a central reviewer for blinded assessment. The central reviewer measured the following parameters and provide a clinical interpretation: heart rate, RR interval, PR interval, QRS interval, QT (uncorrected) interval, QTcB (Bazett's correction) interval, QTcF (Fridericia's correction) interval. The central reviewer was provided the investigator or designated qualified site physician with a central ECG report or confirmatory report to assist them in identifying any clinically significant abnormalities that would preclude the participant from further participation in the study. (NCT00471237)
Timeframe: Up to 12 months
| Intervention | Participants (Count of Participants) |
|---|---|
| Placebo | 1 |
| Ronacaleret, 100 mg Tablet, OD | 5 |
| Ronacaleret, 200 mg Tablet, OD | 4 |
| Ronacaleret, 300 mg Tablet, OD | 3 |
| Ronacaleret, 400 mg Tablet, OD | 3 |
| Alendronate, 70 mg, Capsule, OW | 5 |
| Teriparatide, 20 mcg, SC Injection, OD | 0 |
Participants with albumin-adjusted serum calcium pre-dose values of >11.0 mg/ deciliter (dL) or post-dose values of >12.0 mg/dL were recorded as participants with hypercalcemia. Number of participant with hypercalcemia were reported. (NCT00471237)
Timeframe: Up to Month 12
| Intervention | Participants (Count of Participants) |
|---|---|
| Placebo | 0 |
| Ronacaleret, 100 mg Tablet, OD | 1 |
| Ronacaleret, 200 mg Tablet, OD | 1 |
| Ronacaleret, 300 mg Tablet, OD | 4 |
| Ronacaleret, 400 mg Tablet, OD | 11 |
| Alendronate, 70 mg, Capsule, OW | 0 |
| Teriparatide, 20 mcg, SC Injection, OD | 1 |
A confirmed albumin-adjusted serum calcium pre-dose value of >11.0 mg/dL or post-dose value of >12.0 mg/dL was set as a withdrawal criteria for the study. Number of participants who met this pre-defined stopping criteria were reported. (NCT00471237)
Timeframe: Up to Month 12
| Intervention | Participants (Count of Participants) |
|---|---|
| Placebo | 0 |
| Ronacaleret, 100 mg Tablet, OD | 0 |
| Ronacaleret, 200 mg Tablet, OD | 0 |
| Ronacaleret, 300 mg Tablet, OD | 0 |
| Ronacaleret, 400 mg Tablet, OD | 0 |
| Alendronate, 70 mg, Capsule, OW | 0 |
| Teriparatide, 20 mcg, SC Injection, OD | 0 |
DXA scanners from Hologic and GE Lunar was used to measure BMD by a DXA scan. At least two vertebrae (L1-L4) that were suitable for measurement of BMD were evaluated. The same scanner was used throughout the study for all measurements for a given participant. DXA scans were sent to a central reading facility for quality control and central analysis. Assessments performed on Day 0 were considered as Baseline. Percent change from Baseline was computed as (change from baseline / baseline value) * 100%. Percent change from Baseline in areal bone mineral density (aBMD) was reported. (NCT00471237)
Timeframe: Baseline (Day 0) and 12 Months
| Intervention | Percent change in BMD (Least Squares Mean) |
|---|---|
| Placebo | 0.03 |
| Ronacaleret, 100 mg Tablet, OD | 0.32 |
| Ronacaleret, 200 mg Tablet, OD | 1.39 |
| Ronacaleret, 300 mg Tablet, OD | 1.61 |
| Ronacaleret, 400 mg Tablet, OD | 1.62 |
| Alendronate, 70 mg, Capsule, OW | 4.54 |
Blood samples were collected and analyzed for concentrations of ronacaleret. The individual blood concentration-time data from the intensive pharmacokinetic and pharmacodynamics subgroup of participants were analyzed by standard noncompartmental methods. Blood samples were collected and analyzed for concentrations of ronacaleret. The individual blood concentration-time data from the intensive PK-PD subgroup of participants were analyzed by standard noncompartmental methods. Following log transformation, Cmax of ronacaleret were separately analyzed by ANOVA using mixed effects model, fitting treatment and country/region as fixed effects. (NCT00471237)
Timeframe: Pre-dose (0.0 h) and 12 h post dose at Week 4, 20, 40 min, 1, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, 1-4, 8-12, and 24 h at Month 3, 6 and 12
| Intervention | ng/mL (Geometric Mean) | |
|---|---|---|
| Cmax. Month 6 | Cmax. Month 12 | |
| Ronacaleret, 100 mg Tablet, OD | 572.10 | 661.70 |
| Ronacaleret, 200 mg Tablet, OD | 1050.42 | 999.91 |
| Ronacaleret, 300 mg Tablet, OD | 1756.45 | 2254.26 |
| Ronacaleret, 400 mg Tablet, OD | 1556.58 | 1506.45 |
QCT is a three-dimensional non-projectional technique to quantify BMD with a number of advantages to other densitometric techniques. Cortical and trabecular bone can be separated, trabecular VOI are largely independent of degenerative changes in the spine and 3 dimensional geometric parameters can be determined. BMD as measured by QCT is a true density measured in g/cm^3 in contrast to DXA Which determines an areal density measured in g/cm^2. Baseline values were assessed on Day 0. Percent change from Baseline was computed as (change from baseline / baseline value) * 100%. (NCT00471237)
Timeframe: Baseline (Day 0) and Month 12
| Intervention | Percent change in VOI (Mean) |
|---|---|
| Placebo | 0.04 |
| Ronacaleret, 100 mg Tablet, OD | 0.85 |
| Ronacaleret, 200 mg Tablet, OD | 3.01 |
| Ronacaleret, 300 mg Tablet, OD | 3.58 |
| Ronacaleret, 400 mg Tablet, OD | 3.54 |
| Alendronate, 70 mg, Capsule, OW | 5.39 |
| Teriparatide, 20 mcg, SC Injection, OD | 12.23 |
The potential clinical importance ranges (low and high) of the vital sign parameters-systolic blood pressure (> 30 millimeter of mercury [mmHg] decrease from Baseline, > 30 mmHg increase from Baseline), diastolic blood pressure (> 20 mmHg decrease from Baseline and > 20 mmHg increase from Baseline) and heart rate (<45 and >120 beats per minute). Only those parameters for which at least one value of potential clinical importance was reported are summarized. The number of participants with potential clinical important vital parameter findings at any visit were reported. (NCT00471237)
Timeframe: Up to 12 Months
| Intervention | Participants (Count of Participants) | ||||
|---|---|---|---|---|---|
| Systolic Blood Pressure, High | Systolic Blood Pressure, Low | Diastolic Blood Pressure, High | Diastolic Blood Pressure, Low | Heart Rate, Low | |
| Alendronate, 70 mg, Capsule, OW | 8 | 8 | 3 | 10 | 0 |
| Placebo | 5 | 6 | 2 | 8 | 2 |
| Ronacaleret, 100 mg Tablet, OD | 10 | 8 | 6 | 9 | 0 |
| Ronacaleret, 200 mg Tablet, OD | 8 | 10 | 5 | 4 | 1 |
| Ronacaleret, 300 mg Tablet, OD | 9 | 6 | 1 | 12 | 1 |
| Ronacaleret, 400 mg Tablet, OD | 11 | 4 | 6 | 10 | 1 |
| Teriparatide, 20 mcg, SC Injection, OD | 1 | 3 | 1 | 2 | 0 |
The hematology parameters analyzed were white blood cells (WBC) count with differential WBC count, red blood cells, haemoglobin, haematocrit, mean corpuscular volume and platelet count. The clinical chemistry parameters analyzed were sodium, potassium, calcium, calcium (albumin adjusted), phosphate, bicarbonate, creatinine, bilirubin (total), alanine amino transferase, aspartate amino transferase, glucose, albumin, alkaline phosphatase, creatine phosphokinase, urea, uric acid, total protein, 25-OH vitamin D, 1,25-2(OH) vitamin D, whole parathyroid hormone (PTH 1-84)) and intact PTH (1-84 and 7-84). Only those parameters for which at least one value of potential clinical importance was reported are summarized. The number of participants with potential clinical important laboratory findings at any visit were reported. (NCT00471237)
Timeframe: Up to Month 12
| Intervention | Participants (Count of Participants) | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Monocytes- high | Total neutrophils- high | Total neutrophils- low | Eosinophils- high | Glucose- high | Glucose- low | Basophils- high | Hematocrit- low | Hemoglobin- high | Hemoglobin- low | Platelets- high | White Blood Cell- high | White Blood Cell- low | Calcium- high | Phosphorus- high | Alkaline Phosphatase- high | Total bilirubin- high | |
| Alendronate, 70 mg, Capsule, OW | 28 | 6 | 13 | 11 | 5 | 0 | 1 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 1 | 0 |
| Placebo | 17 | 9 | 16 | 12 | 10 | 3 | 2 | 2 | 1 | 2 | 2 | 1 | 1 | 0 | 1 | 0 | 0 |
| Ronacaleret, 100 mg Tablet, OD | 14 | 11 | 5 | 8 | 6 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 1 | 1 |
| Ronacaleret, 200 mg Tablet, OD | 19 | 10 | 8 | 11 | 9 | 4 | 1 | 0 | 1 | 0 | 1 | 2 | 0 | 1 | 0 | 0 | 2 |
| Ronacaleret, 300 mg Tablet, OD | 17 | 10 | 8 | 18 | 5 | 0 | 0 | 2 | 0 | 2 | 0 | 0 | 2 | 1 | 1 | 3 | 1 |
| Ronacaleret, 400 mg Tablet, OD | 18 | 4 | 14 | 19 | 4 | 3 | 1 | 0 | 1 | 1 | 0 | 1 | 0 | 1 | 0 | 3 | 1 |
| Teriparatide, 20 mcg, SC Injection, OD | 6 | 4 | 4 | 6 | 3 | 0 | 0 | 1 | 1 | 1 | 0 | 1 | 0 | 0 | 1 | 0 | 0 |
Responder rate of participants who remained the same or had any improvement as compared to baseline in DXA BMD of vertebra, femur and vertebra plus femur were reported. Baseline values were assessed on Day 0. Percent change (improvement) from Baseline was computed as (change from baseline / baseline value) * 100%. (NCT00471237)
Timeframe: Baseline (Day 0), Month 5, 6 and 12
| Intervention | Participants (Count of Participants) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Month 5, Vertebra, BMD % change >=0 | Month 5, Femur, BMD % change >=0 | Month 5, Vertebra + Femur, BMD % change >=0 | Month 6, Vertebra, BMD % change >=0 | Month 6, Femur, BMD % change >=0 | Month 6, Vertebra + Femur, BMD % change >=0 | Month 12, Vertebra, BMD % change >=0 | Month 12, Femur, BMD % change >=0 | Month 12, Vertebra + Femur, BMD % change >=0 | Early Withdrawal, Vertebra, BMD % change >=0 | Early Withdrawal, Femur, BMD % change >=0 | Early Withdrawal, Vertebra + Femur, BMD %change>=0 | |
| Alendronate, 70 mg, Capsule, OW | 0 | 0 | 0 | 1 | 1 | 1 | 44 | 40 | 35 | 0 | 0 | 0 |
| Placebo | 0 | 0 | 0 | 0 | 0 | 0 | 16 | 20 | 10 | 1 | 1 | 1 |
| Ronacaleret, 100 mg Tablet, OD | 0 | 0 | 0 | 0 | 0 | 0 | 29 | 23 | 19 | 1 | 1 | 1 |
| Ronacaleret, 200 mg Tablet, OD | 1 | 1 | 1 | 0 | 0 | 0 | 32 | 14 | 12 | 1 | 0 | 0 |
| Ronacaleret, 300 mg Tablet, OD | 0 | 0 | 0 | 0 | 0 | 0 | 35 | 19 | 17 | 2 | 1 | 1 |
| Ronacaleret, 400 mg Tablet, OD | 1 | 0 | 0 | 0 | 0 | 0 | 31 | 16 | 16 | 1 | 1 | 1 |
| Teriparatide, 20 mcg, SC Injection, OD | 0 | 0 | 0 | 0 | 0 | 0 | 34 | 25 | 24 | 1 | 1 | 1 |
DXA scanners from Hologic and GE Lunar was used to measure BMD by a DXA scan. At least two vertebrae (L1-L4) that were suitable for measurement of BMD were evaluated. The same scanner was used throughout the study for all measurements for a given participant. DXA scans were sent to a central reading facility for quality control and central analysis. Baseline values were assessed on Day 0. Percent Change from Baseline was computed as (change from baseline / baseline value) * 100%. Percent change from baseline to month 6 and 12 in aBMD of hip (total hip, femoral neck and trochanter) were reported. (NCT00471237)
Timeframe: Baseline (Day 0), Month 6 and Month 12
| Intervention | Percent change in BMD (Least Squares Mean) | |
|---|---|---|
| Total Hip aBMD, Month 6 | Total Hip aBMD, Month 12 | |
| Alendronate, 70 mg, Capsule, OW | 1.84 | 2.70 |
| Placebo | 0.42 | 0.27 |
| Ronacaleret, 100 mg Tablet, OD | -0.26 | -0.62 |
| Ronacaleret, 200 mg Tablet, OD | -0.37 | -0.75 |
| Ronacaleret, 300 mg Tablet, OD | -0.86 | -1.07 |
| Ronacaleret, 400 mg Tablet, OD | -0.88 | -1.31 |
Percent change in thickness of femur neck cortical VOI thickness and trochanter cortical VOI thickness were at Month 12 measured by QCT were reported. Assessments performed on Day 0 were considered as Baseline. Percent change from Baseline was computed as (change from baseline / baseline value) * 100%. (NCT00471237)
Timeframe: Baseline (Day 0) and Month 12
| Intervention | Percent change in cortical thickness (Mean) | |
|---|---|---|
| Neck cortical VOI Thickness | Trochanter cortical VOI Thickness | |
| Alendronate, 70 mg, Capsule, OW | -0.13 | 0.81 |
| Placebo | -0.85 | -1.00 |
| Ronacaleret, 100 mg Tablet, OD | -0.13 | 0.76 |
| Ronacaleret, 200 mg Tablet, OD | 1.12 | 1.01 |
| Ronacaleret, 300 mg Tablet, OD | -0.88 | -0.82 |
| Ronacaleret, 400 mg Tablet, OD | 0.32 | 1.60 |
| Teriparatide, 20 mcg, SC Injection, OD | 0.39 | 0.76 |
QCT is a three-dimensional non-projectional technique to quantify BMD with a number of advantages to other densitometric techniques. Cortical and trabecular bone can be separated, trabecular volume of interest (VOI) are largely independent of degenerative changes in the spine and 3 dimensional geometric parameters can be determined. BMD as measured by QCT is a true density measured in g/cm^3 in contrast to DXA Which determines an areal density measured in g/cm^2. Baseline values were assessed on Day 0. Percent change from Baseline was computed as (change from baseline / baseline value) * 100%. Percent change from Baseline to month 12 in the volumetric integral, cortical, and trabecular density (BMD) at the hip and lumbar spine measured by QCT were reported. (NCT00471237)
Timeframe: Baseline (Day 0) and Month 12
| Intervention | Percent change in BMD (Mean) | |||||
|---|---|---|---|---|---|---|
| Total vertebra integral VOI BMD | Mid vertebra integral VOI BMD | Mid Cylinder trabecular VOI BMD | Mid Osteo trabecular VOI BMD | Total vertebra trabecular VOI BMD | Mid Osteo cortical VOI BMD | |
| Alendronate, 70 mg, Capsule, OW | 5.04 | 4.85 | 4.88 | 5.15 | 4.97 | 4.98 |
| Placebo | -0.98 | -1.31 | -2.45 | -2.21 | -2.46 | -0.30 |
| Ronacaleret, 100 mg Tablet, OD | 1.09 | 1.20 | 1.75 | 1.81 | 1.67 | 0.63 |
| Ronacaleret, 200 mg Tablet, OD | 3.00 | 4.65 | 6.17 | 7.06 | 5.81 | 2.37 |
| Ronacaleret, 300 mg Tablet, OD | 3.91 | 6.06 | 8.99 | 9.54 | 8.52 | 2.57 |
| Ronacaleret, 400 mg Tablet, OD | 4.83 | 7.33 | 13.29 | 13.21 | 11.40 | 1.22 |
| Teriparatide, 20 mcg, SC Injection, OD | 14.80 | 17.97 | 24.37 | 24.21 | 23.82 | 9.25 |
Blood samples were collected at Baseline (Day 0), Week 4, Month 3, 6, and 12 for measurement of BALP. (NCT00471237)
Timeframe: Baseline (Day 0), Week 4, Month 3, 6, and 12
| Intervention | mcg/L (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Baseline | Week 4 | Month 3 | Month 6 | Month 12 | |
| Placebo | 14.46 | 14.02 | 12.66 | 12.81 | 13.25 |
QCT is a three-dimensional non-projectional technique to quantify BMD with a number of advantages to other densitometric techniques. Cortical and trabecular bone can be separated, trabecular VOI are largely independent of degenerative changes in the spine and 3 dimensional geometric parameters can be determined. BMD as measured by QCT is a true density measured in mg/cm^3 in contrast to DXA Which determines an areal density measured in g/cm^2. Baseline values were assessed on Day 0. Percent change from Baseline was computed as (change from baseline / baseline value) * 100%. (NCT00471237)
Timeframe: Baseline (Day 0) and Month 12
| Intervention | Percent change in BMD (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Femur integral VOI BMD | Femur trabecular VOI BMD | Femur cortical VOI BMD | Neck integral VOI BMD | Neck trabecular VOI BMD | Neck cortical VOI BMD | Trochanter integral VOI BMD | Trochanter trabecular VOI BMD | Trochanter cortical VOI BMD | |
| Alendronate, 70 mg, Capsule, OW | 2.70 | 3.05 | 2.44 | 1.65 | 2.77 | 1.10 | 3.15 | 3.55 | 3.33 |
| Placebo | 0.02 | -0.36 | 1.11 | -0.10 | -0.95 | 1.23 | -0.58 | -1.62 | 0.56 |
| Ronacaleret, 100 mg Tablet, OD | -0.05 | -0.40 | -0.32 | 0.16 | -2.19 | 0.44 | -0.16 | -1.34 | -0.70 |
| Ronacaleret, 200 mg Tablet, OD | -0.81 | -2.16 | -1.46 | -0.94 | -2.68 | -1.67 | -1.53 | -2.54 | -1.53 |
| Ronacaleret, 300 mg Tablet, OD | -0.53 | 1.16 | -1.06 | -1.20 | 1.35 | -1.85 | -1.16 | 2.12 | -1.48 |
| Ronacaleret, 400 mg Tablet, OD | -0.15 | 2.81 | -1.79 | -1.45 | 3.05 | -2.80 | -0.98 | 2.10 | -2.59 |
| Teriparatide, 20 mcg, SC Injection, OD | 3.92 | 13.19 | 0.22 | 2.06 | 11.27 | -0.69 | 4.96 | 14.12 | 1.99 |
Blood samples were collected at Baseline (Day 0), Week 4, Month 3, 6, and 12 for measurement of BALP. (NCT00471237)
Timeframe: Baseline (Day 0), Week 4, Month 3, 6, and 12
| Intervention | mcg/L (Least Squares Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Baseline | Baseline, Placebo contrast | Week 4 | Week 4, Placebo contrast | Month 3 | Month 3, Placebo contrast | Month 6 | Month 6, Placebo contrast | Month 12 | Month 12, Placebo contrast | |
| Alendronate, 70 mg, Capsule, OW | 14.31 | 0.99 | 13.68 | 0.98 | 9.44 | 0.75 | 8.36 | 0.65 | 8.42 | 0.64 |
| Ronacaleret, 100 mg Tablet, OD | 14.96 | 1.03 | 14.72 | 1.05 | 15.23 | 1.20 | 16.31 | 1.27 | 16.64 | 1.26 |
| Ronacaleret, 200 mg Tablet, OD | 14.24 | 0.98 | 14.51 | 1.03 | 15.44 | 1.22 | 17.43 | 1.36 | 18.80 | 1.42 |
| Ronacaleret, 300 mg Tablet, OD | 15.06 | 1.04 | 15.97 | 1.14 | 18.77 | 1.48 | 22.18 | 1.73 | 23.36 | 1.76 |
| Ronacaleret, 400 mg Tablet, OD | 14.12 | 0.98 | 15.72 | 1.12 | 17.85 | 1.41 | 21.47 | 1.68 | 23.28 | 1.76 |
| Teriparatide, 20 mcg, SC Injection, OD | 14.50 | 1.00 | 16.19 | 1.15 | 16.53 | 1.31 | 17.63 | 1.38 | 19.08 | 1.44 |
Blood samples were collected and analyzed for concentrations of ronacaleret. The individual blood concentration-time data from the intensive pharmacokinetic and pharmacodynamics subgroup of participants were analyzed by standard noncompartmental methods. Blood samples were collected and analyzed for concentrations of ronacaleret. The individual blood concentration-time data from the intensive PK-PD subgroup of participants were analyzed by standard noncompartmental methods. Following log transformation, AUC(0-t) and AUC(0-τ) of ronacaleret were separately analyzed by ANOVA using mixed effects model, fitting treatment and country/region as fixed effects. (NCT00471237)
Timeframe: Pre-dose (0.0 h) and 12 h post dose at Week 4, 20, 40 min, 1, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, 1-4, 8-12, and 24 h at Month 3, 6 and 12
| Intervention | nanogram*hour per millilitre (ng*hr/mL) (Geometric Mean) | |||
|---|---|---|---|---|
| AUC 0-t, Month 6 | AUC 0-t, Month 12 | AUC 0-tau, Month 6 | AUC 0-tau, Month 12 | |
| Ronacaleret, 100 mg Tablet, OD | 2495.8751 | 2766.6822 | 3628.0901 | 3922.9369 |
| Ronacaleret, 200 mg Tablet, OD | 4575.8746 | 4548.6490 | 6428.5540 | 6455.1756 |
| Ronacaleret, 300 mg Tablet, OD | 7545.3302 | 9259.3127 | 10825.9083 | 14827.6940 |
| Ronacaleret, 400 mg Tablet, OD | 6712.0537 | 6798.4219 | 9810.4614 | 10079.2847 |
Blood samples were collected at Baseline (Day 0), Week 4, Month 3, 6, and 12 for measurement of P1NP. (NCT00471237)
Timeframe: Baseline (Day 0), Week 4, Month 3, 6, and 12
| Intervention | Microgram per Litre (mcg/L) (Least Squares Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Baseline | Baseline, Placebo contrast | Week 4 | Week 4, Placebo contrast | Month 3 | Month 3, Placebo contrast | Month 6 | Month 6, Placebo contrast | Month 12 | Month 12, Placebo contrast | |
| Alendronate, 70 mg, Capsule, OW | 47.71 | 1.00 | 43.66 | 0.96 | 20.15 | 0.51 | 16.41 | 0.43 | 16.98 | 0.42 |
| Teriparatide, 20 mcg, SC Injection, OD | 48.57 | 1.02 | 92.74 | 2.05 | 99.74 | 2.52 | 117.8 | 3.07 | 119.0 | 2.92 |
| Ronacaleret, 100 mg Tablet, OD | 45.59 | 0.96 | 49.67 | 1.10 | 49.99 | 1.26 | 56.37 | 1.47 | 61.43 | 1.51 |
| Ronacaleret, 200 mg Tablet, OD | 47.70 | 1.00 | 57.36 | 1.27 | 65.21 | 1.65 | 75.73 | 1.97 | 82.69 | 2.03 |
| Ronacaleret, 300 mg Tablet, OD | 46.62 | 0.98 | 60.27 | 1.33 | 73.68 | 1.86 | 90.55 | 2.36 | 98.04 | 2.41 |
| Ronacaleret, 400 mg Tablet, OD | 46.19 | 0.97 | 63.46 | 1.40 | 86.84 | 2.20 | 104.6 | 2.72 | 112.6 | 2.76 |
Blood samples were collected at Baseline (Day 0), Week 4, Month 3, 6, and 12 for measurement of P1NP. (NCT00471237)
Timeframe: Baseline (Day 0), Week 4, Month 3, 6, and 12
| Intervention | Microgram per Litre (mcg/L) (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Baseline | Week 4 | Month 3 | Month 6 | Month 12 | |
| Placebo | 47.66 | 45.32 | 39.53 | 38.41 | 40.74 |
Blood samples were collected and analyzed for concentrations of ronacaleret. The individual blood concentration-time data from the intensive PK-PD subgroup of participants were analyzed by standard noncompartmental methods. Blood concentrations of ronacaleret were reported. (NCT00471237)
Timeframe: Pre-dose (0.0 hour [h]) and 12 h post dose at Week 4, 20, 40 min, 1, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, 1-4, 8-12, and 24 h at Month 3, 6 and 12
| Intervention | nanograms per millilitre (ng/mL) (Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Week 4, Pre-dose | Week 4, 8-12 h post dose | Month 6, Pre-dose | Month 6, 1-4 h post dose | Month 6, 8-12 h post dose | Month 6, 24 h post dose | Month 12, Pre-dose | Month 12, 1-4 h post dose | Month 12, 8-12 h post dose | Month 12, 24 h post dose | |
| Ronacaleret, 100 mg Tablet, OD | 41.22 | 204.82 | 21.37 | 644.90 | 186.69 | 186.21 | 20.68 | 779.92 | 203.39 | 187.23 |
| Ronacaleret, 200 mg Tablet, OD | 37.24 | 328.33 | 65.94 | 1308.35 | 385.03 | 290.74 | 33.47 | 999.63 | 262.20 | 297.20 |
| Ronacaleret, 300 mg Tablet, OD | 85.44 | 581.08 | 74.12 | 1610.74 | 576.35 | 578.63 | 147.63 | 1819.53 | 651.95 | 626.72 |
| Ronacaleret, 400 mg Tablet, OD | 79.40 | 685.14 | 117.94 | 2054.71 | 796.99 | 473.41 | 114.83 | 2128.24 | 740.18 | 512.65 |
Baseline values were assessed on Day 0. Change from Baseline was computed as values at post baseline visit minus Baseline value. Mean change from baseline in weight at Month 6, 12 and early withdrawal were reported. (NCT00471237)
Timeframe: Baseline (Day 0), Month 6, 12 and early withdrawal
| Intervention | Kilogram (Mean) | ||
|---|---|---|---|
| Month 6 | Month 12 | Early withdrawal | |
| Alendronate, 70 mg, Capsule, OW | 0.29 | 0.57 | -0.12 |
| Placebo | -0.02 | 0.32 | -0.45 |
| Ronacaleret, 100 mg Tablet, OD | 0.27 | -0.72 | 0.40 |
| Ronacaleret, 200 mg Tablet, OD | 0.45 | 1.18 | -0.34 |
| Ronacaleret, 300 mg Tablet, OD | -0.24 | -0.22 | 0.37 |
| Ronacaleret, 400 mg Tablet, OD | 0.11 | -0.48 | 0.00 |
| Teriparatide, 20 mcg, SC Injection, OD | 0.51 | 0.09 | -2.15 |
Assessments performed on Day 0 were considered as Baseline. Change from Baseline was computed as values at post baseline visit minus Baseline value. Mean change from baseline in height at Month 6 and 12 and early withdrawal were reported. (NCT00471237)
Timeframe: Baseline (Day 0), Month 6, 12 and early withdrawal
| Intervention | Centimeter (Mean) | ||
|---|---|---|---|
| Month 6 | Month 12 | Early withdrawal | |
| Alendronate, 70 mg, Capsule, OW | -0.07 | -0.08 | -0.37 |
| Placebo | -0.04 | -0.14 | 0.03 |
| Ronacaleret, 100 mg Tablet, OD | 0.17 | 0.04 | 0.17 |
| Ronacaleret, 200 mg Tablet, OD | 0.72 | 0.02 | -0.13 |
| Ronacaleret, 300 mg Tablet, OD | 0.05 | -0.09 | -0.16 |
| Ronacaleret, 400 mg Tablet, OD | -0.04 | -0.17 | -0.16 |
| Teriparatide, 20 mcg, SC Injection, OD | 0.11 | 0.11 | 0 |
DXA scanners from Hologic and GE Lunar was used to measure BMD by a DXA scan. At least two vertebrae (L1-L4) that were suitable for measurement of BMD were evaluated. The same scanner was used throughout the study for all measurements for a given participant. DXA scans were sent to a central reading facility for quality control and central analysis. Baseline values were assessed on Day 0. Percent Change from Baseline was computed as (change from baseline / baseline value) * 100%. Percent change from baseline to month 6 in aBMD was reported. (NCT00471237)
Timeframe: Baseline (Day 0) and Month 6
| Intervention | percent change in BMD (Least Squares Mean) |
|---|---|
| Placebo | 0.66 |
| Ronacaleret, 100 mg Tablet, OD | 0.21 |
| Ronacaleret, 200 mg Tablet, OD | 1.61 |
| Ronacaleret, 300 mg Tablet, OD | 0.47 |
| Ronacaleret, 400 mg Tablet, OD | 1.01 |
| Alendronate, 70 mg, Capsule, OW | 3.42 |
Blood samples were collected and analyzed for concentrations of ronacaleret. The individual blood concentration-time data from the intensive pharmacokinetic and pharmacodynamics subgroup of participants were analyzed by standard noncompartmental methods. (NCT00471237)
Timeframe: Pre-dose (0.0 h) and 12 h post dose at Week 4, 20, 40 min, 1, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, 1-4, 8-12, and 24 h at Month 3, 6 and 12
| Intervention | h (Median) | |
|---|---|---|
| Tmax, Month 6 | Tmax, Month 12 | |
| Ronacaleret, 100 mg Tablet, OD | 1.483 | 1.000 |
| Ronacaleret, 200 mg Tablet, OD | 1.250 | 1.500 |
| Ronacaleret, 300 mg Tablet, OD | 1.700 | 1.500 |
| Ronacaleret, 400 mg Tablet, OD | 1.500 | 1.500 |
Mineralizing surface done on histomorphometric assessment of percutaneous iliac crest bone biopsy. Mineralizing surface measures how much of bone is getting new mineral put on it. The structure and microscopic organization of a small piece of biopsied pelvic bone was analyzed. (NCT00473265)
Timeframe: baseline versus one year
| Intervention | percentage of surface (Mean) | |
|---|---|---|
| Baseline | Year 1 | |
| PTH1-84 | 0.7 | 7.1 |
Bone Mineral Density (BMD) as measured by Dual-energy X-ray absorptiometry (DXA). (NCT00473265)
Timeframe: baseline versus 24 months
| Intervention | percentage of change to BMD (Mean) | ||
|---|---|---|---|
| Lumbar Spine BMD | Femoral Neck BMD | Distal 1/3 Radius BMD | |
| PTH1-84 | 2.9 | 0.95 | -2.4 |
Serum and urinary calcium levels maintained by change in requirements for calcium supplementation (NCT00473265)
Timeframe: 2 years
| Intervention | grams per day of calcium supplementation (Mean) | |
|---|---|---|
| Starting requirements | Requirements at month 24 | |
| PTH1-84 | 3.03 | 1.66 |
Cortical porosity done on histomorphometric assessment of percutaneous iliac crest bone biopsy. Cortical Porosity measures how many tiny holes there are in the solid bone section. The structure and microscopic organization of a small piece of biopsied pelvic bone was analyzed. (NCT00473265)
Timeframe: baseline versus two years
| Intervention | percentage of porosity (Mean) | |
|---|---|---|
| Baseline | Year 2 | |
| PTH1-84 | 7.4 | 9.2 |
Trabecular width was obtained from histomorphometric assessment of percutaneous iliac crest bone biopsy. Trabecular width is the thickness of individual pieces of the spongy bone section. The structure and microscopic organization of a small piece of biopsied pelvic bone was analyzed. (NCT00473265)
Timeframe: baseline versus two years
| Intervention | micrometers (Mean) | |
|---|---|---|
| Baseline | Year 2 | |
| PTH1-84 | 144 | 128 |
trabecular number done on histomorphometric assessment of percutaneous iliac crest bone biopsy. Trabecular number is the number of individual pieces of the spongy bone section. The structure and microscopic organization of a small piece of biopsied pelvic bone was analyzed. (NCT00473265)
Timeframe: baseline versus two years
| Intervention | mm^-1 (Mean) | |
|---|---|---|
| Baseline | Year 2 | |
| PTH1-84 | 1.74 | 2.07 |
Percent Change in Lumbar Spine Bone Mineral Density from Baseline to Week 12 (NCT00489918)
Timeframe: 12 weeks
| Intervention | Percent change (Mean) |
|---|---|
| Macroflux® Placebo | 0.97 |
| Macroflux® 20 mcg | 1.55 |
| Macroflux® 30 mcg | 2.04 |
| Macroflux® 40 mcg | 2.5 |
| FORTEO® | 2.81 |
Percent Change in Total Hip Bone Mineral Density from Baseline to Week 24 (NCT00489918)
Timeframe: 24 Weeks
| Intervention | Percent change (Mean) |
|---|---|
| Macroflux® Placebo | -0.634 |
| Macroflux® 20 mcg | 0.138 |
| Macroflux® 30 mcg | 0.553 |
| Macroflux® 40 mcg | 1.331 |
| FORTEO® | 0.094 |
Percent Change in Lumbar Spine Bone Mineral Density (BMD) from Baseline to Week 24 (NCT00489918)
Timeframe: 24 weeks
| Intervention | percent change (Mean) |
|---|---|
| Macroflux® Placebo | -0.33 |
| Macroflux® 20 mcg | 2.96 |
| Macroflux® 30 mcg | 3.47 |
| Macroflux® 40 mcg | 4.97 |
| FORTEO® | 3.55 |
Absolute Change in Lumbar Spine BMD from Baseline to Week 12 (NCT00489918)
Timeframe: 12 weeks
| Intervention | g/cm^2 (Mean) |
|---|---|
| Macroflux® Placebo | 0.007 |
| Macroflux® 20 mcg | 0.011 |
| Macroflux® 30 mcg | 0.014 |
| Macroflux® 40 mcg | 0.017 |
| FORTEO® | 0.021 |
Percent Change in Femoral Neck BMD from Baseline to Week 24 (NCT00489918)
Timeframe: 24 Weeks
| Intervention | Percent change (Mean) |
|---|---|
| Macroflux® Placebo | 0.172 |
| Macroflux® 20 mcg | 0.949 |
| Macroflux® 30 mcg | 0.599 |
| Macroflux® 40 mcg | 0.750 |
| FORTEO® | -0.012 |
Three-dimensional (3-D) microstructure variables of T12 were assessed by HR-QCT. In contrast with regular QCT that assessed 3 millimeter (mm) slide thickness, HR-QCT used segmentation of 1 single vertebra with approximately 100 consecutive slides reconstructed at 300-400 micrometer (µm) slice increments covering the complete vertebral body. Least Squares (LS) Means were adjusted for age, baseline P1NP, fracture less than 12 months before study start, duration of prior bisphosphonate use, screening glucocorticoid dose, and cumulative glucocorticoid dose before and during the trial. (NCT00503399)
Timeframe: Baseline, 6 months, 18 months
| Intervention | milligram per cubic centimeter (mg/cm^3) (Least Squares Mean) | |||
|---|---|---|---|---|
| Integral BMD at 6 months | Integral BMD at 18 months | Trabecular BMD at 6 months | Trabecular BMD at 18 months | |
| Risedronate | -1.91 | 0.68 | -0.87 | 0.22 |
| Teriparatide | -0.42 | 10.72 | -0.70 | 9.53 |
P1NP was used as a serum biochemical marker of collagen synthesis, reflecting the formation of new osteoid. (NCT00503399)
Timeframe: Baseline, 3 months, 6 months, 18 months
| Intervention | micrograms per deciliter (μg/dL) (Least Squares Mean) | ||
|---|---|---|---|
| P1NP at 3 months | P1NP at 6 months | P1NP at 18 months | |
| Risedronate | -16.09 | -16.50 | -15.58 |
| Teriparatide | 27.33 | 52.55 | 28.48 |
Summary tables of serious AEs (SAEs) and all other non-serious AEs are located in the Reported Adverse Event Module. Fractures that occurred during the study were collected separately as an additional safety variable. The number of participants experiencing hypercalcemia was summarized for each treatment arm. Hypercalcemia was defined as a serum calcium level corrected for albumin of >2.7 millimole per liter (mmol/L) (10.8 milligram per deciliter [mg/dL]). (NCT00503399)
Timeframe: Baseline up to 18 months
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Serious Adverse Events (SAEs) | Other Non-serious AEs | Fractures | Hypercalcemia | |
| Risedronate | 22 | 30 | 5 | 0 |
| Teriparatide | 13 | 22 | 0 | 0 |
Least Squares (LS) Means were adjusted for age, baseline serum aminoterminal propeptide of Type I procollagen (P1NP), fracture less than 12 months before study start, duration of prior bisphosphonate use, screening glucocorticoid dose, and cumulative glucocorticoid dose before and during the trial. (NCT00503399)
Timeframe: Baseline, 18 months
| Intervention | milligram per cubic centimeter (mg/cm^3) (Least Squares Mean) |
|---|---|
| Teriparatide | 12.28 |
| Risedronate | 2.94 |
β-CTx was used as a biochemical marker of bone turnover/resorption, reflecting collagen breakdown of the bone matrix. (NCT00503399)
Timeframe: 3, 6, 18 months
| Intervention | nanograms per deciliter (ng/dL) (Least Squares Mean) | ||
|---|---|---|---|
| β-CTx at 3 months | β-CTx at 6 months | β-CTx at 18 months | |
| Risedronate | -0.15 | -0.14 | -0.11 |
| Teriparatide | 0.12 | 0.25 | 0.03 |
Least Squares (LS) Means were adjusted for age, baseline propeptide of Type I procollagen (P1NP), fracture less than 12 months before study start, duration of prior bisphosphonate use, screening glucocorticoid dose, and cumulative glucocorticoid dose before and during the trial. (NCT00503399)
Timeframe: Baseline, 6 months
| Intervention | milligram per cubic centimeter (mg/cm^3) (Least Squares Mean) |
|---|---|
| Teriparatide | 4.31 |
| Risedronate | 2.52 |
Anterior bending and axial torsion were measured using HR-QCT-based finite element analysis to determine stiffness and strength of T12. Stiffness evaluated strength of the vertebral body, defined as the slope of the initial step of the force-displacement curve. Strength of the vertebral body was evaluated under compressive loading conditions using computer simulation. LS Means were adjusted for age, baseline P1NP, fracture less than 12 months before study start, duration of prior bisphosphonate use, screening glucocorticoid dose, and cumulative glucocorticoid dose before and during the trial. (NCT00503399)
Timeframe: Baseline, 6 months, 18 months
| Intervention | Newton/millimeter/radian (N/mm/rad) (Least Squares Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Anterior bending stiffness at 6 months | Anterior bending stiffness at 18 months | Axial torsion stiffness at 6 months | Axial torsion stiffness at 18 months | Anterior bending strength at 6 months | Anterior bending strength at 18 months | Axial torsion strength at 6 months | Axial torsion strength at 18 months | |
| Risedronate | 415705.0 | 233283.0 | 77830.7 | 56639.3 | 8827.2 | 4822.0 | 3664.0 | 2545.8 |
| Teriparatide | 664969.0 | 1209225.0 | 142902.9 | 279392.8 | 12490.9 | 26046.4 | 6127.7 | 14181.3 |
Dual x-ray absorptiometry (DXA) techniques validated this measurement at skeletal sites that are at risk of osteoporotic fracture, such as lumbar spine, femoral neck, and hip. (NCT00503399)
Timeframe: Baseline, 18 months
| Intervention | grams per square centimeter (g/cm^2) (Mean) | ||
|---|---|---|---|
| Lumbar spine (n=38; n=39) | Hip (n=38; n=37) | Femoral neck (n=38; n=37) | |
| Risedronate | 0.037 | 0.007 | -0.007 |
| Teriparatide | 0.068 | 0.014 | 0.014 |
Axial compression was measured using HR-QCT-based finite element analysis to determine stiffness and strength of T12. Stiffness evaluated the strength of the vertebral body, defined as the slope of the initial step of the force-displacement curve. Strength of the vertebral body was evaluated under compressive loading conditions using computer simulation. LS Means were adjusted for age, baseline P1NP, fracture less than 12 months before study start, duration of prior bisphosphonate use, screening glucocorticoid dose, and cumulative glucocorticoid dose before and during the trial. (NCT00503399)
Timeframe: Baseline, 6 months, 18 months
| Intervention | Newton per millimeter (N/mm) (Least Squares Mean) | |||
|---|---|---|---|---|
| Axial compression stiffness at 6 months | Axial compression stiffness at 18 months | Axial compression strength at 6 months | Axial compression strength at 18 months | |
| Risedronate | 407.6 | 363.7 | 313.6 | 209.4 |
| Teriparatide | 890.7 | 1973.9 | 580.7 | 1287.5 |
Femoral neck bone mineral density (BMD) was analyzed by DXA at Week 24. (NCT00542425)
Timeframe: 6 months
| Intervention | Percent change from baseline (Mean) |
|---|---|
| Placebo | 0.79 |
| BA058 20 µg | 2.69 |
| BA058 40 µg | 2.20 |
| BA058 80 µg | 3.07 |
| Teriparatide | 1.07 |
Total analyzable hip bone mineral density (BMD) was analyzed by DXA at Week 24. (NCT00542425)
Timeframe: 6 months
| Intervention | Percent change from baseline (Mean) |
|---|---|
| Placebo | 0.39 |
| BA058 20 µg | 1.43 |
| BA058 40 µg | 1.97 |
| BA058 80 µg | 2.60 |
| Teriparatide | 0.45 |
PINP, N-terminal propeptide of type I procollagen, is a marker of anabolic bone growth. (NCT00542425)
Timeframe: 6 months
| Intervention | Percent change from baseline (Mean) |
|---|---|
| Placebo | -13.1 |
| BA058 20 µg | 20.0 |
| BA058 40 µg | 90.8 |
| BA058 80 µg | 97.2 |
| Teriparatide | 154.3 |
Total analyzable spine bone mineral density (BMD) was analyzed by DXA at Week 24. (NCT00542425)
Timeframe: 6 months
| Intervention | Percent change from baseline (Mean) |
|---|---|
| Placebo | 1.22 |
| BA058 20 µg | 3.30 |
| BA058 40 µg | 5.21 |
| BA058 80 µg | 6.11 |
| Teriparatide | 5.47 |
Total analyzable spine bone mineral density (BMD) was analyzed by DXA at Week 48. (NCT00542425)
Timeframe: 12 months
| Intervention | Percent change from baseline (Mean) |
|---|---|
| Placebo | 0.74 |
| BA058 20 µg | 5.14 |
| BA058 40 µg | 9.84 |
| BA058 80 µg | 12.94 |
| Teriparatide | 8.63 |
Finite Element Analysis of computed tomography (CT) data from spine is used to estimate the strength of a vertebral body using a virtual axial load. Least squares (LS) mean of the percent change from baseline to 18 months is from an analysis of variance (ANOVA). The model included terms for investigator site and prior bisphosphonate use. (NCT00557310)
Timeframe: Baseline, 18 months
| Intervention | % change of Newtons (Least Squares Mean) |
|---|---|
| Teriparatide | 17.43 |
Volumetric BMD is a measure of the amount of mineral in a given volume of bone. Least squares (LS) mean of the percent change from baseline to 18 months is from an analysis of variance (ANOVA). The model included terms for investigator site and prior bisphosphonate use. (NCT00557310)
Timeframe: Baseline, 18 months
| Intervention | % change of mg/cm³ (Least Squares Mean) |
|---|---|
| Teriparatide | 2.22 |
Volumetric BMD is a measure of the amount of mineral in a given volume of bone, expressed as milligram per cubic centimeter (mg/cm³). Least squares (LS) mean of the percent change from baseline to 18 months is from an analysis of variance (ANOVA). The model included terms for investigator site and prior bisphosphonate use. (NCT00557310)
Timeframe: Baseline, 18 months
| Intervention | % change of mg/cm³ (Least Squares Mean) |
|---|---|
| Teriparatide | 10.05 |
Areal BMD is a measure of the amount of mineral in a given area of bone. Least squares (LS) mean of the percent change from baseline to 18 and 24 months is from an analysis of variance (ANOVA). The model included terms for investigator site and prior bisphosphonate use. (NCT00557310)
Timeframe: Baseline, 18, 24 months
| Intervention | % change of g/cm² (Least Squares Mean) | |
|---|---|---|
| 18 month percent change (n=28) | 24 month percent change (n=25) | |
| Teriparatide | 2.792 | 2.762 |
Areal BMD is a measure of the amount of mineral in a given area of bone. Least squares (LS) mean of the percent change from baseline to 18 and 24 months is from an analysis of variance (ANOVA). The model included terms for investigator site and prior bisphosphonate use. (NCT00557310)
Timeframe: Baseline, 18, 24 months
| Intervention | % change of g/square centimeter (g/cm²) (Least Squares Mean) | |
|---|---|---|
| 18 month percent change (n=28) | 24 month percent change (n=25) | |
| Teriparatide | 7.215 | 8.702 |
Areal BMD is a measure of the amount of mineral in a given area of bone. Least squares (LS) mean of the percent change from baseline to 18 and 24 months is from an analysis of variance (ANOVA). The model included terms for investigator site and prior bisphosphonate use. (NCT00557310)
Timeframe: Baseline, 18, 24 months
| Intervention | % change of g/cm² (Least Squares Mean) | |
|---|---|---|
| 18 month percent change (n=28) | 24 month percent change (n=25) | |
| Teriparatide | -1.891 | 0.776 |
Areal BMD is a measure of the amount of mineral in a given area of bone. Least squares (LS) mean of the percent change from baseline to 18 and 24 months is from an analysis of variance (ANOVA). The model included terms for investigator site and prior bisphosphonate use. (NCT00557310)
Timeframe: Baseline, 18, 24 months
| Intervention | % change of g/cm² (Least Squares Mean) | |
|---|---|---|
| 18 month percent change (n=28) | 24 month percent change (n=25) | |
| Teriparatide | 0.292 | 1.482 |
BV/TV is the estimate of the ratio of detectable bone relative to the total volume of the region of interest. Least squares (LS) mean of the percent change from baseline to 18, 24 months is from a mixed model repeated measurements analysis. The model included terms for investigator site, prior bisphosphonate use, visit and baseline. (NCT00557310)
Timeframe: Baseline, 18, 24 months
| Intervention | % change of ratio (Least Squares Mean) | |
|---|---|---|
| 18 month percent change (n=25) | 24 month percent change (n=21) | |
| Teriparatide | 0.36 | -3.14 |
Cortical thickness (CT) is the thickness of both cortices in a given volume of bone. Least squares (LS) mean of the percent change from baseline to 18, 24 months is from a mixed model repeated measurements analysis. The model included terms for investigator site, prior bisphosphonate use, visit and baseline. (NCT00557310)
Timeframe: Baseline, 18, 24 months
| Intervention | % change of millimeter (mm) (Least Squares Mean) | |
|---|---|---|
| 18 month percent change (n=25) | 24 month percent change (n=21) | |
| Teriparatide | -0.61 | -0.22 |
CTX is a measure of bone resorption. Least squares (LS) mean of the percent change from baseline to 3, 6, 24 months is from a mixed model repeated measurements analysis. The model included terms for investigator site, prior bisphosphonate use, visit and baseline. (NCT00557310)
Timeframe: Baseline, 3, 6, 24 months
| Intervention | % change of nanogram/milliliter (ng/mL) (Least Squares Mean) | ||
|---|---|---|---|
| 3 month percent change (n=32) | 6 month percent change (n=30) | 24 month percent change (n=23) | |
| Teriparatide | 63.53 | 102.56 | 48.28 |
PINP is a measure of bone formation. Least squares (LS) mean of the percent change from baseline to 3, 6, 24 months is from a mixed model repeated measurements analysis. The model included terms for investigator site, prior bisphosphonate use, visit and baseline. (NCT00557310)
Timeframe: Baseline, 3, 6, 24 months
| Intervention | % change of microgram/Liter (µg/L) (Least Squares Mean) | ||
|---|---|---|---|
| 3 month percent change (n=32) | 6 month percent change (n=30) | 24 month percent change (n=23) | |
| Teriparatide | 145.35 | 238.04 | 118.91 |
SCR is a measure of the computed ratio of plate-like to rod-like structures in a given volume of trabecular bone and reflects the integrity of the trabecular network. The higher the value for SCR, the more intact the trabecular network. Least squares (LS) mean of the percent change from baseline to 3, 6, 12, 18, 24 months is from a mixed model repeated measurements analysis. The model included terms for investigator site, prior bisphosphonate use, visit and baseline. (NCT00557310)
Timeframe: Baseline, 3, 6, 12, 18, 24 months
| Intervention | % change of ratio (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| 3 month percent change (n=32) | 6 month percent change (n=30) | 12 month percent change (n=28) | 18 month percent change (n=25) | 24 month percent change (n=21) | |
| Teriparatide | -3.38 | 0.43 | 2.36 | 4.53 | 1.44 |
TEI is the ratio of the sum of topological parameters expected to increase with bone erosion compared to the sum of those expected to decrease. The lower the value for TEI, the more intact the trabecular network. Least squares (LS) mean of the percent change from baseline to 18, 24 months is from a mixed model repeated measurements analysis. The model included terms for investigator site, prior bisphosphonate use, visit and baseline. (NCT00557310)
Timeframe: Baseline, 18, 24 months
| Intervention | % change of ratio (Least Squares Mean) | |
|---|---|---|
| 18 month percent change (n=25) | 24 month percent change (n=21) | |
| Teriparatide | 3.36 | 8.46 |
SCR is a measure of the computed ratio of plate-like to rod-like structures in a given volume of trabecular bone and reflects the integrity of the trabecular network. The higher the value for SCR, the more intact the trabecular network. Least squares (LS) mean of the percent change from baseline to 18 months is from a mixed model repeated measurements analysis. The model included terms for investigator site, prior bisphosphonate use, visit and baseline. (NCT00557310)
Timeframe: Baseline, 18 months
| Intervention | percent (%) change of ratio (Least Squares Mean) |
|---|---|
| Teriparatide | 4.53 |
SCR is a measure of the computed ratio of plate-like to rod-like structures in a given volume of trabecular bone and reflects the integrity of the trabecular network. The higher the value for SCR, the more intact the trabecular network. Least squares (LS) mean of the percent change from baseline to 24 months is from a mixed model repeated measurements analysis. The model included terms for investigator site, prior bisphosphonate use, visit and baseline. (NCT00557310)
Timeframe: Baseline, 24 months
| Intervention | % change of ratio (Least Squares Mean) |
|---|---|
| Teriparatide | 1.44 |
Finite Element Analysis of computed tomography (CT) data from hip is used to estimate the strength of the proximal femur with a virtual sideways fall. Least squares (LS) mean of the percent change from baseline to 18 months is from an analysis of variance (ANOVA). The model included terms for investigator site and prior bisphosphonate use. (NCT00557310)
Timeframe: Baseline, 18 months
| Intervention | % change of Newtons (Least Squares Mean) |
|---|---|
| Teriparatide | 2.54 |
Areal BMD is a measure of the amount of mineral in a given area of bone. Least squares (LS) mean of the percent change from baseline to 18 and 24 months is from an analysis of variance (ANOVA). The model included terms for investigator site and prior bisphosphonate use. (NCT00557310)
Timeframe: Baseline, 18, 24 months
| Intervention | % change of g/cm² (Least Squares Mean) | |
|---|---|---|
| 18 month percent change (n=28) | 24 month percent change (n=25) | |
| Teriparatide | -2.068 | -2.733 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of how easy it was to hold the pen while injecting. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strongly Disagree | 2 | 3 | 4 | 5 = Strongly Agree | |
| Forteo B Pen Users | 0 | 2 | 8 | 29 | 159 |
To assess subject preferences for assurance that drug is delivered for the Forteo 1.1 Pen or the Forteo B Pen through a questionnaire at Visit 2 completed by subjects who switch from the Forteo 1.1 Pen prior to the study entry to the Forteo B Pen during study participation. (NCT00577863)
Timeframe: 4 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strong Preference for Forteo 1.1 Pen | 2 | 3 = No Preference | 4 | 5 = Strong Preference for Forteo B Pen | |
| Forteo 1.1 Pen Users | 4 | 3 | 23 | 16 | 46 |
To assess subject preferences for attaching a new needle for the Forteo 1.1 Pen or the Forteo B Pen through a questionnaire at Visit 2 completed by subjects who switch from the Forteo 1.1 Pen prior to the study entry to the Forteo B Pen during study participation. (NCT00577863)
Timeframe: 4 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strong Preference for Forteo 1.1 Pen | 2 | 3 = No Preference | 4 | 5 = Strong Preference for Forteo B Pen | |
| Forteo 1.1 Pen Users | 2 | 0 | 36 | 8 | 46 |
To assess subject preferences for force on the plunger needed to inject a dose for the Forteo 1.1 Pen or the Forteo B Pen through a questionnaire at Visit 2 completed by subjects who switch from the Forteo 1.1 Pen prior to the study entry to the Forteo B Pen during study participation. (NCT00577863)
Timeframe: 4 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strong Preference for Forteo 1.1 Pen | 2 | 3 = No Preference | 4 | 5 = Strong Preference for Forteo B Pen | |
| Forteo 1.1 Pen Users | 2 | 3 | 14 | 11 | 62 |
To assess subject preferences for injecting a dose for the Forteo 1.1 Pen or the Forteo B Pen through a questionnaire at Visit 2 completed by subjects who switch from the Forteo 1.1 Pen prior to the study entry to the Forteo B Pen during study participation. (NCT00577863)
Timeframe: 4 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strong Preference for Forteo 1.1 Pen | 2 | 3 = No Preference | 4 | 5 = Strong Preference for Forteo B Pen | |
| Forteo 1.1 Pen Users | 2 | 1 | 16 | 6 | 67 |
To assess subject preferences for learning to use the pen for the Forteo 1.1 Pen or the Forteo B Pen through a questionnaire at Visit 2 completed by subjects who switch from the Forteo 1.1 Pen prior to the study entry to the Forteo B Pen during study participation. (NCT00577863)
Timeframe: 4 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strong Preference for Forteo 1.1 Pen | 2 | 3 = No Preference | 4 | 5 = Strong Preference for Forteo B Pen | |
| Forteo 1.1 Pen Users | 2 | 0 | 8 | 7 | 75 |
To assess subject preferences for overall ease of use for the Forteo 1.1 Pen or the Forteo B Pen through a questionnaire at Visit 2 completed by subjects who switch from the Forteo 1.1 Pen prior to the study entry to the Forteo B Pen during study participation. (NCT00577863)
Timeframe: 4 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strong Preference for Forteo 1.1 Pen | 2 | 3 = No Preference | 4 | 5 = Strong Preference for Forteo B Pen | |
| Forteo 1.1 Pen Users | 1 | 3 | 4 | 3 | 81 |
To assess overall subject preferences for the Forteo 1.1 Pen or the Forteo B Pen through a questionnaire at Visit 2 completed by subjects who switch from the Forteo 1.1 Pen prior to the study entry to the Forteo B Pen during study participation. (NCT00577863)
Timeframe: 4 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strong Preference for Forteo 1.1 Pen | 2 | 3 = No Preference | 4 | 5 = Strong Preference for Forteo B Pen | |
| Forteo 1.1 Pen Users | 2 | 1 | 4 | 6 | 79 |
To assess subject preferences for removing a used needle for the Forteo 1.1 Pen or the Forteo B Pen through a questionnaire at Visit 2 completed by subjects who switch from the Forteo 1.1 Pen prior to the study entry to the Forteo B Pen during study participation. (NCT00577863)
Timeframe: 4 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strong Preference for Forteo 1.1 Pen | 2 | 3 = No Preference | 4 | 5 = Strong Preference for Forteo B Pen | |
| Forteo 1.1 Pen Users | 3 | 1 | 36 | 7 | 45 |
To assess subject preferences for setting the dose for the Forteo 1.1 Pen or the Forteo B Pen through a questionnaire at Visit 2 completed by subjects who switch from the Forteo 1.1 Pen prior to the study entry to the Forteo B Pen during study participation. (NCT00577863)
Timeframe: 4 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strong Preference for Forteo 1.1 Pen | 2 | 3 = No Preference | 4 | 5 = Strong Preference for Forteo B Pen | |
| Forteo 1.1 Pen Users | 2 | 0 | 3 | 8 | 79 |
To assess subject preferences for use of the User Manual/Instructions for Use that came with the pen for the Forteo 1.1 Pen or the Forteo B Pen through a questionnaire at Visit 2 completed by subjects who switch from the Forteo 1.1 Pen prior to the study entry to the Forteo B Pen during study participation. (NCT00577863)
Timeframe: 4 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strong Preference for Forteo 1.1 Pen | 2 | 3 = No Preference | 4 | 5 = Strong Preference for Forteo B Pen | |
| Forteo 1.1 Pen Users | 3 | 2 | 15 | 9 | 63 |
Summary of number of complaints, and common complaints (at least 3% complaint rate), from subjects using Forteo B Pen. Functional Complaints were related to device malfunction; Nonfunctional were related to either cosmetic or perception concerns. (NCT00577863)
Timeframe: 46 weeks
| Intervention | number of complaints (Number) | ||||||
|---|---|---|---|---|---|---|---|
| All Complaints | Complaint Category: Functional | Functional (3%): Stopped working, wouldn't inject | Complaint Category: Nonfunctional | Nonfunctional (4%): Pen too large, awkward, bulky | Complaint Category: User Manual Related | User Manual (3.5%): No information on alcohol swab | |
| Forteo B Pen Users | 58 | 9 | 6 | 32 | 8 | 17 | 7 |
Number of subjects with complaints after 8 weeks, and common complaints (at least 3% complaint rate), using Forteo B Pen. Functional Complaints were related to device malfunction; Nonfunctional were related to either cosmetic or perception concerns. (NCT00577863)
Timeframe: 8 weeks
| Intervention | number of participants with complaints (Number) | |||||
|---|---|---|---|---|---|---|
| All Complaints | Complaint Category: Functional | Complaint Category: Nonfunctional | Nonfunctional (4%): Pen too large, awkward, bulky | Complaint Category: User Manual Related | User Manual (3.5%): No information on alcohol swab | |
| Forteo B Pen Users | 31 | 4 | 19 | 8 | 14 | 7 |
Number of subjects with complaints after 46 weeks, and common complaints (at least 3% complaint rate), using Forteo B Pen. Functional Complaints were related to device malfunction; Nonfunctional were related to either cosmetic or perception concerns. (NCT00577863)
Timeframe: 46 weeks
| Intervention | number of participants with complaints (Number) | ||||||
|---|---|---|---|---|---|---|---|
| All Complaints | Complaint Category: Functional | Functional (3%): Stopped working, wouldn't inject | Complaint Category: Nonfunctional | Nonfunctional (4%): Pen too large, awkward, bulky | Complaint Category: User Manual Related | User Manual (3.5%): No information on alcohol swab | |
| Forteo B Pen Users | 37 | 9 | 6 | 21 | 8 | 14 | 7 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of how easy it was to remove the pen from the package. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strongly Disagree | 2 | 3 | 4 | 5 = Strongly Agree | |
| Forteo B Pen Users | 0 | 0 | 5 | 19 | 174 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of how easy it was to remove the pen cap. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strongly Disagree | 2 | 3 | 4 | 5 = Strongly Agree | |
| Forteo B Pen Users | 0 | 0 | 1 | 15 | 182 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of how easy it was to remove a used needle. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strongly Disagree | 2 | 3 | 4 | 5 = Strongly Agree | |
| Forteo B Pen Users | 0 | 2 | 9 | 18 | 168 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of how easy it was to read the label. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strongly Disagree | 2 | 3 | 4 | 5 = Strongly Agree | |
| Forteo B Pen Users | 0 | 2 | 6 | 25 | 165 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of how easy it was to push the black injections button to administer the dose. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strongly Disagree | 2 | 3 | 4 | 5 = Strongly Agree | |
| Forteo B Pen Users | 0 | 0 | 4 | 19 | 175 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of how easy it was to learn to use the pen. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strongly Disagree | 2 | 3 | 4 | 5 = Strongly Agree | |
| Forteo B Pen Users | 1 | 1 | 0 | 16 | 180 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of how easy it was to attach a new needle. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strongly Disagree | 2 | 3 | 4 | 5 = Strongly Agree | |
| Forteo B Pen Users | 1 | 0 | 5 | 17 | 175 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of how convenient Forteo B Pen was to use. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strongly Disagree | 2 | 3 | 4 | 5 = Strongly Agree | |
| Forteo B Pen Users | 0 | 1 | 1 | 19 | 177 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of how easy it was to replace the pen cap. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strongly Disagree | 2 | 3 | 4 | 5 = Strongly Agree | |
| Forteo B Pen Users | 0 | 0 | 0 | 14 | 184 |
Summary of number of complaints, and common complaints (at least 3% complaint rate), from subjects using Forteo B Pen. Functional Complaints were related to device malfunction; Nonfunctional were related to either cosmetic or perception concerns. (NCT00577863)
Timeframe: 8 weeks
| Intervention | number of complaints (Number) | |||||
|---|---|---|---|---|---|---|
| All Complaints | Complaint Category: Functional | Complaint Category: Nonfunctional | Nonfunctional (4%): Pen too large, awkward, bulky | Complaint Category: User Manual Related | User Manual (3.5%): No information on alcohol swab | |
| Forteo B Pen Users | 47 | 4 | 27 | 8 | 16 | 7 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of how easy it was to set the dose. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strongly Disagree | 2 | 3 | 4 | 5 = Strongly Agree | |
| Forteo B Pen Users | 1 | 1 | 3 | 9 | 183 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of how easy it was to use the Forteo B Pen Instructions for Use. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strongly Disagree | 2 | 3 | 4 | 5 = Strongly Agree | |
| Forteo B Pen Users | 0 | 0 | 8 | 16 | 174 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of whether the Forteo B Pen helps them manage their osteoporosis when they are at home. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strongly Disagree | 2 | 3 | 4 | 5 = Strongly Agree | |
| Forteo B Pen Users | 0 | 1 | 3 | 15 | 179 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of whether the Forteo B Pen helps them manage their osteoporosis when they are away from home. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strongly Disagree | 2 | 3 | 4 | 5 = Strongly Agree | |
| Forteo B Pen Users | 2 | 5 | 19 | 26 | 142 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of how confident they were that they received the medication with the Forteo B Pen. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Not At All Confident | 2 | 3 | 4 | 5 = Very Confident | |
| Forteo B Pen Users | 2 | 4 | 10 | 32 | 149 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of the overall ease of use. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strongly Disagree | 2 | 3 | 4 | 5 = Strongly Agree | |
| Forteo B Pen Users | 0 | 0 | 1 | 18 | 179 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of whether the Forteo B Pen reduces their reluctance to take injections. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Strongly Disagree | 2 | 3 | 4 | 5 = Strongly Agree | |
| Forteo B Pen Users | 3 | 2 | 14 | 27 | 151 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject response on whether or not they sometimes reuse needles. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| No | Yes - Occasionally | Yes - Often | Yes - Rarely | |
| Forteo B Pen Users | 197 | 0 | 0 | 1 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of how satisfied they were with the Forteo B Pen. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| 1 = Very Dissatisfied | 2 | 3 | 4 | 5 = Very Satisfied | |
| Forteo B Pen Users | 0 | 0 | 4 | 18 | 176 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject perception of what could be done to improve the Forteo B Pen Instructions for Use. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Larger Print | More Color | Less Color | More Pictures | Less Pictures | More Detail in the Description | Less Detail in the Description | More Questions and Answers | No Improvements Needed | |
| Forteo B Pen Users | 22 | 5 | 1 | 7 | 3 | 10 | 1 | 11 | 156 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject response on when they attach a needle to their Forteo B Pen. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Immediately Before Each Injection | Several Hours Before Each Use | At Home If Injection Is Completed Away From Home | Other | |
| Forteo B Pen Users | 197 | 2 | 5 | 0 |
To assess overall subject perception of the device performance and acceptability through a questionnaire completed by all subjects at Visit 3. Subject response on when they remove the needle from their Forteo B Pen. (NCT00577863)
Timeframe: 8 weeks
| Intervention | participants (Number) | ||
|---|---|---|---|
| Immediately | When I Get Home If Injection Completed Away | Other | |
| Forteo B Pen Users | 197 | 0 | 1 |
Callus formation at the fracture site as defined by a CT scan to determine healing (early/beginning callus formation) or healed (complete callus formation) (NCT00594906)
Timeframe: Measured at 16 weeks
| Intervention | participants (Number) | ||
|---|---|---|---|
| Healed | Healing | Did not compelte CT scan | |
| Forteo Patients | 1 | 4 | 2 |
| Placebo Patients | 0 | 1 | 2 |
Areal BMD at the lumbar spine was measured by dual energy x-ray absorptiometry (DXA) at baseline and at 6, 12, 18, and 24 months, if possible. (NCT00697463)
Timeframe: Baseline, Month 18 or 24 reported
| Intervention | percentage of BMD change (Mean) |
|---|---|
| Women With Idiopathic Osteoporosis (IOP) | 10.8 |
1,25-D was measured at baseline, 4 and 8 hours after PTH infusion (NCT00754442)
Timeframe: baseline, 4 and 8 hours after start of infusion
| Intervention | pg/ml (Mean) | ||
|---|---|---|---|
| Baseline | 4 hours | 8 hours | |
| Controls | 46.2 | 58.8 | 105 |
| Group 1 | 40.6 | 39.8 | 56.4 |
CYP27B1 gene (the gene for 25-hydroxyvitamin D-1-alpha hydroxylase) was sequenced for all in patient group and compared with published control data (NCT00754442)
Timeframe: blood samples taken at baseline and sequenced over several days
| Intervention | participants (Number) |
|---|---|
| Patients | 0 |
Percent increase or decrease in lumbar spine bone mineral density between baseline and 6 months (treatment period) (NCT00759772)
Timeframe: Baseline and 6 months
| Intervention | percentage of change (Mean) |
|---|---|
| Teriparatide | 5.6 |
| Placebo | 0.2 |
Bone mineral density (gm/cm2) of the total hip region of interest on the left (NCT00826228)
Timeframe: Baseline to 6 months
| Intervention | % change in BMD (gm/cm2) from baseline (Mean) |
|---|---|
| PTH/Weight-Bearing | 0.02 |
amino-terminal propeptide of type I collagen (P1NP) (NCT00826228)
Timeframe: Baseline to 6 months
| Intervention | % change from baseline (Mean) |
|---|---|
| PTH/Weight-Bearing | 61.4 |
(NCT00853723)
Timeframe: Baseline, Day 15, Day 30, Day 60, Day 90
| Intervention | mg/dl (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Baseline | Day 15 | Day 30 | Day 60 | Day 90, time 0 | Day 90, time 3 hours | day 90, time 6 hours | |
| PTH 20 mcg/Day | 9.49 | 9.57 | 9.55 | 9.58 | 9.44 | 9.75 | 9.78 |
| PTHrP 400 mcg/Day | 9.48 | 9.95 | 9.73 | 9.71 | 9.56 | 9.90 | 9.90 |
| PTHrP 600 mcg/Day | 9.51 | 9.87 | 9.67 | 9.61 | 9.45 | 9.76 | 9.81 |
"Fractional tubular reabsorption of phosphate (TRP) = 1-{(U phos/P phos) x ( P creat/U creat)} if TRP < or = 0.86 then TMP/GFR = TRP x P phos if TRP > 0.86 then TMP/GFR = 0.3 x TRP/{1-(0.8 x TRP)} x P phos~U= urine, P = plasma" (NCT00853723)
Timeframe: Baseline, Day 15, Day 30, Day 60, Day 90
| Intervention | mg/dl (Mean) | ||||
|---|---|---|---|---|---|
| Baseline | Day 15 | Day 30 | Day 60 | Day 90 | |
| PTH 20 mcg/Day | 3.96 | 4.18 | 4.03 | 4.28 | 4.00 |
| PTHrP 400 mcg/Day | 3.80 | 3.78 | 3.88 | 4.02 | 4.11 |
| PTHrP 600 mcg/Day | 3.71 | 3.47 | 3.61 | 3.84 | 3.90 |
(NCT00853723)
Timeframe: 90 days
| Intervention | mg/gm creatinine (Mean) | |
|---|---|---|
| Baseline | Day 90 | |
| PTH 20 mcg/Day | 209.99 | 232.48 |
| PTHrP 400 mcg/Day | 206.37 | 260.46 |
| PTHrP 600 mcg/Day | 213.07 | 235.25 |
(NCT00853723)
Timeframe: Baseline, Day 15, Day 30, Day 60, Day 90
| Intervention | mg/dl (Mean) | ||||
|---|---|---|---|---|---|
| Baseline | Day 15 | Day 30 | Day 60 | Day 90 | |
| PTH 20 mcg/Day | 4.09 | 4.13 | 4.19 | 4.28 | 4.10 |
| PTHrP 400 mcg/Day | 4.0 | 3.78 | 3.87 | 4.02 | 4.05 |
| PTHrP 600 mcg/Day | 3.93 | 3.68 | 3.71 | 3.97 | 3.98 |
(Serum Creatinine X Urine Calcium)/(Serum Calcium X Urine Creatinine) (NCT00853723)
Timeframe: Baseline, Day 15, Day 30, Day 60, Day 90
| Intervention | % excreted (Mean) | ||||
|---|---|---|---|---|---|
| Baseline | Day 15 | Day 30 | Day 60 | Day 90 | |
| PTH 20 mcg/Day | 2.30 | 2.55 | 2.92 | 2.95 | 3.37 |
| PTHrP 400 mcg/Day | 2.38 | 3.42 | 3.27 | 3.38 | 3.10 |
| PTHrP 600 mcg/Day | 2.71 | 4.18 | 3.74 | 2.89 | 2.89 |
(NCT00853723)
Timeframe: Baseline, Day 15, Day 30, Day 60, Day 90
| Intervention | percentage change from baseline (Mean) | |||
|---|---|---|---|---|
| Day 15 | Day 30 | Day 60 | Day 90 | |
| PTH 20 mcg/Day | 60.67 | 97.27 | 125.46 | 171.49 |
| PTHrP 400 mcg/Day | 32.54 | 48.89 | 34.71 | 46.07 |
| PTHrP 600 mcg/Day | 23.51 | 83.14 | 87.39 | 84.09 |
(NCT00853723)
Timeframe: 90 days
| Intervention | Percent change from baseline (Mean) |
|---|---|
| PTHrP 400 mcg/Day | 1.89 |
| PTHrP 600 mcg/Day | 1.52 |
| PTH 20 mcg/Day | 2.17 |
(NCT00853723)
Timeframe: 90 days
| Intervention | Percent change from baseline (Mean) |
|---|---|
| PTHrP 400 mcg/Day | -0.48 |
| PTHrP 600 mcg/Day | -0.99 |
| PTH 20 mcg/Day | -0.97 |
(NCT00853723)
Timeframe: 90 days
| Intervention | Percent change from baseline (Mean) |
|---|---|
| PTHrP 400 mcg/Day | 0.91 |
| PTHrP 600 mcg/Day | 0.54 |
| PTH 20 mcg/Day | 0.61 |
(NCT00853723)
Timeframe: 90 days
| Intervention | Percent change from baseline (Mean) |
|---|---|
| PTHrP 400 mcg/Day | -0.35 |
| PTHrP 600 mcg/Day | -0.34 |
| PTH 20 mcg/Day | -0.82 |
(NCT00853723)
Timeframe: 90 days
| Intervention | Percent change from baseline (Mean) |
|---|---|
| PTHrP 400 mcg/Day | 0.68 |
| PTHrP 600 mcg/Day | 0.72 |
| PTH 20 mcg/Day | 0.54 |
(NCT00853723)
Timeframe: Baseline, Day 15, Day 30, Day 60, Day 90
| Intervention | pg/ml (Mean) | ||||
|---|---|---|---|---|---|
| Baseline | Day 15 | Day 30 | Day 60 | Day 90 | |
| PTH 20 mcg/Day | 42.51 | 65.25 | 67.29 | 58.15 | 53.73 |
| PTHrP 400 mcg/Day | 49.06 | 84.92 | 76.04 | 67.85 | 64.36 |
| PTHrP 600 mcg/Day | 42.49 | 63.07 | 65.15 | 57.02 | 55.08 |
(NCT00853723)
Timeframe: Baseline, Day 15, Day 30, Day 60, Day 90
| Intervention | percentage change from baseline (Mean) | |||
|---|---|---|---|---|
| Day 15 | Day 30 | Day 60 | Day 90 | |
| PTH 20 mcg/Day | 4.87 | 13.89 | 52.98 | 92.46 |
| PTHrP 400 mcg/Day | -12.40 | 1.60 | 4.13 | 32.65 |
| PTHrP 600 mcg/Day | 10.25 | 9.59 | 14.38 | 25.65 |
Visual analog pain scale is a measurement instrument to measure the level of hip pain. Scores range from 0 to 100 millimeter (mm) with higher score indicating greater pain. Least squares (LS) means obtained from mixed model repeated measures analysis including as fixed effects treatment and time with interaction, further adjusted for type of fracture (31-A1/31-A2), type of reduction (open/close), use of opioids (Yes/No), use of non-steroidal anti-inflammatory drugs, adequate reduction (Yes/No) and interaction between treatment and adequate reduction. (NCT00887354)
Timeframe: 6, 12, 18, and 26 Weeks
| Intervention | millimeter (mm) (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 6 | Week 12 | Week 18 | Week 26 | |
| Risedronate | 23.54 | 19.24 | 18.19 | 13.74 |
| Teriparatide | 16.44 | 9.28 | 6.90 | 4.48 |
Self-reported hip pain scale in which 0=no pain; 1=pain is slight or intermittent, pain on starting to walk but getting less with normal activity; 2=pain occurs only after some activity, disappears quickly with rest; 3=pain is tolerable, permitting limited activity; 4=pain is severe on attempting to walk, prevents all activity; 5=pain is severe and spontaneous. (NCT00887354)
Timeframe: Baseline
| Intervention | percentage of participants (Number) | |||||
|---|---|---|---|---|---|---|
| 0-No pain | 1- Pain slight or intermittent | 2- Pain occurs only after some activity | 3- Pain is tolerable | 4- Pain severe on attempting to walk | 5- Pain severe and spontaneous | |
| Risedronate | 8.2 | 12.9 | 20.0 | 38.8 | 15.3 | 4.7 |
| Teriparatide | 9.4 | 4.7 | 23.5 | 36.5 | 20.0 | 5.9 |
Least squares (LS) means obtained from mixed model repeated measures analysis including as fixed effects treatment and time with interaction, further adjusted for baseline lumbar spine BMD, type of hip fracture (31-A1/31-A2) and glucocorticoids used at baseline (Yes/No). (NCT00887354)
Timeframe: Baseline, Week 26; Baseline, Week 52
| Intervention | g/cm^2 (Least Squares Mean) | |
|---|---|---|
| Week 26 | Week 52 | |
| Risedronate | 0.032 | 0.044 |
| Teriparatide | 0.053 | 0.078 |
"Femoral neck BMD: Least squares (LS) means obtained from mixed model repeated measures analysis including as fixed effects treatment and time with interaction, further adjusted for baseline femoral neck BMD and type of hip fracture (31-A1/31-A2) .~Total hip BMD: Least squares (LS) means obtained from mixed model repeated measures analysis including as fixed effects treatment and time with interaction, further adjusted for baseline total hip BMD, type of hip fracture (31-A1/31-A2) and duration of prior bisphosphonate use." (NCT00887354)
Timeframe: Baseline, Week 26; Baseline, Week 52; Baseline, Week 78
| Intervention | g/cm^2 (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Total Hip 26 Weeks | Total Hip 52 Weeks | Total Hip 78 Weeks | Femoral Neck 26 Weeks | Femoral Neck 52 Weeks | Femoral Neck 78 Weeks | |
| Risedronate | -0.001 | -0.001 | 0.005 | -0.009 | -0.006 | -0.007 |
| Teriparatide | -0.001 | 0.001 | 0.007 | 0.002 | -0.000 | 0.012 |
SF-36 is a self-reported questionnaire consisting of 36 questions covering 8 health domains. Each domain was scored by summing the individual items and transforming the scores into a 0 to 100 scale, with higher scores indicating better health status or functioning. The physical component summary (PCS) has been constructed based on the 8 SF-36 domains and consist of the physical functioning, bodily pain, role-physical, and general health scales (range = 0 to 100, with higher scores indicating better health status for functioning). Least squares (LS) means obtained from mixed model repeated measures analysis including as fixed effects treatment and time with interaction, further adjusted for type of hip fracture (31-A1/31-A2) and adequate reduction (Yes/No). (NCT00887354)
Timeframe: Baseline, Week 6; Baseline, Week 12; Baseline, Week 18; Baseline, Week 26
| Intervention | units on a scale (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 6 | Week 12 | Week 18 | Week 26 | |
| Risedronate | 5.10 | 11.09 | 12.81 | 14.36 |
| Teriparatide | 7.37 | 11.32 | 14.37 | 16.34 |
"Timed Up and Go test measures, in seconds, the time taken by an individual to stand up from a standard chair, walk a distance of 3 meters, turn, walk back to the chair, and sit down. Least squares (LS) means obtained from mixed model repeated measures analysis including as fixed effects treatment and time with interaction, further adjusted for age, type of fracture (31-A1/31-A2), type of reduction (open/close), type of walking aid, baseline SF-36 PCS and baseline Charnley's pain score." (NCT00887354)
Timeframe: 6, 12, 18, and 26 Weeks
| Intervention | seconds (sec) (Least Squares Mean) | |||
|---|---|---|---|---|
| Week 6 | Week 12 | Week 18 | Week 26 | |
| Risedronate | 32.38 | 24.48 | 21.14 | 19.91 |
| Teriparatide | 26.45 | 20.13 | 17.75 | 16.69 |
Least squares (LS) means obtained from mixed model repeated measures analysis including as fixed effects treatment and time with interaction, further adjusted for baseline lumbar spine BMD, type of hip fracture (31-A1/31-A2) and glucocorticoids used at baseline (Yes/No). (NCT00887354)
Timeframe: Baseline, Week 78
| Intervention | gram per square centimeter (g/cm^2) (Least Squares Mean) |
|---|---|
| Teriparatide | 0.094 |
| Risedronate | 0.055 |
"Bone mineral density was measured using dual energy x-ray absorptiometry (DXA). Images were analyzed by a central imaging reader.~Percent change from baseline to month 6 was analyzed using a linear mixed effects model with the percent change from baseline to month 6 in DXA BMD as dependent variable, and baseline BMD value, machine type, geographic region, interaction of baseline BMD and machine type, visit, treatment (categorical) and interaction of treatment and visit as the independent variables." (NCT00896532)
Timeframe: Baseline to 6 months
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Placebo | -0.4 |
| Alendronate | 0.5 |
| Teriparatide | 0.5 |
| Romosozumab 70 mg QM | 0.2 |
| Romosozumab 140 mg Q3M | 0.4 |
| Romosozumab 140 mg QM | 2.1 |
| Romosozumab 210 mg Q3M | 0.9 |
| Romosozumab 210 mg QM | 1.9 |
"Bone mineral density was measured using dual energy x-ray absorptiometry (DXA). Images were analyzed by a central imaging reader.~Percent change from baseline to month 6 was analyzed using a linear mixed effects model with the percent change from baseline to month 6 in DXA BMD as dependent variable, and baseline BMD value, machine type, geographic region, interaction of baseline BMD and machine type, visit, treatment (categorical) and interaction of treatment and visit as the independent variables." (NCT00896532)
Timeframe: Baseline to 6 months
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Placebo | 0.3 |
| Alendronate | 2.6 |
| Teriparatide | 4.8 |
| Romosozumab 70 mg QM | 4.1 |
| Romosozumab 140 mg Q3M | 4.2 |
| Romosozumab 140 mg QM | 7.1 |
| Romosozumab 210 mg Q3M | 4.4 |
| Romosozumab 210 mg QM | 8.2 |
"Bone mineral density was measured using dual energy x-ray absorptiometry (DXA). Images were analyzed by a central imaging reader.~Percent change from baseline to 12 months in BMD was analyzed using a linear mixed effects model with the percent change from baseline to month 12 in DXA BMD as dependent variable, and baseline BMD value, machine type, geographic region, interaction of baseline BMD and machine type, visit, treatment (categorical) and interaction of treatment and visit as the independent variables." (NCT00896532)
Timeframe: Baseline to 12 months
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Placebo | -0.7 |
| Alendronate | 1.9 |
| Teriparatide | 1.3 |
| Romosozumab 70 mg QM | 1.3 |
| Romosozumab 140 mg Q3M | 1.3 |
| Romosozumab 140 mg QM | 3.4 |
| Romosozumab 210 mg Q3M | 1.9 |
| Romosozumab 210 mg QM | 4.1 |
"Bone mineral density was measured using dual energy x-ray absorptiometry (DXA). Images were analyzed by a central imaging reader.~Percent change from baseline to 12 months in BMD was analyzed using a linear mixed effects model with the percent change from baseline to month 12 in DXA BMD as dependent variable, and baseline BMD value, machine type, geographic region, interaction of baseline BMD and machine type, visit, treatment (categorical) and interaction of treatment and visit as the independent variables." (NCT00896532)
Timeframe: Baseline to 12 months
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Placebo | -1.1 |
| Alendronate | 1.2 |
| Teriparatide | 1.1 |
| Romosozumab 70 mg QM | 0.6 |
| Romosozumab 140 mg Q3M | 1.8 |
| Romosozumab 140 mg QM | 4.2 |
| Romosozumab 210 mg Q3M | 1.4 |
| Romosozumab 210 mg QM | 3.7 |
"Bone mineral density was measured using dual energy x-ray absorptiometry (DXA). Images were analyzed by a central imaging reader.~Percent change from baseline in distal radius BMD was analyzed using an analysis of covariance (ANCOVA) model with the percent change from baseline to Month 12 in DXA BMD as dependent variable, baseline BMD value, machine type, interaction of baseline BMD and machine type, treatment (categorical) and geographic region as the independent class variables." (NCT00896532)
Timeframe: Baseline to 12 months
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Placebo | -0.9 |
| Alendronate | -0.3 |
| Teriparatide | -1.7 |
| Romosozumab 70 mg QM | -1.8 |
| Romosozumab 140 mg Q3M | -1.1 |
| Romosozumab 140 mg QM | -1.0 |
| Romosozumab 210 mg Q3M | -0.4 |
| Romosozumab 210 mg QM | -1.2 |
Bone mineral density was measured using dual energy x-ray absorptiometry (DXA). Images were analyzed by a central imaging reader. (NCT00896532)
Timeframe: Baseline to 12 months
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Placebo | -0.1 |
| Alendronate | 4.1 |
| Teriparatide | 7.1 |
| Romosozumab 70 mg QM | 5.4 |
| Romosozumab 140 mg Q3M | 5.4 |
| Romosozumab 140 mg QM | 9.1 |
| Romosozumab 210 mg Q3M | 5.5 |
| Romosozumab 210 mg QM | 11.3 |
| Romosozumab Monthly | 8.6 |
| Romosozumab Every 3 Months | 5.5 |
| Romosozumab 140 mg | 7.3 |
| Romosozumab 210 mg | 8.4 |
Percent change from baseline in the bone turnover marker (BTM) P1NP was analyzed using a linear mixed effects model with the natural logarithm of the ratio of BTM (follow-up versus baseline) as the dependent variables, and visit, treatment (categorical), interaction of treatment and visit and the natural logarithm of the baseline BTM as the independent variables; outcomes were then transformed back to percent change from baseline. (NCT00896532)
Timeframe: Baseline and months 1, 3, 6, 9, and 12
| Intervention | percent change (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Month 1 | Month 3 | Month 6 | Month 9 | Month 12 | |
| Placebo | -0.7 | -5.4 | -5.9 | -10.6 | -8.7 |
| Romosozumab 140 mg Q3M | 61.4 | -15.5 | -22.8 | -23.8 | -23.3 |
| Romosozumab 140 mg QM | 55.0 | 3.8 | -18.6 | -26.1 | -31.2 |
| Romosozumab 210 mg Q3M | 75.8 | -19.5 | -25.5 | -30.1 | -29.7 |
| Romosozumab 210 mg QM | 92.2 | 25.6 | 6.9 | -5.8 | -17.2 |
| Romosozumab 70 mg QM | 24.2 | -9.1 | -20.0 | -26.9 | -23.0 |
"Bone mineral density was measured using dual energy x-ray absorptiometry (DXA). Images were analyzed by a central imaging reader.~Percent change from baseline to month 6 was analyzed using a linear mixed effects model with the percent change from baseline to month 6 in DXA BMD as dependent variable, and baseline BMD value, machine type, geographic region, interaction of baseline BMD and machine type, visit, treatment (categorical) and interaction of treatment and visit as the independent variables." (NCT00896532)
Timeframe: Baseline to 6 months
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Placebo | -0.6 |
| Alendronate | 0.9 |
| Teriparatide | 0.5 |
| Romosozumab 70 mg QM | 0.5 |
| Romosozumab 140 mg Q3M | 0.9 |
| Romosozumab 140 mg QM | 2.2 |
| Romosozumab 210 mg Q3M | 1.1 |
| Romosozumab 210 mg QM | 2.9 |
Percent change from baseline in the bone turnover marker (BTM) P1NP was analyzed using a linear mixed effects model with the natural logarithm of the ratio of BTM (follow-up versus baseline) as the dependent variables, and visit, treatment (categorical), interaction of treatment and visit and the natural logarithm of the baseline BTM as the independent variables; outcomes were then transformed back to percent change from baseline. (NCT00896532)
Timeframe: Baseline and months 1, 3, 6, 9, and 12
| Intervention | percent change (Least Squares Mean) | |||
|---|---|---|---|---|
| Month 3 | Month 6 | Month 9 | Month 12 | |
| Alendronate | -50.8 | -57.0 | -60.8 | -60.8 |
| Teriparatide | 97.1 | 138.0 | 116.8 | 98.3 |
Percent change from baseline in the bone turnover marker (BTM) osteocalcin was analyzed using a linear mixed effects model with the natural logarithm of the ratio of BTM (follow-up versus baseline) as the dependent variables, and visit, treatment (categorical), interaction of treatment and visit and the natural logarithm of the baseline BTM as the independent variables; outcomes were then transformed back to percent change from baseline. (NCT00896532)
Timeframe: Baseline and months 1, 3, 6, 9, and 12
| Intervention | percent change (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Month 1 | Month 3 | Month 6 | Month 9 | Month 12 | |
| Placebo | -1.6 | 4.1 | -7.1 | -6.0 | -14.1 |
| Romosozumab 140 mg Q3M | 60.1 | -5.6 | -16.5 | -29.0 | -24.7 |
| Romosozumab 140 mg QM | 53.1 | 15.6 | -7.4 | -27.7 | -31.1 |
| Romosozumab 210 mg Q3M | 77.9 | -3.7 | -23.2 | -30.7 | -26.2 |
| Romosozumab 210 mg QM | 78.6 | 41.6 | 10.0 | -4.0 | -12.5 |
| Romosozumab 70 mg QM | 28.1 | -0.3 | -11.8 | -26.9 | -27.3 |
Percent change from baseline in the bone turnover marker (BTM) CTX was analyzed using a linear mixed effects model with the natural logarithm of the ratio of BTM (follow-up versus baseline) as the dependent variables, and visit, treatment (categorical), interaction of treatment and visit and the natural logarithm of the baseline BTM as the independent variables; outcomes were then transformed back to percent change from baseline. (NCT00896532)
Timeframe: Baseline and months 1, 3, 6, 9, and 12
| Intervention | percent change (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Month 1 | Month 3 | Month 6 | Month 9 | Month 12 | |
| Romosozumab 140 mg Q3M | -19.2 | -6.2 | -8.4 | 1.3 | 12.2 |
| Romosozumab 140 mg QM | -35.4 | -26.5 | -24.6 | -27.7 | -33.0 |
| Romosozumab 210 mg Q3M | -33.0 | -12.6 | -10.5 | -11.7 | -6.6 |
| Romosozumab 210 mg QM | -28.5 | -3.7 | -8.7 | -17.2 | -22.5 |
| Romosozumab 70 mg QM | -22.1 | -21.5 | -18.1 | -15.1 | -20.3 |
| Placebo | -3.9 | -2.4 | 2.7 | 1.0 | 9.8 |
Percent change from baseline in the bone turnover marker (BTM) CTX was analyzed using a linear mixed effects model with the natural logarithm of the ratio of BTM (follow-up versus baseline) as the dependent variables, and visit, treatment (categorical), interaction of treatment and visit and the natural logarithm of the baseline BTM as the independent variables; outcomes were then transformed back to percent change from baseline. (NCT00896532)
Timeframe: Baseline and months 1, 3, 6, 9, and 12
| Intervention | percent change (Least Squares Mean) | |||
|---|---|---|---|---|
| Month 3 | Month 6 | Month 9 | Month 12 | |
| Alendronate | -65.0 | -64.2 | -64.4 | -66.7 |
| Teriparatide | 69.4 | 93.5 | 81.3 | 77.0 |
Percent change from baseline in the bone turnover marker (BTM) osteocalcin was analyzed using a linear mixed effects model with the natural logarithm of the ratio of BTM (follow-up versus baseline) as the dependent variables, and visit, treatment (categorical), interaction of treatment and visit and the natural logarithm of the baseline BTM as the independent variables; outcomes were then transformed back to percent change from baseline. (NCT00896532)
Timeframe: Baseline and months 1, 3, 6, 9, and 12
| Intervention | percent change (Least Squares Mean) | |||
|---|---|---|---|---|
| Month 3 | Month 6 | Month 9 | Month 12 | |
| Alendronate | -28.7 | -40.6 | -50.9 | -50.3 |
| Teriparatide | 104.7 | 106.7 | 99.9 | 91.6 |
Percent change from baseline in the bone turnover marker (BTM) BSAP was analyzed using a linear mixed effects model with the natural logarithm of the ratio of BTM (follow-up versus baseline) as the dependent variables, and visit, treatment (categorical), interaction of treatment and visit and the natural logarithm of the baseline BTM as the independent variables; outcomes were then transformed back to percent change from baseline. (NCT00896532)
Timeframe: Baseline and months 1, 3, 6, 9, and 12
| Intervention | percent change (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Month 1 | Month 3 | Month 6 | Month 9 | Month 12 | |
| Placebo | -1.1 | -7.6 | -4.1 | 3.5 | 9.2 |
| Romosozumab 140 mg Q3M | 35.1 | -18.0 | -18.2 | -12.5 | -10.8 |
| Romosozumab 140 mg QM | 29.3 | 1.3 | -6.6 | -5.5 | -5.0 |
| Romosozumab 210 mg Q3M | 47.5 | -17.3 | -20.0 | -17.7 | -12.4 |
| Romosozumab 210 mg QM | 60.9 | 27.4 | 13.1 | 10.4 | 9.2 |
| Romosozumab 70 mg QM | 11.7 | -8.5 | -8.7 | -4.9 | -2.6 |
Percent change from baseline in the bone turnover marker (BTM) BSAP was analyzed using a linear mixed effects model with the natural logarithm of the ratio of BTM (follow-up versus baseline) as the dependent variables, and visit, treatment (categorical), interaction of treatment and visit and the natural logarithm of the baseline BTM as the independent variables; outcomes were then transformed back to percent change from baseline. (NCT00896532)
Timeframe: Baseline and months 1, 3, 6, 9, and 12
| Intervention | percent change (Least Squares Mean) | |||
|---|---|---|---|---|
| Month 3 | Month 6 | Month 9 | Month 12 | |
| Alendronate | -30.5 | -35.4 | -32.5 | -31.2 |
| Teriparatide | 21.8 | 29.8 | 41.8 | 45.7 |
(NCT00926380)
Timeframe: Baseline and 2 years
| Intervention | percent change (Mean) |
|---|---|
| Denosumab ONLY | 8.3 |
| Teriparatide (Forteo®) ONLY | 9.5 |
| Denosumab and Teriparatide (Forteo®) | 12.9 |
Eroded surface/bone surface (ES/BS) in the endocortical compartment is the fraction of the entire trabecular surface occupied by resorption bays, including both those with and without osteoclasts. It is an indicator of bone resorption. (NCT00927186)
Timeframe: 6 and 24 months
| Intervention | percentage of surface (Median) | |
|---|---|---|
| 6 months (n=23, 29) | 24 months (n=9, 8) | |
| Teriparatide | 4.06 | 3.43 |
| Zoledronic Acid | 1.87 | 1.88 |
Osteoid surface (OS) in the endocortical compartment is the fraction (%) of the entire trabecular bone surface that is covered by osteoid. (NCT00927186)
Timeframe: 6 and 24 months
| Intervention | percentage of surface (Median) | |
|---|---|---|
| 6 months (n=23, 29) | 24 months (n=9, 8) | |
| Teriparatide | 16.33 | 7.48 |
| Zoledronic Acid | 1.87 | 1.55 |
Tt.FP in CC is a measure of bone formation and is calculated as wall thickness divided by Aj.AR. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 24 months
| Intervention | year (Median) | |
|---|---|---|
| DL and NL (n=9, 2) | DL, Imputed SL (ISL) and NL (n=10, 5) | |
| Teriparatide | 0.60 | 0.68 |
| Zoledronic Acid | 0.51 | 2.62 |
Tt.FP in EC is a measure of bone formation and is calculated as wall thickness divided by Aj.AR. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 6 and 24 months
| Intervention | year (Median) | |||
|---|---|---|---|---|
| DL and NL at 6 Months (n=23, 6) | DL, Imputed SL (ISL) and NL at 6 Months (n=23, 15) | DL and NL at 24 Months (n=8, 2) | DL, ISL and NL at 24 Months (n=9, 3) | |
| Teriparatide | 0.24 | 0.24 | 0.27 | 0.31 |
| Zoledronic Acid | 0.43 | 0.54 | 0.62 | 0.86 |
Wall thickness (WTh.) in the endocortical compartment is measured as the mean distance from the cement line to the marrow space of completed trabecular bone packets. (NCT00927186)
Timeframe: 6 and 24 months
| Intervention | micrometer (µm) (Median) | |
|---|---|---|
| 6 months (n=23, 29) | 24 months (n=9, 8) | |
| Teriparatide | 36.30 | 34.00 |
| Zoledronic Acid | 32.39 | 32.45 |
Tt.FP in CC is a measure of bone formation and is calculated as wall thickness divided by Aj.AR. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 6 months
| Intervention | year (Median) | |
|---|---|---|
| DL and NL (n=28, 16) | DL, ISL and NL (n=28, 18) | |
| Teriparatide | 0.24 | 0.24 |
| Zoledronic Acid | 1.46 | 1.46 |
The length of tetracycline double labels is a measure of the extent of bone formation in the cancellous compartment within individual remodeling units and is measured in millimeters (mm). Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. (NCT00927186)
Timeframe: 24 months
| Intervention | millimeter (mm) (Median) |
|---|---|
| Teriparatide | 0.23 |
| Zoledronic Acid | 0.29 |
The length of tetracycline double labels is a measure of the extent of bone formation in the cancellous compartment within individual remodeling units and is measured in millimeters (mm). Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. (NCT00927186)
Timeframe: 6 months
| Intervention | millimeter (mm) (Median) |
|---|---|
| Teriparatide | 0.35 |
| Zoledronic Acid | 0.24 |
CTX is a measure of bone resorption. (NCT00927186)
Timeframe: Baseline, 12 months
| Intervention | nanogram/milliliter (ng/mL) (Median) |
|---|---|
| Teriparatide | 0.42 |
| Zoledronic Acid | -0.23 |
OC is a measure of osteoblast function. (NCT00927186)
Timeframe: Baseline, 12 months
| Intervention | microgram/liter (µg/L) (Median) |
|---|---|
| Teriparatide | 32.98 |
| Zoledronic Acid | -12.32 |
PINP is a measure of bone formation. (NCT00927186)
Timeframe: Baseline, 12 months
| Intervention | microgram/liter (µg/L) (Median) |
|---|---|
| Teriparatide | 93.50 |
| Zoledronic Acid | -33.00 |
MS/BS in CC is a measure of the proportion of BS on which new mineralized bone is deposited at the time of tetracycline (T) labeling and is calculated as sum of total extent of double label (DL) plus half the extent of single label (SL) divided by BS. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in the biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under a microscope. DL indicates active bone formation, SL or no label (NL) suggests suppression of bone formation. (NCT00927186)
Timeframe: 24 months
| Intervention | percentage of surface (Median) |
|---|---|
| Teriparatide | 3.00 |
| Zoledronic Acid | 0.07 |
MS/BS in CC is a measure of the proportion of BS on which new mineralized bone is deposited at the time of tetracycline (T) labeling and is calculated as sum of total extent of double label (DL) plus half the extent of single label (SL) divided by BS. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in the biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under a microscope. DL indicates active bone formation, SL or no label (NL) suggests suppression of bone formation. (NCT00927186)
Timeframe: 6 months
| Intervention | percentage of surface (Median) |
|---|---|
| Teriparatide | 5.60 |
| Zoledronic Acid | 0.16 |
Osteoid thickness (OTh.) in the cancellous compartment is a measure of the average thickness of osteoid seams. (NCT00927186)
Timeframe: 24 months
| Intervention | micrometer (µm) (Median) |
|---|---|
| Teriparatide | 5.71 |
| Zoledronic Acid | 3.98 |
Osteoid thickness (OTh.) in the cancellous compartment is a measure of the average thickness of osteoid seams. (NCT00927186)
Timeframe: 6 months
| Intervention | micrometer (µm) (Median) |
|---|---|
| Teriparatide | 4.92 |
| Zoledronic Acid | 3.77 |
Eroded surface/bone surface (ES/BS) in the cancellous compartment is the fraction of the entire trabecular surface occupied by resorption bays, including both those with and without osteoclasts. It is an indicator of bone resorption. (NCT00927186)
Timeframe: 24 months
| Intervention | percentage of surface (Median) |
|---|---|
| Teriparatide | 4.44 |
| Zoledronic Acid | 2.39 |
Eroded surface/bone surface (ES/BS) in the cancellous compartment is the fraction of the entire trabecular surface occupied by resorption bays, including both those with and without osteoclasts. It is an indicator of bone resorption. (NCT00927186)
Timeframe: 6 months
| Intervention | percentage of surface (Median) |
|---|---|
| Teriparatide | 4.59 |
| Zoledronic Acid | 2.71 |
Osteoid surface (OS) in the cancellous compartment is the fraction (%) of the entire trabecular bone surface that is covered by osteoid. (NCT00927186)
Timeframe: 24 months
| Intervention | percentage of surface (Median) |
|---|---|
| Teriparatide | 11.19 |
| Zoledronic Acid | 1.26 |
Osteoid surface (OS) in the cancellous compartment is the fraction (%) of the entire trabecular bone surface that is covered by osteoid. (NCT00927186)
Timeframe: 6 months
| Intervention | percentage of surface (Median) |
|---|---|
| Teriparatide | 11.34 |
| Zoledronic Acid | 2.51 |
Osteoid volume (OV) in the cancellous compartment is the percent of a given volume of bone tissue that consists of unmineralized bone (osteoid). (NCT00927186)
Timeframe: 24 months
| Intervention | percentage of volume (Median) |
|---|---|
| Teriparatide | 1.33 |
| Zoledronic Acid | 0.18 |
Osteoid volume (OV) in the cancellous compartment is the percent of a given volume of bone tissue that consists of unmineralized bone (osteoid). (NCT00927186)
Timeframe: 6 months
| Intervention | percentage of volume (Median) |
|---|---|
| Teriparatide | 1.32 |
| Zoledronic Acid | 0.24 |
Wall thickness (WTh.) in the cancellous compartment is measured as the mean distance from the cement line to the marrow space of completed trabecular bone packets. (NCT00927186)
Timeframe: 24 months
| Intervention | micrometer (µm) (Median) |
|---|---|
| Teriparatide | 31.37 |
| Zoledronic Acid | 29.26 |
Wall thickness (WTh.) in the cancellous compartment is measured as the mean distance from the cement line to the marrow space of completed trabecular bone packets. (NCT00927186)
Timeframe: 6 months
| Intervention | µm (Median) |
|---|---|
| Teriparatide | 31.29 |
| Zoledronic Acid | 28.63 |
Ac.f in CC represents the frequency of activation of new remodeling cycles on the bone surface (BFR/BS divided by wall thickness) and is expressed in units of new cycles per unit of time. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 24 months
| Intervention | new cycles/year (Median) | |
|---|---|---|
| DL and NL (n=9, 6) | DL, Imputed SL (ISL) and NL (n=10, 9) | |
| Teriparatide | 0.19 | 0.18 |
| Zoledronic Acid | 0.00 | 0.00 |
Ac.f in CC represents the frequency of activation of new remodeling cycles on BS (bone formation rate [BFR]/BS divided by wall thickness) and is expressed in units of new cycles per unit of time. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 micrometer (µm)/day or counted as missing. (NCT00927186)
Timeframe: 6 months
| Intervention | new cycles/year (Median) | |
|---|---|---|
| DL and NL (n=28, 28) | DL, Imputed SL (ISL) and NL (n=28, 30) | |
| Teriparatide | 0.37 | 0.37 |
| Zoledronic Acid | 0.01 | 0.01 |
Ac.f in EC represents the frequency of activation of new remodeling cycles on the bone surface (BFR/BS divided by wall thickness) and is expressed in units of new cycles per unit of time. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 6 and 24 months
| Intervention | new cycles/year (Median) | |||
|---|---|---|---|---|
| DL and NL at 6 Months (n=23, 20) | DL, Imputed SL (ISL) and NL at 6 Months (n=23, 29) | DL and NL at 24 Months (n=8, 7) | DL, ISL and NL at 24 Months (n=9, 8) | |
| Teriparatide | 0.83 | 0.83 | 0.25 | 0.24 |
| Zoledronic Acid | 0.00 | 0.01 | 0.00 | 0.00 |
a. FP in CC is the mean time required to rebuild a new bone structural unit, calculated as wall thickness divided by MAR. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 24 months
| Intervention | year (Median) | |
|---|---|---|
| DL and NL (n=9, 2) | DL, Imputed SL (ISL) and NL (n=10, 5) | |
| Teriparatide | 0.19 | 0.19 |
| Zoledronic Acid | 0.19 | 0.25 |
a. FP in CC is the mean time required to rebuild a new bone structural unit, calculated as wall thickness divided by MAR. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 6 months
| Intervention | year (Median) | |
|---|---|---|
| DL and NL (n=28, 16) | DL, ISL and NL (n=28, 18) | |
| Teriparatide | 0.15 | 0.15 |
| Zoledronic Acid | 0.16 | 0.16 |
a. FP in EC is the mean time required to rebuild a new bone structural unit, calculated as wall thickness divided by MAR. Participants were given T for two 3 day-periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 6 and 24 months
| Intervention | year (Median) | |||
|---|---|---|---|---|
| DL and NL at 6 Months (n=23, 6) | DL, Imputed SL (ISL) and NL at 6 Months (n=23, 15) | DL and NL at 24 Months (n=8, 2) | DL, ISL and NL at 24 Months (n=9, 3) | |
| Teriparatide | 0.20 | 0.20 | 0.23 | 0.24 |
| Zoledronic Acid | 0.20 | 0.28 | 0.22 | 0.25 |
Aj.AR in CC is MAR averaged over the entire osteoid surface and in a steady state is an estimate of the mean rate of matrix apposition. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 24 months
| Intervention | micrometer (µm)/day (Median) | |
|---|---|---|
| DL and NL (n=9, 6) | DL, Imputed SL (ISL) and NL (n=10, 9) | |
| Teriparatide | 0.13 | 0.12 |
| Zoledronic Acid | 0.00 | 0.02 |
Aj.AR in CC is MAR averaged over the entire osteoid surface and in a steady state is an estimate of the mean rate of matrix apposition. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 6 months
| Intervention | µm/day (Median) | |
|---|---|---|
| DL and NL (n=28, 28) | DL, ISL and NL (n=28, 30) | |
| Teriparatide | 0.34 | 0.34 |
| Zoledronic Acid | 0.02 | 0.02 |
Aj.AR in EC is MAR averaged over the entire osteoid surface and in a steady state is an estimate of the mean rate of matrix apposition. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 6 and 24 months
| Intervention | micrometer (µm)/day (Median) | |||
|---|---|---|---|---|
| DL and NL at 6 Months (n=23, 20) | DL, Imputed SL (ISL) and NL at 6 Months (n=23, 29) | DL and NL at 24 Months (n=8, 7) | DL, ISL and NL at 24 Months (n=9, 8) | |
| Teriparatide | 0.41 | 0.41 | 0.35 | 0.32 |
| Zoledronic Acid | 0.00 | 0.03 | 0.00 | 0.00 |
The length of tetracycline double labels is a measure of the extent of bone formation in the endocortical compartment within individual remodeling units and is measured in millimeters (mm). Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. (NCT00927186)
Timeframe: 6 and 24 months
| Intervention | millimeter (mm) (Median) | |
|---|---|---|
| 6 months (n=23, 6) | 24 months (n=8, 2) | |
| Teriparatide | 0.34 | 0.27 |
| Zoledronic Acid | 0.30 | 0.30 |
BFR in CC is the volume of mineralized bone formed per unit surface bone per unit time (mm³/mm²/year); calculated as MAR times MS/BS. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 24 months
| Intervention | mm³/mm²/year (Median) | |
|---|---|---|
| DL and NL (n=9, 6) | DL, Imputed SL (ISL) and NL (n=10, 9) | |
| Teriparatide | 0.0057 | 0.0057 |
| Zoledronic Acid | 0.0000 | 0.0001 |
BFR in CC is the volume of mineralized bone formed per unit surface bone per unit time (cubic millimeter/square millimeter/year [mm³/mm²/year]); calculated as mineral apposition rate (MAR) times MS/BS. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 6 months
| Intervention | mm³/mm²/year (Median) | |
|---|---|---|
| DL and NL (n=28, 28) | DL, ISL and NL (n=28, 30) | |
| Teriparatide | 0.0116 | 0.0116 |
| Zoledronic Acid | 0.0002 | 0.0002 |
BFR in EC is the volume of mineralized bone formed per unit surface bone per unit time (mm³/mm²/year); calculated as MAR times MS/BS. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 6 and 24 months
| Intervention | mm³/mm²/year (Median) | |||
|---|---|---|---|---|
| DL and NL at 6 Months (n=23, 20) | DL, Imputed SL (ISL) and NL at 6 Months (n=23, 29) | DL and NL at 24 Months (n=8, 7) | DL, ISL and NL at 24 Months (n=9, 8) | |
| Teriparatide | 0.0307 | 0.0307 | 0.0093 | 0.0090 |
| Zoledronic Acid | 0.0000 | 0.0003 | 0.0000 | 0.0000 |
CTX is a measure of bone resorption. (NCT00927186)
Timeframe: Baseline, 1, 3, 6 months
| Intervention | nanogram/milliliter (ng/mL) (Median) | ||
|---|---|---|---|
| Change at 1 month (n= 32, 31) | Change at 3 months (n= 32, 29) | Change at 6 months (n= 25, 28) | |
| Teriparatide | 0.06 | 0.26 | 0.31 |
| Zoledronic Acid | -0.37 | -0.35 | -0.32 |
OC is a measure of osteoblast function. (NCT00927186)
Timeframe: Baseline, 1, 3, 6 months
| Intervention | µg/L (Median) | ||
|---|---|---|---|
| Change at 1 month (n= 32, 32) | Change at 3 months (n=32, 30) | Change at 6 months (n= 25, 29) | |
| Teriparatide | 22.35 | 29.93 | 30.85 |
| Zoledronic Acid | -3.39 | -12.30 | -14.06 |
PINP is a measure of bone formation. (NCT00927186)
Timeframe: Baseline, 1, 3, 6 months
| Intervention | microgram/Liter (µg/L) (Median) | ||
|---|---|---|---|
| Change at 1 month (n= 32, 31) | Change at 3 months (n= 32, 29) | Change at 6 months (n= 25, 28) | |
| Teriparatide | 65.50 | 66.00 | 84.00 |
| Zoledronic Acid | -15.00 | -39.00 | -37.50 |
MAR in CC is a measure of the linear rate of production of mineralized bone matrix by osteoblasts and is measured by the mean distance between two consecutive labels divided by the time interval. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 24 months
| Intervention | micrometer (µm)/day (Median) | |
|---|---|---|
| DL and NL (n=9, 6) | DL, Imputed SL (ISL) and NL (n=10, 9) | |
| Teriparatide | 0.44 | 0.43 |
| Zoledronic Acid | 0.00 | 0.30 |
MAR in CC is a measure of the linear rate of production of mineralized bone matrix by osteoblasts and is measured by the mean distance between two consecutive T labels divided by the time interval. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 6 months
| Intervention | micrometer (µm)/day (Median) | |
|---|---|---|
| DL and NL (n=28, 28) | DL, ISL and NL (n=28, 30) | |
| Teriparatide | 0.56 | 0.56 |
| Zoledronic Acid | 0.35 | 0.33 |
MAR in EC is a measure of the linear rate of production of mineralized bone matrix by osteoblasts and is measured by the mean distance between two consecutive labels divided by the time interval. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 6 and 24 months
| Intervention | micrometer (µm/day) (Median) | |||
|---|---|---|---|---|
| DL and NL at 6 Months (n=23, 20) | DL, Imputed SL (ISL) and NL at 6 Months (n=23, 29) | DL and NL at 24 Months (n=8, 7) | DL, ISL and NL at 24 Months (n=9, 8) | |
| Teriparatide | 0.50 | 0.50 | 0.43 | 0.42 |
| Zoledronic Acid | 0.00 | 0.30 | 0.00 | 0.00 |
Mlt in CC is the period between deposition and subsequent mineralization of osteoid. Mlt is calculated as O.Th divided by Aj.AR. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 24 months
| Intervention | day (Median) | |
|---|---|---|
| DL and NL (n=9, 2) | DL, Imputed SL (ISL) and NL (n=10, 5) | |
| Teriparatide | 38.84 | 45.33 |
| Zoledronic Acid | 45.67 | 128.37 |
Mlt in CC is the period between deposition and subsequent mineralization of osteoid. Mlt is calculated as Osteoid Thickness (O.Th) divided by Aj.AR. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 6 months
| Intervention | day (Median) | |
|---|---|---|
| DL and NL (n=28, 16) | DL, ISL and NL (n=28, 18) | |
| Teriparatide | 13.63 | 13.63 |
| Zoledronic Acid | 75.72 | 75.72 |
Mlt in EC is the period between deposition and subsequent mineralization of osteoid. Mlt is calculated as O.Th divided by Aj.AR. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 6 and 24 months
| Intervention | day (Median) | |||
|---|---|---|---|---|
| DL and NL at 6 Months (n=23, 6) | DL, Imputed SL (ISL) and NL at 6 Months (n=23, 15) | DL and NL at 24 Months (n=8, 2) | DL, ISL and NL at 24 Months (n=9, 3) | |
| Teriparatide | 12.63 | 12.63 | 15.67 | 17.04 |
| Zoledronic Acid | 26.97 | 26.70 | 42.86 | 29.03 |
MS/BS in EC is a measure of the proportion of BS on which new mineralized bone is deposited at the time of tetracycline (T) labeling and is calculated as sum of total extent of double label (DL) plus half the extent of single label (SL) divided by BS. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in the biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under a microscope. DL indicates active bone formation, SL or no label (NL) suggests suppression of bone formation. (NCT00927186)
Timeframe: 6 and 24 months
| Intervention | percentage of surface (Median) | |
|---|---|---|
| 6 months (n=23, 29) | 24 months (n=9, 8) | |
| Teriparatide | 18.64 | 5.82 |
| Zoledronic Acid | 0.30 | 0.00 |
Number of samples with single or double tetracycline labels, both single and double labels, or no labels in the cancellous compartment were compared between teriparatide and zoledronic acid treated participants. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. (NCT00927186)
Timeframe: 24 months
| Intervention | samples (Number) | |||
|---|---|---|---|---|
| No Label | Single Label Only | Double Label Only | Single and Double Label | |
| Teriparatide | 0 | 1 | 0 | 9 |
| Zoledronic Acid | 4 | 3 | 0 | 2 |
Number of samples with single or double tetracycline labels, both single and double labels, or no labels in the cancellous compartment were compared between teriparatide and zoledronic acid treated participants. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. (NCT00927186)
Timeframe: 6 months
| Intervention | samples (Number) | |||
|---|---|---|---|---|
| No Label | Single Label Only | Double Label Only | Single and Double Label | |
| Teriparatide | 0 | 0 | 0 | 28 |
| Zoledronic Acid | 12 | 2 | 3 | 13 |
Number of samples with single or double tetracycline labels, both single and double labels, or no labels in the endocortical compartment were compared between teriparatide and zoledronic acid treated participants. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. (NCT00927186)
Timeframe: 6 and 24 months
| Intervention | samples (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| No Label at 6 months (n=23, 29) | Single Label Only at 6 months (n=23, 29) | Double Label Only at 6 months (n=23, 29) | Single and Double Label at 6 months (n=23, 29) | No Label at 24 months (n=9, 8) | Single Label Only at 24 months (n=9, 8) | Double Label Only at 24 months (n=9, 8) | Single and Double Label at 24 months (n=9, 8) | |
| Teriparatide | 0 | 0 | 0 | 23 | 0 | 1 | 0 | 8 |
| Zoledronic Acid | 14 | 9 | 0 | 6 | 5 | 1 | 0 | 2 |
Omt in CC is the period between the onset of deposition and onset of mineralization of a given amount of osteoid. Omt is calculated as O.Th divided by MAR. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 24 months
| Intervention | day (Median) | |
|---|---|---|
| DL and NL (n=9, 2) | DL, Imputed SL (ISL) and NL (n=10, 5) | |
| Teriparatide | 13.42 | 13.52 |
| Zoledronic Acid | 17.38 | 13.92 |
Omt in CC is the period between the onset of deposition and onset of mineralization of a given amount of osteoid. Omt is calculated as O.Th divided by MAR. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 6 months
| Intervention | day (Median) | |
|---|---|---|
| DL and NL (n=28, 16) | DL, ISL and NL (n=28, 18) | |
| Teriparatide | 9.99 | 9.99 |
| Zoledronic Acid | 9.05 | 9.05 |
Omt in EC is the period between the onset of deposition and onset of mineralization of a given amount of osteoid. Omt is calculated as O.Th divided by MAR. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. (NCT00927186)
Timeframe: 6 and 24 Months
| Intervention | day (Median) | |||
|---|---|---|---|---|
| DL and NL at 6 Months (n=23, 6) | DL, Imputed SL (ISL) and NL at 6 Months (n=23, 15) | DL and NL at 24 Months (n=8, 2) | DL, ISL and NL at 24 Months (n=9, 3) | |
| Teriparatide | 10.57 | 10.57 | 12.30 | 13.03 |
| Zoledronic Acid | 11.27 | 11.34 | 14.94 | 12.12 |
Osteoid thickness (OTh.) in the endocortical compartment is a measure of the average thickness of osteoid seams. (NCT00927186)
Timeframe: 6 and 24 months
| Intervention | micrometer (µm) (Median) | |
|---|---|---|
| 6 months (n=23, 29) | 24 months (n=9, 8) | |
| Teriparatide | 4.94 | 5.23 |
| Zoledronic Acid | 3.70 | 3.53 |
The percent of single or double tetracycline labels per bone surface (sLS/BS, dLS/BS) in the cancellous compartment. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. (NCT00927186)
Timeframe: 24 months
| Intervention | percentage of tetracycline labels (Median) | |
|---|---|---|
| sLS/BS | dLS/BS | |
| Teriparatide | 2.25 | 1.69 |
| Zoledronic Acid | 0.15 | 0.00 |
The percent of single or double tetracycline labels per bone surface (sLS/BS, dLS/BS) in the cancellous compartment. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. (NCT00927186)
Timeframe: 6 months
| Intervention | percentage of tetracycline labels (Median) | |
|---|---|---|
| sLS/BS | dLS/BS | |
| Teriparatide | 3.19 | 4.13 |
| Zoledronic Acid | 0.02 | 0.07 |
The percent of single or double tetracycline labels per bone surface (sLS/BS, dLS/BS) in the endocortical compartment. Participants were given T for two 3-day periods, 14 days apart. T fluoresces under certain light and temporarily binds to new bone. New bone in biopsy is seen as the amount of bone between 2 fluorescently T labeled lines under microscope. DL indicates active bone formation, SL or NL suggests suppression of bone formation. (NCT00927186)
Timeframe: 6 and 24 months
| Intervention | percentage of tetracycline labels (Median) | |||
|---|---|---|---|---|
| sLS/BS at 6 months (n=23, 29) | dLS/BS at 6 months (n=23, 29) | sLS/BS at 24 months (n=9, 8) | dLS/BS at 24 months (n=9, 8) | |
| Teriparatide | 5.56 | 13.46 | 3.75 | 2.77 |
| Zoledronic Acid | 0.25 | 0.00 | 0.00 | 0.00 |
To assess the time course of the treatment, the BMD data of the lumbar spine was assessed by dual energy X-ray absorptiometry (DXA) and analyzed using a mixed model repeated measures (MMRM) method, with the repeated measure occurring at each visit (for example, 6 and 12 month). BMD values are corrected data and have been standardized across the machine types (Hologic and Lunar). (NCT01011556)
Timeframe: Baseline to 6 Months and 12 Months
| Intervention | percentage change in BMD (Least Squares Mean) | |
|---|---|---|
| 6 months (n=54, 52, 51, 58) | 12 months (n=52, 48, 45, 50) | |
| 20 Mcg Subcutaneous Teriparatide | 4.72 | 8.12 |
| 30 Mcg Transdermal Teriparatide | 0.19 | 0.62 |
| 50 Mcg Transdermal Teriparatide | 0.78 | 0.66 |
| 80 Mcg Transdermal Teriparatide | 1.19 | 1.93 |
Bone mineral density (BMD) of the lumbar spine was assessed by dual energy X-ray absorptiometry (DXA). BMD values are corrected data and have been standardized across the machine types (Hologic and Lunar). Analyses were performed using ANCOVA model with the baseline value as a covariate and pooled site and treatment as fixed effects. (NCT01011556)
Timeframe: Baseline, 6 Months
| Intervention | percentage change in BMD (Least Squares Mean) |
|---|---|
| 20 Mcg Subcutaneous Teriparatide | 4.74 |
| 30 Mcg Transdermal Teriparatide | 0.16 |
| 50 Mcg Transdermal Teriparatide | 0.88 |
| 80 Mcg Transdermal Teriparatide | 1.19 |
(NCT01011556)
Timeframe: Pre-dose, 30 minutes, 2 hours at Baseline and 12 Months
| Intervention | beats per minute (bpm) (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| BL, supine, 30 min (n=56,54,51,62) | BL, supine, 2 h (n=56,56,53,63) | BL, standing, 30 min (n=56,54,51,62) | BL, standing, 2 h (n=56,56,53,64) | 12 mon, supine, 30 min (n=51,47,44,51) | 12 mon, supine, 2 h (n=51,47,44,51) | 12 mon, standing, 30 min (n=51,47,44,51) | 12 mon, standing, 2 h (n=51,47,44,51) | |
| 20 Mcg Subcutaneous Teriparatide | 1.8 | 1.5 | 1.6 | 1.0 | 2.5 | 1.6 | 1.2 | 0.9 |
| 30 Mcg Transdermal Teriparatide | 1.7 | 0.9 | -1.0 | -0.8 | 1.4 | 1.1 | 0.0 | 0.1 |
| 50 Mcg Transdermal Teriparatide | -0.8 | -0.8 | 0.7 | 0.5 | -0.1 | -0.3 | -0.7 | -0.4 |
| 80 Mcg Transdermal Teriparatide | -0.6 | -0.4 | -1.2 | -1.0 | -0.2 | -0.8 | -0.4 | -0.7 |
(NCT01011556)
Timeframe: Baseline, 6 Months, 12 Months
| Intervention | millimole/day (mmol/day) (Mean) | ||
|---|---|---|---|
| Baseline | 6 months (n=54, 50, 49, 56) | 12 months (n=51, 47, 41, 51) | |
| 20 Mcg Subcutaneous Teriparatide | 4.45 | 2.02 | 5.25 |
| 30 Mcg Transdermal Teriparatide | 4.21 | 0.70 | 4.97 |
| 50 Mcg Transdermal Teriparatide | 4.26 | 1.20 | 4.80 |
| 80 Mcg Transdermal Teriparatide | 4.24 | 1.35 | 4.51 |
Participants were tested for anti-recombinant teriparatide and anti-synthetic teriparatide titers. Either none were detected (ND) or antibodies were determined to be present if the teriparatide specific antibody titers were at least 1:8 (titer 1:8). (NCT01011556)
Timeframe: Baseline and 1, 3, 12, and 13 Months (mon)
| Intervention | participants (Number) | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline: anti-recombinant ND (n=57, 54, 53, 64) | Baseline:anti-recombinant titer 1:8(n=57,54,53,64) | 1 mon:anti-recombinant ND (n=54,54,51,62) | 1 mon:anti-recombinant titer 1:8 (n=54,54,51,62 | 3 mon:anti-recombinant ND (n=55,52,51,61) | 3 mon:anti-recombinant titer 1:8 (n=55,52,51,6 | 12 mon:anti-recombinant ND (n=52,48,45,51) | 12 mon:anti-recombinant titer 1:8 (n=52,48,45,51) | 13 mon:anti-recombinant ND (n=50,46,44,50) | 13 mon:anti-recombinant titer 1:8 (n=50,46,44,50) | Baseline:anti-synthetic ND (n=57,54,53,64) | Baseline:anti-synthetic titer 1:8 (n=57,54,53,64) | 1 mon:anti-synthetic ND (N=54,54,51,62) | 1 mon:anti-synthetic titer 1:8 (N=54,54,51,62) | 3 mon:anti-synthetic ND (n=55,52,51,61) | 3 mon:anti-synthetic titer 1:8 (n=55,52,51,61) | 12 mon:anti-synthetic ND (n=52,48,45,51) | 12 mon:anti-synthetic titer 18 (n=52,48,45,51) | 13 mon:anti-synthetic ND (n=50,46,44,50) | 13 mon:anti-synthetic titer 1:8 (n=50,46,44,50) | |
| 20 Mcg Subcutaneous Teriparatide | 57 | 0 | 54 | 0 | 55 | 0 | 52 | 0 | 50 | 0 | 57 | 0 | 54 | 0 | 55 | 0 | 52 | 0 | 50 | 0 |
| 30 Mcg Transdermal Teriparatide | 54 | 0 | 54 | 0 | 52 | 0 | 48 | 0 | 46 | 0 | 54 | 0 | 54 | 0 | 52 | 0 | 48 | 0 | 46 | 0 |
| 50 Mcg Transdermal Teriparatide | 52 | 1 | 51 | 0 | 50 | 1 | 44 | 1 | 43 | 1 | 52 | 1 | 50 | 1 | 50 | 1 | 44 | 1 | 43 | 1 |
| 80 Mcg Transdermal Teriparatide | 64 | 0 | 62 | 0 | 61 | 0 | 51 | 0 | 50 | 0 | 64 | 0 | 62 | 0 | 61 | 0 | 51 | 0 | 50 | 0 |
Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) measured at pre-dose and 30 minutes (min) and 2 hours (hr) post-dose in both the supine and standing position. (NCT01011556)
Timeframe: Pre-Dose, 30 minutes, 2 hours Post-Dose at Baseline and 12 Months
| Intervention | mmHg (Mean) | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| BL, supine, SBP, 30 min (n=56,54,51,62) | BL, supine, SBP, 2 h (n=56,56,53,63) | BL, supine, DBP, 30 min (n=56,54,51,62) | BL, supine, DBP, 2 h (n=56,56,53,63) | 12mon, supine, SBP, 30min (n=51,47,44,51) | 12mon, supine, SBP, 2 h (n=51,47,44,51) | 12mon, supine, DBP, 30min (n=52,48,45,51) | 12mon, supine, DBP, 2 h (n=51,47,44,51) | BL, standing, SBP, 30 min (n=56,54,51,62) | BL, standing, SBP, 2 h (n=56,56,53,64) | BL, standing, DBP, 30 min (n=56,54,51,62) | BL, standing, DBP, 2 h (n=56,56,53,64) | 12mon, standing, SBP, 30min(n=51,47,44,51) | 12mon, standing, SBP, 2 h (n=51,47,44,51) | 12mon, standing, DBP, 30 min(n=51,47,44,51 | 12mon, standing, DBP, 2 h (n=51,47,44,51) | |
| 20 Mcg Subcutaneous Teriparatide | -0.6 | -0.3 | -1.9 | -2.1 | 0.8 | -0.2 | -1.8 | -1.3 | -1.3 | -1.7 | -2.3 | -2.3 | -0.6 | -0.1 | -1.8 | 1.1 |
| 30 Mcg Transdermal Teriparatide | 2.0 | -0.9 | 1.4 | -0.8 | -2.2 | -1.8 | -1.8 | -3.3 | 2.5 | -1.6 | 0.2 | -2.1 | -0.9 | -0.4 | -2.4 | -2.0 |
| 50 Mcg Transdermal Teriparatide | -1.0 | -3.5 | -2.5 | -3.6 | -1.1 | -2.5 | -2.1 | -1.3 | -0.6 | -3.8 | -1.2 | -1.1 | 0.5 | -1.3 | -3.5 | -1.9 |
| 80 Mcg Transdermal Teriparatide | -0.8 | -0.6 | -1.1 | -1.6 | -2.0 | -1.9 | -1.2 | -2.0 | -0.5 | 0.0 | -1.2 | -1.7 | -0.8 | -0.9 | 1.4 | 0.1 |
Procollagen Type 1 N-Terminal Propeptide (P1NP) is a marker of bone formation. (NCT01011556)
Timeframe: Baseline, 1 Month
| Intervention | percentage change in P1CP (Median) |
|---|---|
| 20 Mcg Subcutaneous Teriparatide | 80.10 |
| 30 Mcg Transdermal Teriparatide | 4.63 |
| 50 Mcg Transdermal Teriparatide | 12.30 |
| 80 Mcg Transdermal Teriparatide | 23.84 |
Serum calcium adjusted for serum albumin levels is calculated using the following formula: Total Calcium + [(40 - albumin) x 0.02]. Analysis for serum calcium and albumin adjusted serum calcium were collected at predose, 4 hours (h) post-dose (PD) and 6 h PD at baseline and 12 months (mon). (NCT01011556)
Timeframe: Baseline, 12 Months
| Intervention | millimole/Liter (mmol/L) (Mean) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline- predose; no adjustment (n=54,53,51,62) | Baseline- 4 h PD; no adjustment (n=55,53,51,63) | Baseline- 6 h PD; no adjustment (n=52,51,48,59) | 12 mon-predose; no adjustment (n=52,47,45,50) | 12 mon-4 h PD; no adjustment (n=51,46,44,51) | 12 mon-6 h PD; no adjustment (n=50,45,44,51) | baseline-predose albumin adjusted (n=53,53,50,60) | baseline-4 h PD; albumin adjusted (n=52,52,50,61) | baseline-6 h PD; albumin adjusted (n=49,50,47,57) | 12 mon- predose albumin adjusted (n=52,47,45,50) | 12 mon- 4 h PD; albumin adjusted (n=51,46,44,51) | 12 mon-6 h PD; albumin adjusted (n=52,47,45,50) | |
| 20 Mcg Subcutaneous Teriparatide | 2.391 | 2.432 | 2.440 | 2.463 | 2.516 | 2.532 | 2.363 | 2.418 | 2.423 | 2.461 | 2.523 | 2.547 |
| 30 Mcg Transdermal Teriparatide | 2.362 | 2.358 | 2.369 | 2.427 | 2.428 | 2.426 | 2.341 | 2.348 | 2.363 | 2.432 | 2.438 | 2.443 |
| 50 Mcg Transdermal Teriparatide | 2.389 | 2.403 | 2.400 | 2.427 | 2.430 | 2.443 | 2.376 | 2.403 | 2.404 | 2.449 | 2.458 | 2.481 |
| 80 Mcg Transdermal Teriparatide | 2.392 | 2.393 | 2.397 | 2.432 | 2.464 | 2.467 | 2.373 | 2.386 | 2.394 | 2.442 | 2.482 | 2.483 |
CEUQ consists of 5 sections and 16 questions using a 5-point Likert scale designed to collect measures for ease of use (S1), convenience of use (S2), confidence of use (S3), fear of use (S4), and overall satisfaction with therapy (S5). CEUQ is not a validated instrument. (NCT01011556)
Timeframe: baseline up to 12 months
| Intervention | participants (Number) | ||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| S1-Stronly Disagree | S1-Somewhat Disagree | S1-Neutral | S1-Somewhat Agree | S1-Strongly Agree | S2-Strongly Disagree | S2-Somewhat Disagree | S2-Neutral | S2-Somewhat Agree | S2-Strongly Agree | S3-Not Confident | S3-Somewhat Not Confident | S3-Neutral | S3-Somewhat Confident | S3-Very Confident | S4-Extremely Fearful | S4-Somewhat Fearful | S4-Neutral | S4-Somewhat Not Fearful | S4-Not Fearful | S5-Very Dissatisfied | S5-Somewhat Dissatisfied | S5-Neutral | S5-Somewhat Satisfied | S5-Very Satisfied | |
| 20 Mcg Subcutaneous Teriparatide | 0 | 0 | 0 | 11 | 44 | 0 | 0 | 1 | 11 | 43 | 0 | 0 | 0 | 13 | 42 | 0 | 1 | 1 | 9 | 44 | 0 | 0 | 1 | 10 | 44 |
| 30 Mcg Transdermal Teriparatide | 0 | 0 | 0 | 9 | 45 | 0 | 0 | 1 | 12 | 41 | 0 | 1 | 0 | 15 | 38 | 0 | 1 | 0 | 16 | 37 | 0 | 1 | 0 | 13 | 40 |
| 50 Mcg Transdermal Teriparatide | 0 | 0 | 1 | 8 | 42 | 0 | 0 | 1 | 9 | 41 | 1 | 0 | 3 | 11 | 36 | 1 | 0 | 1 | 9 | 40 | 0 | 1 | 2 | 10 | 38 |
| 80 Mcg Transdermal Teriparatide | 0 | 0 | 0 | 10 | 52 | 0 | 0 | 0 | 12 | 50 | 0 | 1 | 4 | 17 | 40 | 0 | 1 | 0 | 13 | 48 | 0 | 0 | 1 | 18 | 43 |
Severity of edema was categorized based on a 5 point scale: 0=no edema, 4=severe edema (defined as an area raised more than 1 millimeter and extending beyond area of exposure) (NCT01011556)
Timeframe: 13 Month follow-up
| Intervention | participants (Number) | |
|---|---|---|
| 0=no edema | 1=very slight edema to 4=severe edema | |
| 20 Mcg Subcutaneous Teriparatide | 41 | 0 |
| 30 Mcg Transdermal Teriparatide | 39 | 0 |
| 50 Mcg Transdermal Teriparatide | 39 | 0 |
| 80 Mcg Transdermal Teriparatide | 43 | 0 |
Severity of erythema was categorized based on a 5 point scale: 0=no erythema, 4=severe erythema (defined as beet red to eschar) (NCT01011556)
Timeframe: 13 Month follow-up
| Intervention | participants (Number) | |
|---|---|---|
| 0=no erythema | 1=very slight erythema to 4=severe erythema | |
| 20 Mcg Subcutaneous Teriparatide | 41 | 0 |
| 30 Mcg Transdermal Teriparatide | 39 | 0 |
| 50 Mcg Transdermal Teriparatide | 39 | 0 |
| 80 Mcg Transdermal Teriparatide | 43 | 0 |
C-terminal telopeptide is a marker of bone resorption. (NCT01011556)
Timeframe: Baseline, 1 Month, 3 Months, 6 Months, 12 Months
| Intervention | percentage change in CTX (Mean) | |||
|---|---|---|---|---|
| 1 month (n=49, 53, 49, 60) | 3 months (n=50, 51, 49, 59) | 6 months (n=48, 49, 48, 56) | 12 months (n=47, 46, 43, 49) | |
| 20 Mcg Subcutaneous Teriparatide | 20.57 | 87.78 | 123.36 | 97.52 |
| 30 Mcg Transdermal Teriparatide | 8.05 | 30.66 | 37.36 | 37.75 |
| 50 Mcg Transdermal Teriparatide | 13.35 | 42.40 | 68.63 | 61.25 |
| 80 Mcg Transdermal Teriparatide | 21.66 | 90.36 | 127.81 | 114.11 |
Procollagen Type 1 N-Terminal Propeptide (P1NP) is a marker of bone formation. (NCT01011556)
Timeframe: Baseline, 1 Month, 3 Months, 6 Months, 12 Months
| Intervention | percentage change in P1NP (Mean) | |||
|---|---|---|---|---|
| 1 month (n=49, 53, 49, 60) | 3 months (n=50, 51, 49, 59) | 6 months (n=48, 49, 48, 56) | 12 months (n=47, 46, 43, 49) | |
| 20 Mcg Subcutaneous Teriparatide | 112.47 | 174.88 | 284.89 | 232.41 |
| 30 Mcg Transdermal Teriparatide | 19.29 | 35.68 | 62.99 | 72.17 |
| 50 Mcg Transdermal Teriparatide | 27.78 | 53.53 | 93.82 | 97.14 |
| 80 Mcg Transdermal Teriparatide | 42.06 | 116.34 | 221.28 | 178.02 |
Bone mineral density (BMD) of the lumbar spine was assessed by dual energy X-ray absorptiometry (DXA). BMD values are corrected data and have been standardized across the machine types (Hologic and Lunar). Analyses were performed using ANCOVA model and least square (LS) means were adjusted for baseline BMD values as a covariate and pooled site and treatment as fixed effects. (NCT01011556)
Timeframe: Baseline, 12 Months
| Intervention | percentage change in BMD (Least Squares Mean) |
|---|---|
| 20 Mcg Subcutaneous Teriparatide | 7.80 |
| 30 Mcg Transdermal Teriparatide | 0.63 |
| 50 Mcg Transdermal Teriparatide | 0.32 |
| 80 Mcg Transdermal Teriparatide | 1.63 |
Bone area is a defined region of interest of bone. (NCT01078805)
Timeframe: Baseline, up to month 24
| Intervention | percent change of centimeter square (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Femoral Neck | Forearm | Inter-Trochanter | L1-L4 | Total Hip | Trochanter | Wards Triangle | |
| FORTEO (Teriparatide)-Treated | 2.231 | 4.680 | 1.828 | 3.907 | 2.648 | 3.395 | 1.826 |
BMC is an estimate of the amount of mineral (such as calcium) in the bone. (NCT01078805)
Timeframe: Baseline, up to month 24
| Intervention | percentage (%) change of grams (g) (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Femoral Neck | Forearm | Inter-Trochanter | L1-L4 | Total Hip | Trochanter | Wards Triangle | |
| FORTEO (Teriparatide)-Treated | 4.187 | 7.243 | 5.716 | 20.774 | 8.303 | 4.968 | 50.996 |
A BMD test measures the amount of mineral (such as calcium) in a defined area of bone, grams per square centimeter (g/cm²). (NCT01078805)
Timeframe: Baseline, up to month 24
| Intervention | percentage (%) change of BMD (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Femoral Neck | Forearm | Inter-Trochanter | Lumbar spine vertebrae numbered 1 through 4(L1-L4) | Total Hip | Trochanter | Wards Triangle | |
| FORTEO (Teriparatide)-Treated | 2.569 | 0.626 | 1.532 | 6.419 | 3.766 | 2.604 | 3.394 |
Clinical vertebral fracture was defined as a fracture that caused pain and/or discomfort, came to medical attention, and was confirmed by the investigator. Vertebral fracture sites included thoracic vertebra number 4 (T4) through lumbar spine vertebra number 4 (L4). Vertebral fracture is binary outcome (Yes/No). Percentage of participants= number of participants with new vertebral fracture/ number of participants at risk * 100. (NCT01078805)
Timeframe: up to 24 months
| Intervention | Percentage of participants (Number) | |||
|---|---|---|---|---|
| 0 to 6 months (n=3720) | 6 to 12 months (n=2996) | 12 to 18 months (n=2606) | 18 to 24 months (n=2266) | |
| FORTEO (Teriparatide)-Treated | 0.67 | 0.40 | 0.35 | 0.35 |
Non-vertebral fragility fracture is defined as low trauma fracture, such as a fall from standing height. It is binary outcome (Yes/No). Percentage of participants = number of participants with new Non-Vertebral Fragility Fracture/ number of participants at risk * 100. (NCT01078805)
Timeframe: up to 24 months
| Intervention | Percentage of participants (Number) | |||
|---|---|---|---|---|
| 0 to 6 months (n=3720) | 6 to 12 months (n=2970) | 12 to 18 months (n=2570) | 18 to 24 months (n=2225) | |
| FORTEO (Teriparatide)-Treated | 1.42 | 0.91 | 0.70 | 0.81 |
Visual analog pain scale is a measurement instrument to measure the level of pain. Scores range from 0 to 100. Higher score indicates greater pain. Mean percentage change is (Pain score at baseline visit - Pain score at Month 24)/Pain score at baseline visit*100%. (NCT01078805)
Timeframe: Baseline, Month 24
| Intervention | percentage change of pain score (Mean) |
|---|---|
| FORTEO (Teriparatide)-Treated | -36.2 |
Visual analog pain scale is a measurement instrument to measure the level of pain. Scores range from 0 to 100. Higher score indicates greater pain. Mean percentage change is (Pain score at baseline visit - Pain score at Month 24)/Pain score at baseline visit*100%. (NCT01078805)
Timeframe: Baseline, Month 24
| Intervention | percentage change of pain score (Mean) |
|---|---|
| FORTEO (Teriparatide)-Treated | -24.9 |
Treatment adherence is the duration of time participants were on Forteo therapy during the 24-month treatment phase of the study. (NCT01078805)
Timeframe: up to 24 months
| Intervention | days (Mean) | |||
|---|---|---|---|---|
| 0 to 6 months (n=701) | 6 to 12 months (n=382) | 12 to 18 months (n=338) | 18 to 24 months (n=2299) | |
| FORTEO (Teriparatide)-Treated | 72.5 | 272.5 | 450.7 | 743.7 |
Average fractional content of bone expressed in percent (NCT01153425)
Timeframe: Change between baseline and 12 months
| Intervention | Percentage of Change (Mean) |
|---|---|
| Teriparatide (Forteo) | 1.0 |
| Zoledronic Acid (Reclast) | 0.6 |
Ratio of the volume densities of surface (S) and curve (C)-type voxels, S/C (NCT01153425)
Timeframe: Change between baseline and 12 months
| Intervention | Percentage of Change (Mean) |
|---|---|
| Teriparatide (Forteo) | 9.1 |
| Zoledronic Acid (Reclast) | 7.1 |
One-third radius BMD was measured at the baseline, three month and six month visits. The outcome data is an overall average and range from all time points. (NCT01166958)
Timeframe: BMD measured at the baseline, 3 month, and 6 month visits.
| Intervention | g/cm2 (Mean) |
|---|---|
| Daily Teriparatide (Forteo) | 0.6858 |
| Monthly Cycles of Teriparatide Followed by Raloxifene | 0.687 |
Hip BMD was measured at the baseline, three month and six month visits. The outcome data is an overall average and range from all time points. (NCT01166958)
Timeframe: BMD measured at the baseline, 3 month, and 6 month visits.
| Intervention | g/cm2 (Mean) |
|---|---|
| Daily Teriparatide (Forteo) | 0.7951 |
| Monthly Cycles of Teriparatide Followed by Raloxifene | 0.7898 |
Serum P1NP was measured at all study visits following the screening visit. The outcome data is an overall average and range from all time points. (NCT01166958)
Timeframe: These were measured at the baseline and 1, 1.5, 2, 2.5, 3, 4, 5 and 6 month visits.
| Intervention | mcg/L (Mean) |
|---|---|
| Daily Teriparatide (Forteo) | 128.7 |
| Monthly Cycles of Teriparatide Followed by Raloxifene | 83.8 |
Spine BMD was measured at the baseline, three month and six month visits. The outcome data is an overall average and range from all time points. (NCT01166958)
Timeframe: BMD measured at the baseline, 3 month, and 6 month visits.
| Intervention | g/cm2 (Mean) |
|---|---|
| Daily Teriparatide (Forteo) | 0.9599 |
| Monthly Cycles of Teriparatide Followed by Raloxifene | 0.9006 |
Serum CTX was measured at all study visits following the screening visit. The outcome data is an overall average and range from all time points. (NCT01166958)
Timeframe: These were measured at the baseline and 1, 1.5, 2, 2.5, 3, 4, 5 and 6 month visits.
| Intervention | ng/mL (Mean) |
|---|---|
| Daily Teriparatide (Forteo) | 0.9887 |
| Monthly Cycles of Teriparatide Followed by Raloxifene | 0.5445 |
Arms were compared for total number of adverse events, including severe and serious adverse events. (NCT01171690)
Timeframe: Approximately 90 days after surgery
| Intervention | events (Number) |
|---|---|
| Teriparatide | 0 |
| Control | 0 |
"Hospital length of stay from initiation of therapy with calcium and calcitriol to ready to discharge from a calcium perspective (calcium level > 7.5 mg/dL and increasing x 2 over 12 hours in an asymptomatic patient with stable therapy and no need for intravenous (IV) calcium in last 24 hours)." (NCT01171690)
Timeframe: Approximately 7 days after surgery
| Intervention | days (Mean) |
|---|---|
| Teriparatide | 1.1 |
| Control | 2.4 |
The mean change in C-terminal telopeptide from baseline after 12 month of treatment (NCT01225055)
Timeframe: Baseline to 12 Months
| Intervention | ng/ml (Mean) | |||
|---|---|---|---|---|
| 0 months | 3 months | 6 months | 12 months | |
| Teriparatide | 0.38 | 0.72 | 0.74 | 0.59 |
| Teriparatide and Vibration | 0.38 | 0.43 | 0.44 | 0.45 |
| Vibration | 0.31 | 0.25 | 0.25 | 0.29 |
The mean change in Bone-specific alkaline phosphatase from baseline after 12 month of therapy (NCT01225055)
Timeframe: Baseline to 12 Months
| Intervention | ng/ml (Mean) | |||
|---|---|---|---|---|
| 0 months | 3 months | 6 months | 12 months | |
| Teriparatide | 15.3 | 18.4 | 20.3 | 20.4 |
| Teriparatide and Vibration | 12.4 | 12.8 | 16.2 | 14.0 |
| Vibration | 13.9 | 11.6 | 11.3 | 11.8 |
The mean change in Amino-terminal of type 1 collagen from baseline after 12 months of treatment (NCT01225055)
Timeframe: Baseline to 12 Months
| Intervention | ng/ml (Mean) | |||
|---|---|---|---|---|
| 0 months | 3 months | 6 months | 12 months | |
| Teriparatide | 67.1 | 128 | 163 | 124 |
| Teriparatide and Vibration | 67.9 | 90.1 | 125 | 77.0 |
| Vibration | 64.7 | 51.8 | 54.5 | 49.8 |
The mean change in BMD of the total hip after 12 month of treatment (NCT01225055)
Timeframe: Baseline to 12 Months
| Intervention | g/cm^2 (Mean) | |||
|---|---|---|---|---|
| 0 months | 3 months | 6 months | 12 months | |
| Teriparatide | 0.66 | 0.65 | 0.67 | 0.66 |
| Teriparatide and Vibration | 0.64 | 0.65 | 0.65 | 0.65 |
| Vibration | 0.63 | 0.63 | 0.63 | 0.64 |
The mean change in BMD at the lumbar spine from baseline after 12 month of treatment (NCT01225055)
Timeframe: Baseline to 12 Months
| Intervention | g/cm^2 (Mean) | |||
|---|---|---|---|---|
| 0 months | 3 months | 6 months | 12 months | |
| Teriparatide | 1.04 | 1.05 | 1.07 | 1.09 |
| Teriparatide and Vibration | 1.02 | 1.04 | 1.05 | 1.07 |
| Vibration | 1.00 | 1.01 | 1.02 | 1.02 |
The mean change in BMD of the femoral neck after 12 month of treatment (NCT01225055)
Timeframe: Baseline to 12 Months
| Intervention | g/cm^2 (Mean) | |||
|---|---|---|---|---|
| 0 months | 3 months | 6 months | 12 months | |
| Teriparatide | 0.66 | 0.66 | 0.67 | 0.66 |
| Teriparatide and Vibration | 0.62 | 0.63 | 0.63 | 0.63 |
| Vibration | 0.63 | 0.64 | 0.62 | 0.63 |
Number of evaluation points (patches) showing defined Draize score. Erythema and edema were used to determine skin irritation and sensitization. Score 0 = No Erythema/Edema; Score 1 = Very slight Erythema/Edema (barely perceptible); Score 2 = Well defined Erythema/Edema (edges of area well defined by definite raising); Score 3 = Moderate to Severe Erythema/Edema (raised approximately 1 mm); Score 4 = Severe Edema (raised more than 1 mm and extending beyond area of exposure). (NCT01250145)
Timeframe: Days 1 - 19 and 34 - 37
| Intervention | patches with Draize scores (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Erythema: Score 0 | Erythema: Score 1 | Erythema: Score 2 | Erythema: Score 3 | Edema: Score 0 | Edema: Score 1 | Edema: Score 2 | Edema: Score 3 | Edema: Score 4 | |
| Part B: Active Patch - 1 Hour Post Patch Removal | 122 | 1503 | 840 | 14 | 930 | 1141 | 399 | 5 | 4 |
| Part B: Active Patch - 24 Hours Post Patch Application | 436 | 1899 | 138 | 1 | 1759 | 661 | 53 | 1 | 0 |
| Part B: Active Patch - Prior to Patch Application | 1399 | 1050 | 30 | 0 | 2280 | 197 | 2 | 0 | 0 |
| Part B: Placebo Patch - 1 Hour Post Patch Removal | 271 | 1698 | 495 | 10 | 1572 | 766 | 136 | 0 | 0 |
| Part B: Placebo Patch - 24 Hours Post Patch Application | 784 | 1578 | 107 | 0 | 2014 | 435 | 19 | 1 | 0 |
| Part B: Placebo Patch - Prior to Patch Application | 1525 | 924 | 25 | 0 | 2330 | 143 | 1 | 0 | 0 |
Number of patches with adhesion score. Score 0 = ≥90% adhered (essentially no lift off the skin); Score 1= ≥75% to <90% adhered (some edges only lifting off the skin); Score 2 = ≥50% to <75% adhered (less than half of the patch lifting off the skin); Score 3 = >0% to <50% adhered but not detached (more than half of the patch lifting off the skin without falling off); Score 4 = 0% adhered - patch detached (patch completely off the skin). (NCT01250145)
Timeframe: Days 1 - 19 and 34 - 37
| Intervention | patches with adhesive score (Number) | ||||
|---|---|---|---|---|---|
| Score 0 | Score 1 | Score 2 | Score 3 | Score 4 | |
| Active Patch | 2608 | 40 | 13 | 9 | 13 |
| Placebo Patch | 2608 | 31 | 17 | 17 | 5 |
Number of patches with adhesion score. Score 0 = ≥90% adhered (essentially no lift off the skin); Score 1= ≥75% to <90% adhered (some edges only lifting off the skin); Score 2 = ≥50% to <75% adhered (less than half of the patch lifting off the skin); Score 3 = >0% to <50% adhered but not detached (more than half of the patch lifting off the skin without falling off); Score 4 = 0% adhered - patch detached (patch completely off the skin). (NCT01250145)
Timeframe: Day 1 through Day 22
| Intervention | patches with adhesive score (Number) | ||||
|---|---|---|---|---|---|
| Score 0 | Score 1 | Score 2 | Score 3 | Score 4 | |
| Active Patch | 879 | 8 | 1 | 0 | 1 |
| Placebo Patch | 882 | 7 | 0 | 0 | 0 |
Number of evaluation points (patches) showing defined Draize score. Erythema and edema were used to determine skin irritation. Score 0 = No Erythema/Edema; Score 1 = Very slight Erythema/Edema (barely perceptible); Score 2 = Well defined Erythema/Edema (edges of area well defined by definite raising); Score 3 = Moderate to Severe Erythema/Edema (raised approximately 1 millimeter [mm]). (NCT01250145)
Timeframe: Day 1 through Day 22
| Intervention | patches with Draize scores (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Erythema: Score 0 | Erythema: Score 1 | Erythema: Score 2 | Erythema: Score 3 | Edema: Score 0 | Edema: Score 1 | Edema: Score 2 | Edema: Score 3 | |
| Part A: Active Patch - 1 Hour Post Patch Removal | 40 | 674 | 176 | 0 | 113 | 600 | 175 | 1 |
| Part A: Active Patch - 24 Hours Post Patch Application | 146 | 633 | 106 | 2 | 370 | 454 | 62 | 1 |
| Part A: Active Patch - Prior to Patch Application | 299 | 523 | 65 | 1 | 604 | 270 | 13 | 1 |
| Part A: Placebo Patch - 1 Hour Post Patch Removal | 69 | 713 | 108 | 0 | 298 | 511 | 80 | 0 |
| Part A: Placebo Patch - 24 Hours Post Patch Application | 205 | 601 | 79 | 2 | 539 | 322 | 26 | 0 |
| Part A: Placebo Patch - Prior to Patch Application | 390 | 452 | 45 | 1 | 716 | 166 | 5 | 1 |
"Bone turnover was assessed indirectly by evaluating cellular parameters of PTH action (i.e. numbers of osteoblasts, osteoclasts, apoptotic osteoblasts). The methods used to obtain the outcomes described below were bone histomorphometry using the following abbreviation:~Ct.T.Ar: Ct Cort(ex)(ical) Tissue Area (2D)b First set refers to baseline pre-drug data and second set was taken at the end of the drug administration phase." (NCT01279187)
Timeframe: 10 weeks
| Intervention | mm2/week (Mean) | |
|---|---|---|
| Ct.T.Ar first set Cortical Tissue Area | Ct. T.Ar second set Cortical Tissue Area | |
| Control | 1.8 | 1.8 |
| Teriparatide | 2.2 | 2.2 |
"Bone histomorphometry was used to assess bone perimeter length in mm as follows:~Cn.Pm cancellous: Cancellous Bone Perimeter Ec.Pm: endocortical bone perimeter Ps.Pm: Periosteal Periosteal bone perimeter" (NCT01279187)
Timeframe: 10 weeks
| Intervention | mm (Mean) | ||
|---|---|---|---|
| Cn.Pm cancellous Cancellous bone Perimeter | Ec.Pm endocortical bone perimeter | Ps.Pm Periosteal Periosteal bone perimeter | |
| Control | 18.7 | 3.6 | 4.3 |
| Teriparatide | 20.8 | 2.9 | 4.1 |
"Oc.S/BS cancellous: Osteoclast suface divided by bone surface. Osteoclastic surface as percent of total bone surface in cancellous bone. Percent cancellous bone perimeter with osteoclasts (large, multinuclear, TRAP positive cells).~OS/BS cancellous: Osteoid surface divided by bone surface. Percentage of cancellous bone perimeter covered with osteoid.~Oc.S/BS endocortical: Osteoclastic surface as percent of total bone surface in endocortical bone.~OS/BS endocortical: Percentage of endocortical bone perimeter covered with osteoid.~Oc.S/BS Periosteal: Osteoclastic surface as percent of total bone surface in periosteal bone.~Ob.S/BS Periosteal: Percent periosteal bone perimeter with osteoid and adjacent osteoblasts, identified as plump cells with a single, eccentric nucleus and a pale-staining golgi apparatus. Osteoblast Surface divided by bone surface in periosteal bone.~OS/BS Periosteal: Percentage of periosteal bone perimeter covered with osteoid." (NCT01279187)
Timeframe: 10 weeks
| Intervention | percentage (%) (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Oc.S/BS cancellous | OS/BS cancellous | Oc.S/BS endocortical | OS/BS endocortical | Oc.S/BS Periosteal | Ob.S/BS Periosteal | OS/BS Periosteal | |
| Control | 0.15 | 12 | 0.3 | 17 | 0.4 | 5 | 25 |
| Teriparatide | 0.34 | 8 | 0 | 14 | 0.1 | 6 | 5 |
To determine the impact of PTH on bone quality and bone turnover in the oral cavity. The primary outcome variable will be bone formation rate. (NCT01279187)
Timeframe: 10 weeks
| Intervention | mm2/week (Median) |
|---|---|
| Teriparatide | 1.76 |
| Control | 2.22 |
"Bone turnover was assessed indirectly by bone histomorphometry using the following abbreviations: Mineral Apposition Rate (MAR): Distance between 2 fluorochrome markers that comprise a double label on the surfaces of cancellous bone measured at an average of 4 equally-spaced sites per double label. These measurements will be performed on 20 double fluorochrome labels per bone and the average divided by the time between the midpoints of the two labeling periods. MAR serves as an index of osteoblast activity. Reported for cancellous (Cn), endocortical (Ec) at baseline (pre-drug intervention, listed as first set) and at the end of drug intervention (second set). First set refers to baseline information (pre-drug), and second set refers to data evaluated at the end of the drug administration phase. Periosteal (Ps) data and Ec.Mar Endocortical MAR second set was reviewed but no analyzable labeling was noted and so this data is not reported." (NCT01279187)
Timeframe: 10 weeks
| Intervention | um/day (Mean) | ||
|---|---|---|---|
| Cn.MAR (Cancellous MAR) - first set | Ec.MAR Endocortical MAR - first set | Cn.MAR Cancellous MAR- second set | |
| Control | 0.3 | 0.6 | 0.3 |
| Teriparatide | 0.5 | 0.7 | 0.2 |
"The self-reported pain Visual Analog Score (VAS), the score range is 0-100 with higher scores indicating more pain.~European Quality of Life - 5 Dimensions (EQ-5D) is a standardized instrument for measuring generic health status, the scale range is from 0.000 (death) to 1.000 (perfect health).~Oswestry Disability Index (ODI) provides information about how back or leg pain is affecting the ability to manage in everyday life, the points range from 0-50, which is doubled and reported as a percentage. Higher scores indicate higher disability." (NCT01292252)
Timeframe: One year
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Visual Analog Score (VAS) | European Quality of Life - 5 Dimensions (EQ-5D) | Oswestry Disability Index (ODI) | |
| Control: Saline Placebo | 9.67 | 0.708 | 31.9 |
| Treatment: Forteo, Terapeptide 20 ug | 11.67 | 0.733 | 32.3 |
Quality of spine fusion, measured by the number of participants with complete spine fusion at 1 year. Spine fusion at one year was assessed using thin-section helical computed tomography (CT) scan of the lumbar spine. (NCT01292252)
Timeframe: One year
| Intervention | Participants (Count of Participants) |
|---|---|
| Treatment: Forteo, Terapeptide 20 ug | 11 |
| Control: Saline Placebo | 6 |
Number of participants with serious adverse events and other (not including serious) adverse events at one year are reported. (NCT01292252)
Timeframe: One year
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Serious Adverse Events | Other (Not Including Serious) Adverse Events | |
| Control: Saline Placebo | 1 | 6 |
| Treatment: Forteo, Terapeptide 20 ug | 1 | 9 |
(NCT01321723)
Timeframe: 24 weeks from baseline
| Intervention | percentage of change (Mean) |
|---|---|
| Forsteo (Teriparatide) | 5.07 |
| PTH Analog Tablets | 2.21 |
| Placebo | -0.17 |
(NCT01321723)
Timeframe: 24 weeks from baseline
| Intervention | percentage of change (Mean) |
|---|---|
| Forsteo (Teriparatide) | 210.07 |
| PTH Analog Tablets | 12.05 |
| Placebo | -1.75 |
Serum collagen type I (CTx-1) fragments generated during osteoclastic bone turnover are biomarkers for bone resorption. β-CrossLaps electrochemiluminescent sandwich immunoassay was used. (NCT01321723)
Timeframe: 24 weeks from baseline
| Intervention | percentage of change (Mean) |
|---|---|
| Forsteo (Teriparatide) | 113.32 |
| PTH Analog Tablets | 12.72 |
| Placebo | 15.13 |
AUC: (PTH analog tablets timepoints - baseline to 5.75 hours) (Forsteo injection timepoints - baseline to 2 hours) (NCT01321723)
Timeframe: 24 weeks
| Intervention | pg* hr/mL (Mean) |
|---|---|
| Forsteo (Teriparatide) | 152 |
| PTH Analog Tablets | 165 |
(NCT01321723)
Timeframe: 24 weeks
| Intervention | participants (Number) |
|---|---|
| Forsteo (Teriparatide) | 23 |
| PTH Analog Tablets | 30 |
| Placebo | 21 |
(NCT01343004)
Timeframe: Basline and 18 months
| Intervention | percent change from baseline (Mean) |
|---|---|
| Placebo | 0.48 |
| BA058 80 mcg (Abaloparatide) | 9.20 |
| Teriparatide | 9.12 |
(NCT01343004)
Timeframe: Baseline and 18 months
| Intervention | percent change (Mean) |
|---|---|
| Placebo | -0.08 |
| BA058 80 mcg (Abaloparatide) | 3.44 |
| Teriparatide | 2.81 |
(NCT01343004)
Timeframe: 18 months
| Intervention | Hypercalcemic events (Number) |
|---|---|
| Placebo | 5 |
| BA058 80 mcg (Abaloparatide) | 15 |
| Teriparatide | 34 |
(NCT01343004)
Timeframe: 18 months
| Intervention | participants (Number) |
|---|---|
| Placebo | 30 |
| BA058 80 mcg (Abaloparatide) | 4 |
| Teriparatide | 6 |
(NCT01343004)
Timeframe: 18 months
| Intervention | Participants (Number) |
|---|---|
| Placebo | 33 |
| BA058 80 mcg (Abaloparatide) | 18 |
| Teriparatide | 24 |
(NCT01343004)
Timeframe: Baseline and 18 months
| Intervention | percent change (Mean) |
|---|---|
| Placebo | -0.44 |
| BA058 80 mcg (Abaloparatide) | 2.90 |
| Teriparatide | 2.26 |
Both hands were scanned using a CT scanner. A semi-automated software tool was used to segment the erosion margins in 3D. A board certified radiologist identified the individual erosions in six sub-regions: radius, ulna, proximal carpals, distal carpals, metacarpophalangeal (MCP) joints and proximal interphalangeal (PIP) joints. The average total in a single hand/wrist was calculated. A negative change from Baseline(less joint erosions) indicates improvement. (NCT01400516)
Timeframe: Baseline and Month 12
| Intervention | cubic millimeter (mm^3) (Median) | |
|---|---|---|
| Baseline | Change from Baseline at Month 12 | |
| Control Arm | 571.4 | 9.1 |
| Teriparatide | 369.8 | -0.4 |
The DAS28 score is a measure of the patient's disease activity calculated using the tender joint count (TJC) [28 joints], swollen joint count (SJC) [28 joints], patient's global assessment of disease activity [visual analog scale: 0=no disease activity to 100=maximum disease activity] and C-Reactive Protein (CRP) for a total possible score of 2 to 10. Higher values indicate higher disease activity. A negative change from baseline indicates improvement. (NCT01400516)
Timeframe: Baseline and Month 12
| Intervention | score on a scale (Mean) | |
|---|---|---|
| Baseline | Change from Baseline at Month 12 | |
| Control Arm | 2.73 | -0.50 |
| Teriparatide | 2.66 | 0.42 |
BMD was measured at the lumbosacral spine antero-posterior and at the femoral neck using a densitometer. A positive change from Baseline (increased bone density) indicates improvement. (NCT01400516)
Timeframe: Baseline and Month 12
| Intervention | grams/centimeters squared (g/cm^2) (Mean) | |||
|---|---|---|---|---|
| Spine, Baseline | Spine, Change from Baseline at Month12 | Femoral neck, Baseline | Femoral neck, Change from Baseline at Month 12 | |
| Control Arm | 0.93 | -0.002 | 0.73 | -0.03 |
| Teriparatide | 0.91 | 0.06 | 0.68 | 0.03 |
Total serum calcium concentration adjusted by serum albumin concentration. Corrected calcium (mg/dL) = total serum calcium concentration (mg/dL) + 4.0 - serum albumin concentration (grams per deciliter [g/dL]). Postdose refers to after Teriparatide dose. (NCT01430104)
Timeframe: Day 28 (16 and 24 hours postdose)
| Intervention | participants (Number) | |
|---|---|---|
| 16 hours postdose | 24 hours postdose | |
| 600 mg Aspara-CA + 1 µg Alfarol + 20 µg Teriparatide | 0 | 0 |
Daily profiles of corrected mean serum calcium levels were determined for each participant. Corrected calcium (milligram per deciliter [mg/dL]) = total serum calcium concentration (mg/dL) + 4.0 - serum albumin concentration (grams per deciliter [g/dL]). The Least Squares (LS) means were adjusted for Day, Timepoint, Day*Timepoint, and random error. At baseline, participants received only Aspara-CA and Alfarol supplements and the timepoints were based on the times before Aspara-CA and Alfarol administration (predose) and after Aspara-CA and Alfarol administration (postdose). During the 28-day Teriparatide Treatment Period, timepoints were based on before Teriparatide administration (predose) and after Teriparatide administration (postdose). (NCT01430104)
Timeframe: Baseline (Day -1 of 14-day Lead-in Period) and Day 1 and Day 7 and Day 14 and Day 28 at 0 hours (h), 2 h, 4 h, 6 h, 16 h, and 24 h postdose (28-day Teriparatide Treatment Period)
| Intervention | mg/dL (Least Squares Mean) | |||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline: 0 h predose | Baseline: 2 h postdose | Baseline: 4 h postdose | Baseline: 6 h postdose | Baseline: 16 h postdose | Baseline: 24 h postdose | Day 1: 0 h predose | Day 1: 2 h postdose | Day 1: 4 h postdose | Day 1: 6 h postdose | Day 1: 16 h postdose | Day 1: 24 h postdose | Day 7: 0 h predose (n=28) | Day 7: 2 h postdose (n=28) | Day 7: 4 h postdose (n=28) | Day 7: 6 h postdose (n=28) | Day 7: 16 h postdose (n=28) | Day 7: 24 h postdose (n=28) | Day 14: 0 h predose (n=28) | Day 14: 2 h postdose (n=28) | Day 14: 4 h postdose (n=28) | Day 14: 6 h postdose (n=28) | Day 14: 16 h postdose (n=28) | Day 14: 24 h postdose (n=28) | Day 28: 0 h predose (n=28) | Day 28: 2 h postdose (n=28) | Day 28: 4 h postdose (n=28) | Day 28: 6 h postdose (n=28) | Day 28: 16 h postdose (n=28) | Day 28: 24 h postdose (n=28) | |
| 600 mg Aspara-CA + 1 µg Alfarol + 20 µg Teriparatide | 9.00 | 9.11 | 8.98 | 8.92 | 8.97 | 8.74 | 8.74 | 9.17 | 9.16 | 9.14 | 8.85 | 8.70 | 9.02 | 9.41 | 9.43 | 9.36 | 9.02 | 8.82 | 8.99 | 9.35 | 9.39 | 9.29 | 9.03 | 8.89 | 8.98 | 9.41 | 9.42 | 9.33 | 9.04 | 8.85 |
Total serum calcium concentration adjusted by serum albumin concentration. Corrected calcium (mg/dL) = total serum calcium concentration (mg/dL) + 4.0 - serum albumin concentration (grams per deciliter [g/dL]). Serum calcium levels presented are for any time postdose on any day during the 28-day Teriparatide Treatment Period. (NCT01430104)
Timeframe: Day 1 up to Day 28 (Teriparatide Treatment Period)
| Intervention | participants (Number) | |
|---|---|---|
| Serum Calcium > 11.0 mg/dL | Serum Calcium > 13.5 mg/dL | |
| 600 mg Aspara-CA + 1 µg Alfarol + 20 µg Teriparatide | 0 | 0 |
Urine calcium levels presented are for any day during the 28-day Teriparatide Treatment Period. (NCT01430104)
Timeframe: Day 1 up to Day 28 (28-day Teriparatide Treatment Period)
| Intervention | participants (Number) |
|---|---|
| 600 mg Aspara-CA + 1 µg Alfarol + 20 µg Teriparatide | 0 |
(NCT01430104)
Timeframe: Day 1, Day 7, Day 14, Day 28 (28-day Teriparatide Treatment Period)
| Intervention | grams per day (g/day) (Mean) | |||
|---|---|---|---|---|
| Change from Baseline at Day 1 | Change from Baseline at Day 7 (N=27) | Change from Baseline at Day 14 (N=27) | Change from Baseline at Day 28 (N=27) | |
| 600 mg Aspara-CA + 1 µg Alfarol + 20 µg Teriparatide | 0.01 | 0.02 | 0.01 | 0.01 |
Corrected calcium (milligram per deciliter [mg/dL]) = total serum calcium concentration (mg/dL) + 4.0 - serum albumin concentration (grams per deciliter [g/dL]). The Least Squares (LS) means were controlled for Day, Timepoint, Day*Timepoint, and random error. Postdose refers to after Teriparatide dose. (NCT01430104)
Timeframe: Baseline (Day -1 of the 14-day Lead-in Period), Day 1, Day 7, Day 14, Day 28 at 0 hours (h), 2 h, 4 h, 6 h, 16 h, and 24 h postdose (28-day Teriparatide Treatment Period)
| Intervention | mg/dL (Least Squares Mean) | |||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Change from Baseline Day 1: 0 h predose | Change from Baseline at Day 1: 2 h postdose | Change from Baseline at Day 1: 4 h postdose | Change from Baseline at Day 1: 6 h postdose | Change from Baseline at Day 1: 16 h postdose | Change from Baseline at Day 1: 24 h postdose | Change from Baseline at Day 7: 0 h predose, n=28 | Change from Baseline at Day 7: 2 h postdose, n=28 | Change from Baseline at Day 7: 4 h postdose, n=28 | Change from Baseline at Day 7: 6 h postdose, n=28 | Change from Baseline at Day 7: 16 h postdose, n=28 | Change from Baseline at Day 7: 24 h postdose, n=28 | Change from Baseline at Day 14: 0 h predose, n=28 | Change from Baseline at Day 14: 2 h postdose, n=28 | Change from Baseline at Day 14: 4 h postdose, n=28 | Change from Baseline at Day 14: 6 h postdose, n=28 | Change from Baseline at Day 14: 16 h postdose,n=28 | Change from Baseline at Day 14: 24 h postdose,n=28 | Change from Baseline at Day 28: 0 h predose, n=28 | Change from Baseline at Day 28: 2 h postdose, n=28 | Change from Baseline at Day 28: 4 h postdose, n=28 | Change from Baseline at Day 28: 6 h postdose, n=28 | Change from Baseline at Day 28: 16 h postdose,n=28 | Change from Baseline at Day 28: 24 h postdose,n=28 | |
| 600 mg Aspara-CA + 1 µg Alfarol + 20 µg Teriparatide | -0.255 | 0.059 | 0.183 | 0.221 | -0.117 | -0.038 | 0.018 | 0.286 | 0.450 | 0.436 | 0.061 | 0.068 | -0.018 | 0.232 | 0.404 | 0.368 | 0.068 | 0.143 | -0.021 | 0.286 | 0.436 | 0.404 | 0.082 | 0.104 |
(NCT01430104)
Timeframe: Day 1 (Predose, 28-day Teriparatide Treatment Period) and Day 8 and Day 15 and Day 29 (Follow-up Period) and Day 35 (Follow-up Period)
| Intervention | picogram per milliliter (pg/mL) (Mean) | ||||
|---|---|---|---|---|---|
| Day 1 | Day 8 (N=28) | Day 15 (N=28) | Day 29 (N=28) | Day 35 (N=28) | |
| 600 mg Aspara-CA + 1 µg Alfarol + 20 µg Teriparatide | 54.0 | 105.3 | 108.5 | 98.1 | 53.9 |
(NCT01430104)
Timeframe: Day 1 (Predose, 28-day Teriparatide Treatment Period) and Day 8 and Day 15 and Day 29 (Follow-up Period) and Day 35 (Follow-up Period)
| Intervention | nanogram per milliliter (ng/mL) (Mean) | ||||
|---|---|---|---|---|---|
| Day 1 | Day 8 (N=28) | Day 15 (N=28) | Day 29 (N=28) | Day 35 (N=28) | |
| 600 mg Aspara-CA + 1 µg Alfarol + 20 µg Teriparatide | 23.0 | 22.1 | 21.5 | 20.1 | 21.6 |
(NCT01430104)
Timeframe: Day 1 and Day 7 and Day 14 and Day 28 (28-day Teriparatide Treatment Period)
| Intervention | grams per day (g/day) (Mean) | |||
|---|---|---|---|---|
| Day 1 | Day 7 (N=27) | Day 14 (N=27) | Day 28 (N=27) | |
| 600 mg Aspara-CA + 1 µg Alfarol + 20 µg Teriparatide | 0.13 | 0.14 | 0.13 | 0.13 |
Dual Energy X-ray Absorptiometry (DXA) will be used to measuring bone mineral density (BMD). (NCT01440803)
Timeframe: Baseline and 12 months
| Intervention | percentage of change (Mean) |
|---|---|
| Teriparatide (Forteo) | 10.1 |
| Placebo Saline Injection | 4.1 |
Revision surgery (re-operation) was defined as any additional surgical intervention performed or recommended at the site of the index procedure, except those that were planned at the time of the index procedure. (NCT01473589)
Timeframe: 12 months
| Intervention | percentage of participants (Number) |
|---|---|
| Teriparatide | 87 |
| Placebo | 86 |
Prefracture ambulatory status was defined as either ambulatory with or without a walking aid. A participant was considered to have regained their prefracture ambulatory status if the participant's postsurgery ambulatory status was returned to or was improved from their pre-surgery ambulatory status. Percentage was calculated as = (number of participants who regained their ambulatory status / total number analyzed) * 100. (NCT01473589)
Timeframe: Up to 12 months
| Intervention | percentage of participants (Number) |
|---|---|
| Teriparatide | 73.2 |
| Placebo | 56.9 |
"Functional healing was defined as ability to walk with a gait speed ≥ 0.05 meters/second (m/s) with a change from baseline ≥ -0.1 m/s. The walking test involved having the participant walk a distance of 7 meters (m) at a self-selected, comfortable pace. A 4-m portion of the test was timed to determine the participant's gait speed in m/s.~Percentage was calculated as: (number of participants with functional evidence of healing / total number of participants analyzed) * 100." (NCT01473589)
Timeframe: 12 Months
| Intervention | percentage of participants (Number) |
|---|---|
| Teriparatide | 85.4 |
| Placebo | 74.0 |
The walking test involved having the participant walk a distance of 7 m at a self-selected, comfortable pace. A 4-m portion of the test was timed to determine the participant's gait speed in m/s. LS means was calculated using ANCOVA and adjusted for baseline, treatment group, region, fracture type, and fixation type. (NCT01473589)
Timeframe: Baseline, up to 6 Months
| Intervention | m/s (Least Squares Mean) |
|---|---|
| Teriparatide | -0.672 |
| Placebo | 1.524 |
"The signs of femoral neck fracture healing included disappearance of the fracture line on radiographs. If a participant had radiographic evidence of healing at the 12-month visit, that participant was considered to have radiographic evidence of healing.~Percentage was calculated as: (number of participants with radiographic evidence of healing / total number of participants analyzed) * 100." (NCT01473589)
Timeframe: Randomization up to 12 months
| Intervention | percentage of participants (Number) |
|---|---|
| Teriparatide | 78.3 |
| Placebo | 78.7 |
The worst pain numeric rating scale (NRS) was used to assess the impact of pain on a participant's life. NRS Item 3 assessed the worst musculoskeletal pain severity during the walking test. Pain was measured by an 11-point Likert scale. The following cut-points were used to categorize the NRS responses: 0 = no pain, 1 to 4 = mild pain, 5 to 6 = moderate pain, and 7 to 10 = severe pain. Participants with an NRS score of <7 were categorized as having no severe fracture-site pain with ambulation and no worsening of NRS scores >2 from baseline. Percentage was calculated as: (Number of participants with pain control during ambulation / total number of participants) * 100. (NCT01473589)
Timeframe: Up to 12 months
| Intervention | percentage of participants (Number) |
|---|---|
| Teriparatide | 91.5 |
| Placebo | 89.8 |
Ability to ambulate was defined as ambulatory with convalescent aid or without convalescent aid. Percentage was calculated as: (number of participants able to ambulate / number of total participants analyzed) * 100. (NCT01473589)
Timeframe: Up to 12 months
| Intervention | percentage of participants (Number) |
|---|---|
| Teriparatide | 97.9 |
| Placebo | 98 |
The EQ-5D is a 5-item, self-reported, generic, multidimensional, health-related, quality-of-life instrument with 5 items. Overall health state score was also self-reported using a visual analogue scale (VAS) marked on a scale scored from 0 (worse imaginable health state) to 100 (best imaginable health state). LS mean was calculated using ANCOVA and adjusted for baseline, treatment group, and region. (NCT01473589)
Timeframe: Baseline, up to 6 Months
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Teriparatide | 7.4 |
| Placebo | 7.6 |
The worst pain NRS was used to assess the impact of pain on a participant's life. Fracture-site pain severity was assessed for pain on weight bearing. Pain was measured by an 11-point Likert scale. Participants with an NRS score of <7 during weight bearing and no worsening of NRS >2 from baseline were categorized as having no severe fracture-site pain. Percentage was calculated as: (number of participants with pain control during weight bearing / total number of participants) * 100. (NCT01473589)
Timeframe: Up to 12 months
| Intervention | percentage of participants (Number) |
|---|---|
| Teriparatide | 89.4 |
| Placebo | 88.0 |
Time to revision surgery was defined as the time from initial hip fracture surgery to revision surgery, or recommendation for revision surgery if recommended but not performed. Time to revision surgery was censored at the date of the last contact. (NCT01473589)
Timeframe: Baseline to revision surgery (up to 14.14 Months)
| Intervention | days (Median) |
|---|---|
| Teriparatide | 358.5 |
| Placebo | 350 |
The worst pain NRS was used to assess the impact of pain on a participant's life. Participants with an NRS score of <7 were categorized as having no severe fracture-site pain. Least Squares (LS) means was calculated using analysis of covariance (ANCOVA) and adjusted for baseline, treatment group, region, fracture type, and fixation type. (NCT01473589)
Timeframe: Baseline, 6 Months
| Intervention | units on a scale (Least Squares Mean) | ||
|---|---|---|---|
| During ambulation (n = 45, 46) | During 24 hours preceding visit (n = 47, 50) | On weight bearing (n = 46, 49) | |
| Placebo | 0.2 | -0.8 | 0.8 |
| Teriparatide | 0.2 | -0.3 | 0.7 |
SF-12 is a self-reported questionnaire covering a mental component score (MCS) and a physical component score (PCS), each scoring from a 0 to 100 (worst to best) scale. LS mean was calculated using ANCOVA and adjusted for baseline, treatment group, region, fracture type, fixation type, visit, and visit-by-treatment interaction. (NCT01473589)
Timeframe: Baseline, up to 6 Months
| Intervention | units on a scale (Least Squares Mean) | |
|---|---|---|
| PCS Month 6 (n = 49, 49) | MCS Month 6 (n = 49, 49) | |
| Placebo | -4.75 | -0.49 |
| Teriparatide | -3.73 | -0.58 |
WOMAC is: a self-reported questionnaire that consisted of 24 questions covering 3 health domains: Pain (5 items: during walking, using stairs, in bed, sitting or lying, and standing), Stiffness (2 items: after first waking and later in the day), and Physical Function. Each domain was scored by summing the individual items and transforming the scores into a 0 to 100 (best to worst) scale. LS mean was calculated using ANCOVA and adjusted for baseline, treatment group, region, fracture type, fixation type, visit, and visit-by-treatment interaction. (NCT01473589)
Timeframe: Baseline, up to 6 Months
| Intervention | units on a scale (Least Squares Mean) | ||
|---|---|---|---|
| Physical Function Score - Month 6 (n=48, 51) | Pain Score - Month 6 ( n = 51, 51) | Stiffness Score - Month 6 (n = 51, 51) | |
| Placebo | 12.8 | 10.3 | 11.8 |
| Teriparatide | 12.9 | 8.2 | 13.1 |
The worst pain NRS was used to assess the impact of pain on a participant's life. Fracture-site pain severity was assessed for pain in the 24 hours preceding a visit. Pain was measured by an 11-point Likert scale. Participants with an NRS score of <7 in the 24 hours preceding a visit and no worsening of NRS >2 from baseline were categorized as having no severe fracture-site pain. Percentage was calculated as: (number of participants with pain control during 24 hours preceding a visit / total number of participants) * 100. (NCT01473589)
Timeframe: Up to 12 months
| Intervention | percentage of participants (Number) |
|---|---|
| Teriparatide | 88.0 |
| Placebo | 82.4 |
The NRS was used to assess the impact of pain on a participant's life. Fracture-site pain severity was assessed for pain in the 24 hours preceding a visit. Pain was measured by an 11-point Likert scale. Participants with an NRS score of <7 in the 24 hours preceding a visit and no worsening of NRS score >2 from baseline were categorized as having no severe fracture-site pain. Percentage was calculated as: (number of participants with pain control during 24 hours preceding a visit / total number of participants analyzed) * 100. (NCT01473602)
Timeframe: Up to 12 months
| Intervention | Percentage of participants (Number) |
|---|---|
| Teriparatide | 81.8 |
| Placebo | 92.9 |
WOMAC: was a self-reported questionnaire that consisted of 24 questions covering 3 health domains: Pain (5 items: during walking, using stairs, in bed, sitting or lying, and standing), Stiffness (2 items: after first waking and later in the day), and Physical Function. Each domain was scored by summing the individual items and transforming the scores into a 0 to 100 (best to worst) scale. Lower scores indicated better health status or functioning. LS means was calculated using ANCOVA adjusted for baseline, treatment group, region, fracture type, fixation type, visit, and visit-by-treatment interaction. (NCT01473602)
Timeframe: Baseline, up to 6 Months
| Intervention | Units on a scale (Least Squares Mean) | ||
|---|---|---|---|
| Physical Function Score - Month 6 (n=11, 12) | Pain Score - Month 6 (n=12, 13) | Stiffness Score - Month 6 (n=12, 15) | |
| Placebo | 1.1 | 13.6 | 16.9 |
| Teriparatide | 10.5 | 10.6 | 13.5 |
The EQ-5D is a 5-item, self-reported, generic, multidimensional, health-related, quality-of-life instrument with 5 items. Overall health state score was also self-reported using a visual analogue scale (VAS) marked on a scale scored from 0 (worst imaginable health state) to 100 (best imaginable health state). Higher scores represented better health state with 0 representing worst imaginable health state and 100 representing best imaginable health state. LS means was calculated using ANCOVA adjusted for baseline, treatment group, region. (NCT01473602)
Timeframe: Baseline, 6 Months
| Intervention | Units on a scale (Least Squares Mean) |
|---|---|
| Teriparatide | 13.0 |
| Placebo | 10.4 |
SF-12 is a self-reported questionnaire covering a mental component score (MCS) and a physical component score (PCS), each scoring from a 0 to 100 (worst to best) scale. LS means was calculated using ANCOVA adjusted for baseline, treatment group, region, fracture type, fixation type, visit, and visit-by-treatment interaction. (NCT01473602)
Timeframe: Baseline, 6 Months
| Intervention | Units on a scale (Least Squares Mean) | |
|---|---|---|
| PCS Month 6 (n=12, 14) | MCS Month 6 (n=12, 14) | |
| Placebo | 1.78 | -10.71 |
| Teriparatide | 0.89 | -8.84 |
The worst pain NRS was used to assess the impact of pain on a participant's life. Participants with an NRS score of <7 were categorized as having no severe fracture-site pain. Least squares (LS) means was calculated using analysis of covariance (ANCOVA) adjusted for baseline, treatment group, region, fracture type, and fixation type. (NCT01473602)
Timeframe: Baseline, 6 Months
| Intervention | Units on a scale (Least Squares Mean) | ||
|---|---|---|---|
| During ambulation ( n= 10, 13) | During 24 hours preceding visit (n= 10, 14) | On weight bearing (n= 10, 13) | |
| Placebo | -1.3 | -1.4 | -1.4 |
| Teriparatide | -1.6 | -1.2 | -2.0 |
Ability to ambulate was defined as ambulatory with or without convalescent aid. Percentage was calculated as: (number of participants able to ambulate / total number of participants analyzed) * 100. (NCT01473602)
Timeframe: Up to 12 months
| Intervention | Percentage of participants (Number) |
|---|---|
| Teriparatide | 76.9 |
| Placebo | 93.3 |
The walking test involved having the participant walk a distance of 7 m at a self-selected, comfortable pace. A 4-m portion of the test was timed to determine the participant's gait speed in m/s. LS means was calculated using ANCOVA adjusted for baseline, treatment group, region, fracture type, and fixation type (NCT01473602)
Timeframe: Baseline, 6 Months
| Intervention | m/s (Least Squares Mean) |
|---|---|
| Teriparatide | 0.168 |
| Placebo | 0.118 |
The worst pain NRS was used to assess the impact of pain on a participant's life. Fracture-site pain severity was assessed for pain on weight bearing. Pain was measured by an 11-point Likert scale. Participants with an NRS score of <7 during weight bearing and no worsening of NRS score >2 from baseline were categorized as having no severe fracture-site pain. Percentage was calculated as: (number of participants with pain control during weight bearing / total number of participants) * 100. (NCT01473602)
Timeframe: Up to 12 months
| Intervention | Percentage of participants (Number) |
|---|---|
| Teriparatide | 90.9 |
| Placebo | 84.6 |
"The signs of femoral neck fracture healing and healing complications included disappearance of the fracture line on radiographs. If a participant had radiographic evidence of healing at the 12-month visit, that participant was considered to have radiographic evidence of healing.~Percentage was calculated as: (number of participants with radiographic evidence of healing / total number of participants analyzed) * 100." (NCT01473602)
Timeframe: Randomization up to 12 months
| Intervention | Percentage of participants (Number) |
|---|---|
| Teriparatide | 55.6 |
| Placebo | 65.0 |
Time to revision surgery was defined as the time from initial hip fracture surgery to revision surgery, or recommendation for revision surgery if recommended but not performed. Time to revision surgery was censored at the date of the last contact. (NCT01473602)
Timeframe: Baseline to Revision Surgery (up to 14.14 Months)
| Intervention | Days (Median) |
|---|---|
| Teriparatide | 333.5 |
| Placebo | 361 |
The worst pain numeric rating scale (NRS) was used to assess the impact of pain on a participant's life. NRS Item 3 assessed the worst musculoskeletal pain severity during the walking test. Pain was measured by an 11-point Likert scale. The following cut-points were used to categorize the NRS responses: 0 = no pain, 1 to 4 = mild pain, 5 to 6 = moderate pain, and 7 to 10 = severe pain. Higher scores indicated more severe pain. Participants with an NRS score of <7 and no worsening of NRS scores >2 from baseline were categorized as having no severe fracture-site pain. Percentage was calculated as: (number of participants with pain control during ambulation / total number of participants analyzed) * 100. (NCT01473602)
Timeframe: Up to 12 months
| Intervention | Percentage of participants (Number) |
|---|---|
| Teriparatide | 90.0 |
| Placebo | 100.0 |
Revision surgery (re-operation) was defined as any additional surgical intervention performed or recommended at the site of the index procedure, except those that were planned at the time of the index procedure. (NCT01473602)
Timeframe: 12 months
| Intervention | Percentage of participants (Number) |
|---|---|
| Teriparatide | 74 |
| Placebo | 93 |
"Functional healing was defined as ability to walk with a gait speed ≥ 0.05 meters/second (m/s) with a change from baseline ≥ -0.1 m/s. The walking test involved having the participant walk a distance of 7 meters (m) at a self-selected, comfortable pace. A 4-m portion of the test was timed to determine the participant's gait speed in m/s.~Percentage was calculated as: (number of participants with functional evidence of healing / total number of participants analyzed) * 100." (NCT01473602)
Timeframe: Up to 12 Months
| Intervention | Percentage of participants (Number) |
|---|---|
| Teriparatide | 76.9 |
| Placebo | 66.7 |
Prefracture ambulatory status was defined as either ambulatory with or without a walking aid. A participant was considered to have regained their prefracture ambulatory status if the participant's postsurgery ambulatory status was returned to or was improved from their pre-surgery ambulatory status. Percentage was calculated as = (number of participants who regained their ambulatory status / total number of participants analyzed) *100. (NCT01473602)
Timeframe: Up to 12 months
| Intervention | Percentage of participants (Number) |
|---|---|
| Teriparatide | 47.1 |
| Placebo | 62.5 |
counting the total new morphometric vertebral fractures as determined by x-ray from baseline through end of study (NCT01611571)
Timeframe: baseline through 18 months
| Intervention | vertebral fracture (Number) |
|---|---|
| Active Risedronate Active Teriparatide | 1 |
| Active Risedronte Placebo Teriparatide | 1 |
| Placebo Risedronate Active Teriparatide | 0 |
change in spine bone density at 18 months measured by DXA 18 and 24 months (NCT01611571)
Timeframe: 18 months
| Intervention | % change in LS BMD (Least Squares Mean) |
|---|---|
| Active Risedronate Active Teriparatide | 6.95 |
| Active Risedronte Placebo Teriparatide | 3.76 |
| Placebo Risedronate Active Teriparatide | 5.68 |
Change in the Femoral Neck BMD at 18 month (NCT01611571)
Timeframe: 18 months
| Intervention | % change in TH BMD (Mean) |
|---|---|
| Active Risedronate Active Teriparatide | 8.45 |
| Active Risedronte Placebo Teriparatide | 0.5 |
| Placebo Risedronate Active Teriparatide | 3.89 |
change in 1/3 radius of forearm bone density as measured by DXA (NCT01611571)
Timeframe: baseline and 18 months
| Intervention | % change in 1/3 Radius BMD (Mean) |
|---|---|
| Active Risedronate Active Teriparatide | 1.6 |
| Active Risedronte Placebo Teriparatide | 0.11 |
| Placebo Risedronate Active Teriparatide | 0.02 |
change in hip bone density measured by DXA (NCT01611571)
Timeframe: baseline and 18 months
| Intervention | % change in TH BMD (Mean) |
|---|---|
| Active Risedronate Active Teriparatide | 3.86 |
| Active Risedronte Placebo Teriparatide | 0.82 |
| Placebo Risedronate Active Teriparatide | 0.29 |
(NCT01656629)
Timeframe: up to 3 months
| Intervention | percent change in osteoprogenitor cells (Mean) |
|---|---|
| Teriparatide | 0.0000242 |
| Alendronate | 0.0000104 |
| Calcium and Vitamin D | -0.0000068 |
Number of participants with persistence of alignment as determined by a radiologist. (NCT01705587)
Timeframe: at 10 weeks for immediate teriparatide group
| Intervention | Participants (Count of Participants) |
|---|---|
| Immediate Teriparatide | 5 |
| Delayed Teriparatide | 4 |
Percent change in Bone Mineral Density (BMD) as assessed by dual x-ray absorptiometry (DXA) at the spine, contralateral hip, distal 1/3 radius, and femoral neck (NCT01705587)
Timeframe: at 6 and 12 months
| Intervention | percentage change in BMD (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Spine-PA (6 months) | Spine-PA (12 months) | Total Hip (6 months) | Total Hip (12 months) | Femoral Neck (6 months) | Femoral Neck (12 months) | Distal 1/3 Radius (6 months) | Distal 1/3 Radius (12 months) | |
| Delayed Teriparatide | -0.6 | 5.4 | -0.8 | 1.5 | -2.7 | -1.9 | -0.7 | -6.1 |
| Immediate Teriparatide | 2.1 | 2.8 | -1.6 | -0.3 | -1.8 | -2.5 | -0.6 | -1.9 |
Assessed by quality of life questionnaire (SF-36). There are 8 subscales each ranging from 0-100 with higher scores indicating better quality of life. (NCT01705587)
Timeframe: at 12 months
| Intervention | units on a scale (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Physical functioning | Physical health limitations | Emotional health limitations | Energy/Fatigue | Emotional well-being | Social functioning | Pain | General health | |
| Delayed Teriparatide | 65.0 | 68.8 | 72.9 | 59.4 | 70.0 | 65.6 | 59.4 | 67.2 |
| Immediate Teriparatide | 49.3 | 48.2 | 75.0 | 54.5 | 80.7 | 92.9 | 72.9 | 66.1 |
The radiologic indices of fracture healing included (1) cortical continuity on two of four cortices, (2) persistence of alignment, (3) decreased conspicuity of fracture line, and (4) increased callus formation. For each of these indices, healing was graded on a scale of 1 to 4 with 1 = no change (less than 25%), 2 = minimum healing (25-50%), 3 = moderate healing (50-75%), and 4 = complete healing (greater than 75%). A composite score was calculated by summing the subscale scores for the 4 indices. Composite score scale ranged from 4 to 16 with higher scores indicating more complete healing. The primary grading was performed by a radiologist with expertise in musculoskeletal radiology, then independently repeated by a second radiologist, both of whom were blinded to the study allocation. (NCT01705587)
Timeframe: 6, 12 months of treatment
| Intervention | units on a scale (Mean) | |
|---|---|---|
| 6 mo | 12 mo | |
| Delayed Teriparatide | 11.2 | 13.2 |
| Immediate Teriparatide | 12.6 | 15.4 |
The EQ-5D-5L is a generic, multidimensional, health-related, quality-of-life instrument completed on five dimensions to measure health-related quality of life. The profile allowed participants to rate their health state in five health domains: mobility, self-care, usual activities, pain/discomfort, and anxiety/depression using a five level scale (no problems, slight problems, moderate problems, severe problems, and unable to/extreme problems). The responses are used to derive the health state index scores using the United States (US) cross walk algorithm, with scores ranging from -0.11 to 1.0. A higher score indicates better health state. (NCT01709110)
Timeframe: Baseline, 24 Months
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Baseline | 24 Months | |
| Risedronate | 0.72 | 0.76 |
| Teriparatide | 0.70 | 0.74 |
A major non-vertebral fracture is a fracture at any of the following non-vertebral sites hip, radius, humerus, ribs, pelvis, tibia and femur. Non-vertebral fractures were determined by direct questioning at each visit, and confirmed by the site investigators by x-ray, radiology or surgical report. Fractures resulting from a severe trauma such as a traffic collision, a beating, or having been struck by a falling or moving. (NCT01709110)
Timeframe: Baseline through 24 Months
| Intervention | Participants (with at least one event) (Number) |
|---|---|
| Teriparatide | 18 |
| Risedronate | 31 |
Vertebrae were graded as moderate (SQ2), or severe (SQ3) fractures, based on ~25 to 40% (moderate) or ~40% or more (severe) decrease in anterior, central, or posterior vertebral height (T4 through L4). (NCT01709110)
Timeframe: Baseline through 24 Months
| Intervention | Participants (with at least one event) (Number) |
|---|---|
| Teriparatide | 26 |
| Risedronate | 63 |
(NCT01709110)
Timeframe: Baseline through 24 Months
| Intervention | Participants (with at least one event) (Number) |
|---|---|
| Teriparatide | 2 |
| Risedronate | 12 |
"The incidence of new vertebral fractures was assessed by quantitative vertebral morphometry measurements (QM) with qualitative visual semiquantitative grading (SQ) confirmation.~A new vertebral fracture was diagnosed in a vertebra that was non-fractured at the baseline radiological examination. It was defined as a loss of vertebral body height of at least 20% and 4 mm from the baseline radiograph by vertebral QM, based upon placement of six points by a trained, central reader. Any fractures identified by QM were confirmed using SQ: if the vertebral body also had an increase of one or more severity grade, it was considered an incident vertebral fracture." (NCT01709110)
Timeframe: Baseline through 24 Months
| Intervention | Participants (with at least one event) (Number) |
|---|---|
| Teriparatide | 28 |
| Risedronate | 64 |
A non-vertebral fracture is a fracture at any of the following non-vertebral sites: clavicle, scapula, ribs, sternum, sacrum, coccyx, humerus, radius, ulna, carpus, pelvis, hip, femur, patella, tibia, fibula, ankle, calcaneus, tarsus, and metatarsal. Non-vertebral fractures were determined by direct questioning at each visit, and confirmed by the site investigators by x-ray, radiology or surgical report. Fractures resulting from a severe trauma such as a traffic collision, a beating, or having been struck by a falling or moving object were not considered fragility fractures but traumatic fractures. (NCT01709110)
Timeframe: Baseline through 24 Months
| Intervention | Participants (with at least one event) (Number) |
|---|---|
| Teriparatide | 25 |
| Risedronate | 38 |
"A clinical vertebral fracture was defined as a new or worsening vertebral fracture, confirmed by radiography, that was associated with signs and symptoms highly suggestive of a vertebral fracture.~All non-vertebral fractures that occurred and were diagnosed between visits required the confirmation by the site investigators after evaluating the original x-ray film(s), the radiology or surgical report. For clinical vertebral fractures, the final confirmation of the diagnosis required the centralized evaluation by a trained, independent reader." (NCT01709110)
Timeframe: Baseline through 24 Months
| Intervention | Participants (with at least one event) (Number) |
|---|---|
| Teriparatide | 30 |
| Risedronate | 61 |
Traumatic fractures were considered if resulting from a severe trauma such as a traffic collision, a beating, or having been struck by a falling or moving object. (NCT01709110)
Timeframe: Baseline through 24 Months
| Intervention | Participants (with at least one event) (Number) |
|---|---|
| Teriparatide | 40 |
| Risedronate | 57 |
Worsening of a pre-existing fracture was considered if the decrease in vertebral height was at least one severity grade in the semi-quantitative assessment, confirmed by a trained central reader, where vertebrae were graded as normal (SQ0) or as with mild (SQ1), moderate (SQ2), or severe (SQ3) fractures, defined as ~20 to 25% (mild), ~25 to 40% (moderate) or ~40% or more (severe) decrease in anterior, central, or posterior vertebral height (T4 to L4). (NCT01709110)
Timeframe: Baseline through 24 Months
| Intervention | Participants (with at least one event) (Number) |
|---|---|
| Teriparatide | 31 |
| Risedronate | 69 |
Participants rated the worst back pain during the 24 hours preceding the visit at baseline and each post-baseline visit. An 11-point numerical back pain rating scale (rated from 0 = no back pain to 10 = worst possible back pain) was used. (NCT01709110)
Timeframe: Baseline, 24 Months
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Baseline | 24 Months | |
| Risedronate | 4.5 | 3.4 |
| Teriparatide | 4.5 | 3.4 |
(NCT01709110)
Timeframe: Baseline, 24 Months
| Intervention | Centimeter (cm) (Mean) | |
|---|---|---|
| Baseline | 24 Months | |
| Risedronate | 155.0 | 154.5 |
| Teriparatide | 154.7 | 154.3 |
The EQ-5D-5L is a generic, multidimensional, health-related, quality-of-life instrument completed on five dimensions to measure health-related quality of life. The profile allowed participants to rate their health state in five health domains: mobility, self-care, usual activities, pain/discomfort, and anxiety/depression using a five level scale (no problems, slight problems, moderate problems, severe problems, and unable to/extreme problems). The responses are used to derive the health state index scores using the United Kingdom (UK) algorithm, with scores ranging from -0.59 to 1.0. A higher score indicates better health state. (NCT01709110)
Timeframe: Baseline, 24 Months
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Baseline | 24 Months | |
| Risedronate | 0.62 | 0.68 |
| Teriparatide | 0.59 | 0.65 |
The primary outcome was the between-group difference in the teriparatide-induced change in serum c-telopeptide from baseline to week 8. (NCT01750086)
Timeframe: 8 weeks
| Intervention | percentage of change in CTX (Mean) |
|---|---|
| Denosumab 60mg Subcutaneous Injection | -7 |
| Alendronate 70mg Weekly x 8 Weeks | 43 |
ES/BS is the fraction of the entire trabecular surface occupied by resorption bays, including both those with and without osteoclasts. It is an indicator of bone resorption. Percentage = (ES/BS) *100. (NCT01753856)
Timeframe: 3 months post first dose of study drug
| Intervention | percentage of BS (Median) | ||
|---|---|---|---|
| CC (n=31, 35) | EC (n=30, 35) | IC (n=30, 35) | |
| Denosumab | 1.52 | 1.65 | 1.27 |
| Teriparatide | 3.73 | 3.79 | 11.19 |
"The percentage of mineralizing surface where post-treatment DLs in the CC, EC, and PC were classified as remodeling-based or modeling based bone formation based on collagen fiber orientation and whether the underlying reversal line was scalloped or smooth.~Percentage = percentage remodeling- or modeling-based formation units * MS/BS" (NCT01753856)
Timeframe: 3 months post first dose of study drug
| Intervention | percentage of the total formation unit (Median) | |||||
|---|---|---|---|---|---|---|
| Remodeling-Based Bone Formation in CC (n=31, 35) | Modeling-Based Bone Formation in CC (n=31, 35) | Remodeling-Based Bone Formation in EC (n=30, 35) | Modeling-Based Bone Formation in EC (n=30, 35) | Remodeling-Based Bone Formation in PC (n=30, 35) | Modeling-Based Bone Formation in PC (n=30, 35) | |
| Denosumab | 0.87 | 0.09 | 5.42 | 0.00 | 0.00 | 0.00 |
| Teriparatide | 16.67 | 2.06 | 32.92 | 6.58 | 0.00 | 4.69 |
OS is the percentage of the entire trabecular BS that is covered by osteoid. Percentage = (OS / BS) *100. (NCT01753856)
Timeframe: 3 months post first dose of study drug
| Intervention | percentage of BS (Median) | ||
|---|---|---|---|
| CC (n=31, 35) | EC (n=30, 35) | IC (n=30, 35) | |
| Denosumab | 3.46 | 6.95 | 4.34 |
| Teriparatide | 20.51 | 30.85 | 17.81 |
The percentage of overfilled remodeling sites in the CC, EC, and PC were defined as the percentage of observed remodeling units in which the second DL (TET) extended beyond the limits of the scalloped reversal line and into the adjacent, previously unresorbed surface of the bone. Percentage = (overfilled remodeling bone formation unit / total bone formation unit) * 100. (NCT01753856)
Timeframe: 3 months post first dose of study drug
| Intervention | percentage of overfilled remodeling site (Median) | ||
|---|---|---|---|
| CC (n=31, 32) | EC (n=30, 29) | PC (n=29, 5) | |
| Denosumab | 0.00 | 0.00 | 0.00 |
| Teriparatide | 17.74 | 21.98 | 0.00 |
At baseline (18 days prior to randomization / study drug administration), DEM was administered. 22 days prior to the biopsy procedure (biopsy obtained 3 months post first dose of study drug), TET was administered. New bone in the biopsy was seen as the amount of bone between the 2 fluorescently DEM- or TET-labeled lines under a microscope. A DL indicated active bone formation and a SL or NL suggested suppression of bone formation. Percentage = (Single or double TET labels / BS) *100. (NCT01753856)
Timeframe: 3 months post first dose of study drug
| Intervention | percentage of TET label (Median) | |||||||
|---|---|---|---|---|---|---|---|---|
| sLS/BS, in CC (n=31, 35) | dLS/BS, in CC (n=31, 35) | sLS/BS, in EC (n=30, 35) | dLS/BS, in EC (n=30, 35) | sLS/BS, in IC (n=30, 35) | dLS/BS, in IC (n=30, 35) | sLS/BS, in PC (n=30, 35) | dLS/BS, in PC (n=30, 35) | |
| Denosumab | 1.28 | 0.22 | 7.18 | 1.68 | 4.66 | 0.83 | 0.00 | 0.00 |
| Teriparatide | 15.44 | 10.44 | 24.24 | 28.84 | 15.28 | 14.96 | 9.37 | 0.00 |
W.Th is the distance from the cement line to the marrow space of completed trabecular bone packets. (NCT01753856)
Timeframe: 3 months post first dose of study drug
| Intervention | µm (Median) | ||
|---|---|---|---|
| CC (n=31, 35) | EC (n=30, 35) | IC (n=30, 35) | |
| Denosumab | 24.03 | 30.08 | 37.80 |
| Teriparatide | 26.29 | 31.88 | 38.25 |
MS /BS is a measure of the proportion of BS on which new mineralized bone is deposited at the time of DEM or TET labeling, and calculated as the sum of the total extent of double label (DL) plus half the extent of single label (SL) divided by BS. At baseline (18 days prior to randomization / study drug administration), DEM was administered (3 days on, 12 days off, 3 days on). 22 days prior to the biopsy procedure (biopsy obtained 3 months post first dose of study drug), TET was administered (same dosing schedule as DEM). Both DEM and TET temporarily bind to new bone and fluoresce under UV light. New bone in the biopsy was seen as the amount of bone between the 2 fluorescently DEM- or TET-labeled lines under a microscope. A DL indicated active bone formation and a SL or no label (NL) suggested varying degrees of suppression of bone formation. (NCT01753856)
Timeframe: Baseline, 3 months post first dose of study drug
| Intervention | percentage of BS (Median) |
|---|---|
| Teriparatide | 12.43 |
| Denosumab | -2.51 |
OV is the percentage of a given volume of bone tissue that consists of new unmineralized bone matrix (osteoid). Percentage = (OV/BV) *100. (NCT01753856)
Timeframe: 3 months post first dose of study drug
| Intervention | percentage of BV (Median) |
|---|---|
| Teriparatide | 2.58 |
| Denosumab | 0.39 |
Ac.f is the probability of new remodeling cycles initiated on the BS per year. Ac.f = (BFR/BS) / wall thickness. At baseline (18 days prior to randomization / study drug administration), DEM was administered. 22 days prior to the biopsy procedure (biopsy obtained 3 months post first dose of study drug), TET was administered. New bone in the biopsy was seen as the amount of bone between the 2 fluorescently DEM- or TET-labeled lines under a microscope. A DL indicated active bone formation and a SL or NL suggests suppression of bone formation. SL cases were imputed to a value of 0.3 µm/day or counted as missing. NL cases were assigned a value of zero. (NCT01753856)
Timeframe: 3 months post first dose of study drug
| Intervention | new cycles per year (Median) | |||||
|---|---|---|---|---|---|---|
| DL Only, in CC (n=31, 26) | DL and Imputed SL, in CC (n=31, 35) | DL Only, in EC (n=30, 29) | DL and Imputed SL, in EC (n=30, 35) | DL Only, in IC (n=30, 25) | DL and Imputed SL, in IC (n=30, 35) | |
| Denosumab | 0.10 | 0.06 | 0.35 | 0.34 | 0.17 | 0.12 |
| Teriparatide | 1.41 | 1.41 | 2.77 | 2.77 | 1.88 | 1.88 |
Aj.AR is MAR averaged over the entire osteoid surface and in a steady state is an estimate of the mean rate of matrix apposition. At baseline (18 days prior to randomization / study drug administration), DEM was administered. 22 days prior to the biopsy procedure (biopsy obtained 3 months post first dose of study drug), TET was administered. New bone in the biopsy was seen as the amount of bone between the 2 fluorescently DEM- or TET-labeled lines under a microscope. A DL indicated active bone formation and a SL or NL suggested suppression of bone formation. BFR = MAR * (MS/BS). SL cases were imputed to a value of 0.3 µm/day or counted as missing. NL cases were counted as missing. (NCT01753856)
Timeframe: 3 months post first dose of study drug
| Intervention | µm/day (Median) | |||||
|---|---|---|---|---|---|---|
| DL Only, in CC (n=31, 24) | DL and Imputed SL, in CC (n=31, 33) | DL Only, in EC (n=30, 25) | DL and Imputed SL, in EC (n=30, 30) | DL Only, in IC (n=30, 24) | DL and Imputed SL, in IC (n=30, 33) | |
| Denosumab | 0.21 | 0.14 | 0.65 | 0.58 | 0.58 | 0.35 |
| Teriparatide | 0.58 | 0.58 | 0.76 | 0.76 | 1.03 | 1.03 |
The length of TET DLs is a measure of the extent of bone formation in each compartment within individual remodeling units and is measured in mm. At baseline (18 days prior to randomization / study drug administration), DEM was administered. 22 days prior to the biopsy procedure (biopsy obtained 3 months post first dose of study drug), TET was administered. New bone in the biopsy was seen as the amount of bone between the 2 fluorescently DEM- or TET-labeled lines under a microscope. A DL indicated active bone formation. (NCT01753856)
Timeframe: 3 months post first dose of study drug
| Intervention | mm (Mean) | |||
|---|---|---|---|---|
| DL, in CC (n=31, 24) | DL, in EC (n=30, 25) | DL, in IC (n=30, 24) | DL, in PC (n=10, 1) | |
| Denosumab | 0.31 | 0.35 | 0.27 | 0.32 |
| Teriparatide | 0.40 | 0.48 | 0.43 | 0.38 |
BFR/BS is the volume of mineralized bone formed per unit surface of bone per unit of time [mm cubed per mm squared per year (mm³/mm²/year)]. At baseline (18 days prior to randomization / study drug administration), DEM was administered. 22 days prior to the biopsy procedure (biopsy obtained 3 months post first dose of study drug), TET was administered. New bone in the biopsy was seen as the amount of bone between the 2 fluorescently DEM- or TET-labeled lines under a microscope. A DL indicates active bone formation, a SL or NL suggests suppression of bone formation. BFR = MAR * (MS/BS). SL cases were imputed to a value of 0.3 mcm/day or counted as missing. NL cases were assigned a value of zero. (NCT01753856)
Timeframe: Baseline, 3 months post first dose of study drug
| Intervention | mm³/mm²/year (Median) | |||||||
|---|---|---|---|---|---|---|---|---|
| DL Only, in CC (n=30, 26) | DL and Imputed SL, in CC (n=31, 35) | DL Only, in EC (n=29, 28) | DL and Imputed SL, in EC (n=30, 35) | DL Only, in IC (n=30, 25) | DL and Imputed SL, in IC (n=30, 35) | DL Only, in PC (n=6, 16) | DL and Imputed SL, in PC (n=30, 35) | |
| Denosumab | -0.0056 | -0.0055 | -0.0069 | -0.0069 | -0.0184 | -0.0184 | 0.0000 | -0.0005 |
| Teriparatide | 0.0280 | 0.0275 | 0.0509 | 0.0501 | 0.0455 | 0.0455 | 0.0231 | 0.0015 |
BMUs are local groups of osteoblasts and osteoclasts that act in concert to complete a single remodeling cycle. The label length is a measure of the extent of the mineralization front within each BMU in the CC, EC, IC and PC. At baseline (18 days prior to randomization / study drug administration), DEM was administered. 22 days prior to the biopsy procedure (biopsy obtained 3 months post first dose of study drug), TET was administered. New bone in the biopsy was seen as the amount of bone between the 2 fluorescently DEM- or TET-labeled lines under a microscope. A DL indicated active bone formation, and a SL or NL suggested suppression of bone formation. (NCT01753856)
Timeframe: Baseline, 3 months post first dose of study drug
| Intervention | millimeters (mm) (Median) | |||
|---|---|---|---|---|
| CC (n=30, 24) | EC (n=28, 25) | IC (n=30, 24) | PC (n=4, 1) | |
| Denosumab | 0.05 | 0.03 | 0.02 | 0.10 |
| Teriparatide | 0.19 | 0.25 | 0.18 | 0.12 |
MAR is a measure of the linear rate of production of mineralized bone matrix by osteoblasts and is measured by the mean distance between 2 consecutive labels divided by the time interval. At baseline (18 days prior to randomization / study drug administration), DEM was administered. 22 days prior to the biopsy procedure (biopsy obtained 3 months post first dose of study drug), TET was administered. New bone in the biopsy was seen as the amount of bone between the 2 fluorescently DEM- or TET-labeled lines under a microscope. A DL indicated active bone formation, and a SL or NL suggested suppression of bone formation. SL cases were imputed to a value of 0.3 micrometers per day (µm/day) or counted as missing. NL cases were reported as missing. (NCT01753856)
Timeframe: Baseline, 3 months post first dose of study drug
| Intervention | mcm/day (Median) | |||||||
|---|---|---|---|---|---|---|---|---|
| DL Only, in CC (n=30, 24) | DL and Imputed SL, in CC (n=31, 33) | DL Only, in EC (n=28, 25) | DL and Imputed SL, in EC (n=29, 31) | DL Only, in IC (n=30, 24) | DL and Imputed SL, in IC (n=30, 34) | DL Only, in PC (n=4, 1) | DL and Imputed SL, in PC (n=19, 4) | |
| Denosumab | -0.04 | -0.06 | -0.07 | -0.09 | -0.18 | -0.22 | -0.04 | -0.04 |
| Teriparatide | 0.00 | 0.01 | 0.03 | 0.03 | 0.20 | 0.20 | 0.05 | 0.00 |
MS /BS is a measure of the proportion of BS on which new mineralized bone is deposited at the time of DEM or TET labeling and is calculated as the sum of the total extent of DL plus half the extent of SL divided by BS. At baseline (18 days prior to randomization / study drug administration), DEM was administered (3 days on, 12 days off, 3 days on). 22 days prior to the biopsy procedure (biopsy obtained 3 months post first dose of study drug), TET was administered (same dosing schedule as DEM). Both DEM and TET temporarily bind to new bone and fluoresce under UV light. New bone in the biopsy was seen as the amount of bone between the 2 fluorescently DEM- or TET-labeled lines under a microscope. A DL indicated active bone formation and a SL or NL suggested varying degrees of suppression of bone formation. (NCT01753856)
Timeframe: Baseline, 3 months post first dose of study drug
| Intervention | percentage of BS (Median) | ||
|---|---|---|---|
| EC | IC | PC | |
| Denosumab | -2.97 | -6.70 | -0.39 |
| Teriparatide | 26.12 | 9.39 | 2.40 |
MS /BS is a measure of the proportion of BS on which new mineralized bone is deposited at the time of DEM or TET labeling and is calculated as the sum of the total extent of DL plus half the extent of SL divided by BS. At baseline (18 days prior to randomization / study drug administration), DEM was administered (3 days on, 12 days off, 3 days on). 22 days prior to the biopsy procedure (biopsy obtained 3 months post first dose of study drug), TET was administered (same dosing schedule as DEM). Both DEM and TET temporarily bind to new bone and fluoresce under UV light. New bone in the biopsy was seen as the amount of bone between the 2 fluorescently DEM- or TET-labeled lines under a microscope. A DL indicated active bone formation and a SL or NL suggested varying degrees of suppression of bone formation. (NCT01753856)
Timeframe: 3 months post first dose of study drug
| Intervention | percentage of BS (Median) | |||
|---|---|---|---|---|
| CC (n=31, 35) | EC (n=30, 35) | IC (n=30, 35) | PC (n=30, 35) | |
| Denosumab | 0.96 | 5.42 | 3.05 | 0.00 |
| Teriparatide | 18.73 | 39.50 | 21.69 | 4.69 |
(NCT01753856)
Timeframe: 3 months post first dose of study drug
| Intervention | Samples (Number) | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| DL and SL, in CC (n=31, 35) | DL Only, in CC (n=31, 35) | SL Only, in CC (n=31, 35) | No Label, in CC (n=31, 35) | DL and SL, in EC (n=30, 35) | DL Only, in EC (n=30, 35) | SL Only, in EC (n=30, 35) | No Label, in EC (n=30, 35) | DL and SL, in IC (n=30, 35) | DL Only, in IC (n=30, 35) | SL Only, in IC (n=30, 35) | No Label, in IC (n=30, 35) | DL and SL, in PC (n=30, 35) | DL Only, in PC (n=30, 35) | SL Only, in PC (n=30, 35) | No Label, in PC (n=30, 35) | |
| Denosumab | 24 | 0 | 9 | 2 | 25 | 0 | 6 | 4 | 24 | 0 | 10 | 1 | 1 | 0 | 4 | 30 |
| Teriparatide | 31 | 0 | 0 | 0 | 30 | 0 | 0 | 0 | 30 | 0 | 0 | 0 | 10 | 0 | 19 | 1 |
O.Th is a measure of the average thickness of osteoid seams. (NCT01753856)
Timeframe: 3 months post first dose of study drug
| Intervention | micrometers (mcm) (Median) | ||
|---|---|---|---|
| CC (n= 31, 35) | EC (n= 30, 35) | IC (n= 30, 35) | |
| Denosumab | 3.78 | 4.33 | 4.68 |
| Teriparatide | 6.12 | 6.99 | 7.08 |
PTH regulates calcium and phosphate metabolism in bone and kidney, and is typically measured in serum using the intact PTH assay. Percentage = (PTH value at specified time points - PTH value at baseline) / PTH value at baseline * 100. (NCT01753856)
Timeframe: Baseline, 1, 3, and 6 months post first dose of study drug
| Intervention | percentage change in PTH (Median) | ||
|---|---|---|---|
| 1 month (n=28, 34) | 3 months (n=18, 28) | 6 months (n=27, 33) | |
| Denosumab | 72.24 | 46.68 | 30.40 |
| Teriparatide | -26.89 | -32.16 | -40.18 |
CTX is a marker of bone turnover and is a measure of bone resorption. Percentage = (CTX value at specified time points - CTX value at baseline) / (CTX value at baseline) * 100. (NCT01753856)
Timeframe: Baseline, 1, 3, and 6 months post first dose of study drug
| Intervention | percentage change in CTX (Median) | ||
|---|---|---|---|
| 1 month (n=31, 33) | 3 months (n=21, 29) | 6 months (n=29, 33) | |
| Denosumab | -90.70 | -90.77 | -82.50 |
| Teriparatide | 6.09 | 73.04 | 89.13 |
Osteocalcin is a marker of bone turnover and a measure of osteoblast function. Percentage = (osteocalcin value at specified time points - osteocalcin value at baseline) / (osteocalcin value at baseline) * 100. (NCT01753856)
Timeframe: Baseline, 1, 3, and 6 months post first dose of study drug
| Intervention | percentage change in osteocalcin (Median) | ||
|---|---|---|---|
| 1 month (n=31, 33) | 3 months (n=20, 29) | 6 months (n=29, 31) | |
| Denosumab | -6.56 | -45.70 | -50.53 |
| Teriparatide | 90.53 | 123.66 | 187.29 |
P1NP is a marker of bone turnover and is a measure of bone formation. Percentage = (P1NP value at specified time points - P1NP value at baseline) / P1NP value at baseline * 100. (NCT01753856)
Timeframe: Baseline, 1, 3, and 6 months post first dose of study drug
| Intervention | percentage change in P1NP (Median) | ||
|---|---|---|---|
| 1 month (n=33, 34) | 3 months (n=22, 29) | 6 months (n=31, 32) | |
| Denosumab | -11.56 | -66.64 | -68.24 |
| Teriparatide | 134.38 | 213.15 | 284.22 |
In this study, post-treatment DLs in the CC, EC, and PC were classified as remodeling-based or modeling-based bone formations which was determined by whether the underlying reversal line was scalloped or smooth and by the collagen fiber orientation. Percentage = (remodeling-based formation units or modeling-based formation units/ total bone formation units) * 100. (NCT01753856)
Timeframe: 3 months post first dose of study drug
| Intervention | percentage of the total formation unit (Median) | |||||
|---|---|---|---|---|---|---|
| Remodeling-Based Bone Formation in CC (n=31, 32) | Modeling-Based Bone Formation in CC (n=31, 32) | Remodeling-Based Bone Formation in EC (n=30, 29) | Modeling-Based Bone Formation in EC (n=30, 29) | Remodeling-Based Bone Formation in PC (n=29, 5) | Modeling-Based Bone Formation in PC (n=29, 5) | |
| Denosumab | 90.83 | 9.17 | 100.00 | 0.00 | 0.00 | 100.00 |
| Teriparatide | 89.02 | 10.98 | 83.33 | 16.67 | 0.00 | 100.0 |
Integral BMD was measured by quantitative computed tomography (QCT) at the total hip. (NCT01796301)
Timeframe: Baseline and month 6
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Teriparatide | -0.8 |
| Romosozumab | 2.3 |
Bone mineral density was measured by dual-energy X-ray absorptiometry (DXA). (NCT01796301)
Timeframe: Baseline and month 12
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Teriparatide | 5.4 |
| Romosozumab | 9.8 |
Bone mineral density was measured by dual-energy X-ray absorptiometry (DXA). (NCT01796301)
Timeframe: Baseline and month 6
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Teriparatide | 3.5 |
| Romosozumab | 7.2 |
Bone mineral density was measured by dual-energy X-ray absorptiometry (DXA). (NCT01796301)
Timeframe: Baseline and month 6
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Teriparatide | -1.1 |
| Romosozumab | 2.1 |
Bone mineral density was measured by dual-energy X-ray absorptiometry (DXA). (NCT01796301)
Timeframe: Baseline and month 6
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Teriparatide | -0.8 |
| Romosozumab | 2.3 |
Total hip integral BMC was measured using quantitative computed tomography (QCT). (NCT01796301)
Timeframe: Baseline and month 12
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Teriparatide | 0.0 |
| Romosozumab | 3.6 |
Total hip integral BMC was measured using quantitative computed tomography (QCT). (NCT01796301)
Timeframe: Baseline and month 6
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Teriparatide | -0.7 |
| Romosozumab | 2.4 |
Bone mineral density was measured by dual-energy X-ray absorptiometry (DXA). Percent change from baseline through month 12 is the average of the treatment effect at months 6 and 12. (NCT01796301)
Timeframe: Baseline, month 6 and month 12
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Teriparatide | -0.6 |
| Romosozumab | 2.6 |
Integral BMD was measured by quantitative computed tomography (QCT) at the total hip. (NCT01796301)
Timeframe: Baseline and month 12
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Teriparatide | -0.2 |
| Romosozumab | 3.4 |
Bone mineral density was measured by dual-energy X-ray absorptiometry (DXA). (NCT01796301)
Timeframe: Baseline and month 12
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Teriparatide | -0.5 |
| Romosozumab | 2.9 |
Cortical BMD was measured by quantitative computed tomography (QCT) at the total hip. (NCT01796301)
Timeframe: Baseline and month 6
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Teriparatide | -2.7 |
| Romosozumab | 0.7 |
Total hip estimated strength was assessed by finite element analysis (FEA) of QCT scans. (NCT01796301)
Timeframe: Baseline and month 12
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Teriparatide | -0.7 |
| Romosozumab | 2.5 |
Cortical BMD was measured by quantitative computed tomography (QCT) at the total hip. (NCT01796301)
Timeframe: Baseline and month 12
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Teriparatide | -3.6 |
| Romosozumab | 1.1 |
Total hip estimated strength was assessed by finite element analysis (FEA) of QCT scans. (NCT01796301)
Timeframe: Baseline and month 6
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Teriparatide | -1.0 |
| Romosozumab | 2.1 |
Bone mineral density was measured by dual-energy X-ray absorptiometry (DXA). (NCT01796301)
Timeframe: Baseline and month 12
| Intervention | percent change (Least Squares Mean) |
|---|---|
| Teriparatide | -0.2 |
| Romosozumab | 3.2 |
F18 PET/CT scan of foot was performed at baseline and at 12 months following intervention. Main outcome measure was Standardised Uptake value (SUV max) with intervention. A higher score on the scale suggest better outcome (NCT02023411)
Timeframe: 12 months
| Intervention | g/ml (Mean) |
|---|---|
| Teriparatide | 26.1 |
| Placebo | 22.9 |
"Any of the following will be taken as a secondary end point:~The number of participants with~new onset fracture~new onset/progression of deformity~amputation" (NCT02023411)
Timeframe: 12 months
| Intervention | Participants (Count of Participants) |
|---|---|
| Teriparatide | 0 |
| Placebo | 0 |
"The mean percent change in BMD of the femoral neck after 24 months of treatment. Arms/Groups (3) below are divided into the Arms/Groups these subjects were in the parent protocol (NCT01225055) for the 12 month duration of this previous study. These subjects were then enrolled in this 12 month extension study (NCT02025179) and all received Teriparatide and vibration for 12 months as described in the protocol section. The Baseline refers to the baseline at the parent protocol (NCT01225055). The 24 months refers to period after the completion of the 12 month parent protocol (NCT01225055) and this 12 month extension study (NCT02025179)." (NCT02025179)
Timeframe: Baseline to 24 Months
| Intervention | Percent change (Mean) |
|---|---|
| Teriparatide | 2.73 |
| Vibration | -0.06 |
| Teriparatide and Vibration | 4.71 |
"The mean percent change in BMD at the lumbar spine from baseline after 24 months of treatment. Arms/Groups (3) below are divided into the Arms/Groups these subjects were in the parent protocol (NCT01225055) for the 12 month duration of this previous study. These subjects were then enrolled in this 12 month extension study (NCT02025179) and all received Teriparatide and vibration for 12 months as described in the protocol section. The Baseline refers to the baseline at the parent protocol (NCT01225055). The 24 months refers to period after the completion of the 12 month parent protocol (NCT01225055) and this 12 month extension study (NCT02025179)." (NCT02025179)
Timeframe: Baseline to 24 Months
| Intervention | Percent change (Mean) |
|---|---|
| Teriparatide | 14.4 |
| Vibration | 7.05 |
| Teriparatide and Vibration | 8.98 |
"The mean percent change in BMD of the total hip after 24 months of treatment. Arms/Groups (3) below are divided into the Arms/Groups these subjects were in the parent protocol (NCT01225055) for the 12 month duration of this previous study. These subjects were then enrolled in this 12 month extension study (NCT02025179) and all received Teriparatide and vibration for 12 months as described in the protocol section. The Baseline refers to the baseline at the parent protocol (NCT01225055). The 24 months refers to period after the completion of the 12 month parent protocol (NCT01225055) and this 12 month extension study (NCT02025179)." (NCT02025179)
Timeframe: Baseline to 24 months
| Intervention | Percent change (Mean) |
|---|---|
| Teriparatide | 6.73 |
| Vibration | -0.34 |
| Teriparatide and Vibration | 4.24 |
"The mean percent change in Bone-specific alkaline phosphatase from baseline after 24 months of treatment. Arms/Groups (3) below are divided into the Arms/Groups these subjects were in the parent protocol (NCT01225055) for the 12 month duration of this previous study. These subjects were then enrolled in this 12 month extension study (NCT02025179) and all received Teriparatide and vibration for 12 months as described in the protocol section. The Baseline refers to the baseline at the parent protocol (NCT01225055). The 24 months refers to period after the completion of the 12 month parent protocol (NCT01225055) and this 12 month extension study (NCT02025179)." (NCT02025179)
Timeframe: Baseline to 24 Months
| Intervention | Percent change (Mean) |
|---|---|
| Teriparatide | 11.5 |
| Vibration | 12.6 |
| Teriparatide and Vibration | 10.9 |
"The mean percent change in C-terminal telopeptide from baseline after 24 months of treatment. Arms/Groups (3) below are divided into the Arms/Groups these subjects were in the parent protocol (NCT01225055) for the 12 month duration of this previous study. These subjects were then enrolled in this 12 month extension study (NCT02025179) and all received Teriparatide and vibration for 12 months as described in the protocol section. The Baseline refers to the baseline at the parent protocol (NCT01225055). The 24 months refers to period after the completion of the 12 month parent protocol (NCT01225055) and this 12 month extension study (NCT02025179)." (NCT02025179)
Timeframe: Baseline to 24 Months
| Intervention | Percent change (Mean) |
|---|---|
| Teriparatide | -19.8 |
| Vibration | -14.8 |
| Teriparatide and Vibration | -2.12 |
"The mean percent change in Amino-terminal of type 1 collagen from baseline after 24 months of treatment. Arms/Groups (3) below are divided into the Arms/Groups these subjects were in the parent protocol (NCT01225055) for the 12 month duration of this previous study. These subjects were then enrolled in this 12 month extension study (NCT02025179) and all received Teriparatide and vibration for 12 months as described in the protocol section. The Baseline refers to the baseline at the parent protocol (NCT01225055). The 24 months refers to period after the completion of the 12 month parent protocol (NCT01225055) and this 12 month extension study (NCT02025179)." (NCT02025179)
Timeframe: Baseline to 24 Months
| Intervention | Percent change (Mean) |
|---|---|
| Teriparatide | 102 |
| Vibration | 104 |
| Teriparatide and Vibration | 58 |
(NCT02176382)
Timeframe: Baseline and 42 months
| Intervention | percent change in BMD (Mean) |
|---|---|
| Standard Dose Teriparatide | 7.69 |
| High Dose Teriparatide | 12.70 |
Bone markers of bone activity tracked over time for changes.1 Yr. Change in PTH (NCT02440581)
Timeframe: 1 Year (at baseline and one year)
| Intervention | pg/ml (Mean) |
|---|---|
| Control, Low Turnover | 89 |
| Treatment, Low Turnover | 379 |
| Control, High Turnover | -125 |
| Treatment, High Turnover | -240 |
Bone markers of bone activity tracked over time for changes.1 Yr. Change in BSAP (NCT02440581)
Timeframe: 1 year (at baseline and one year)
| Intervention | pg/ml (Mean) |
|---|---|
| Control, Low Turnover | .61 |
| Treatment, Low Turnover | -1.01 |
| Control, High Turnover | -8.92 |
| Treatment, High Turnover | -10.36 |
At one year the investigators will asses bone mass using QCT of the total hip and compare one year changes in bone mass between the treatment and control groups. (NCT02440581)
Timeframe: One Year (at baseline and one year)
| Intervention | g/cm^3 (Mean) |
|---|---|
| Control, Low Turnover | -10.71 |
| Treatment, Low Turnover | 5.72 |
| Control, High Turnover | -3.52 |
| Treatment, High Turnover | .2 |
At one year the investigators will asses differences between the treatment and control groups in changes in Coronary Artery Calcifications by MDCT. 1 Yr. Change in Sqrt CAC Vol. (NCT02440581)
Timeframe: One year (at baseline and one year)
| Intervention | Hounsfield Unit (Mean) |
|---|---|
| Control, Low Turnover | 2.78 |
| Treatment, Low Turnover | 4.48 |
| Control, High Turnover | 4.97 |
| Treatment, High Turnover | 3.47 |
Bone markers of bone activity tracked over time for changes. 1 Yr. Change in FGF-23 (NCT02440581)
Timeframe: 1 Year (at baseline and 1 year)
| Intervention | pg/ml (Mean) |
|---|---|
| Control, Low Turnover | 985 |
| Treatment, Low Turnover | 326 |
| Control, High Turnover | 3337 |
| Treatment, High Turnover | 607 |
More rapidly improved functional outcome using a short physical performance battery to assess lower extremity function (walking speed, repeated chair stands, and balance) at 3 months. Scale is 0 to 100 with higher scores indicating better physical performance. (NCT02972424)
Timeframe: 3 months
| Intervention | score on a scale (Mean) |
|---|---|
| Teriparatide | 74.2 |
| Placebo | 59.9 |
Evidence of cortical bridging based on Focus CT, (NCT02972424)
Timeframe: 3 months
| Intervention | Participants (Count of Participants) |
|---|---|
| Teriparatide | 9 |
| Placebo | 8 |
Pain at 12 months as assessed by the Numeric Rating Scale (0 to 10 where 0 means no pain and 10 worst pain) (NCT02972424)
Timeframe: 12 months
| Intervention | score on a scale (Mean) |
|---|---|
| Teriparatide | 1.5 |
| Placebo | 1.9 |
More rapidly improved functional outcome using a short physical performance battery to assess lower extremity function (walking speed, repeated chair stands, and balance) at 12 months. Scale is 0 to 100 with higher scores indicating better performance. (NCT02972424)
Timeframe: 12 months
| Intervention | score on a scale 0-100 (Mean) |
|---|---|
| Teriparatide | 70.0 |
| Placebo | 64.9 |
"Leads to a faster reduction in pain as assessed by the Numeric Rating Scale of 0 (no pain) to 10 (worst pain).~The mean reduction in pain score from 0 to 3 months is reported. Higher scores mean a greater reduction in pain." (NCT02972424)
Timeframe: 3 months
| Intervention | score on a scale (Mean) |
|---|---|
| Teriparatide | 1.94 |
| Placebo | 2.78 |
"Cancellous bone formation rate at month 3 is calculated from the cancellous (trabecular) compartment of the iliac crest bone biopsy specimens.~Bone formation rate (BFR/BS, mm3/mm2/day): amount of new bone formed in unit time per unit of bone surface. It is calculated by multiplying the mineralizing surface/bone surface (MS/BS) by the mineral apposition rate (MAR) - see below for how MS/BS and MAR are calculated.~Mineralizing surface (MS/BS, %): is the percent of bone surface that displays a tetracycline label reflecting active mineralization. It is calculated as the double-labeled surface plus one half of the single-labeled surface and is expressed as a function of total bone surface. It is a measure of the proportion of bone surface upon which new mineralized bone was being deposited during the period of tetracycline labeling.~Mineral apposition rate (MAR mm/day): is the mean distance between the double labels, divided by the time interval between them." (NCT04026256)
Timeframe: 3 months after first dose of study drug
| Intervention | mm3/mm2/day (Mean) |
|---|---|
| Teriparatide Only | 0.13 |
| Denosumab Only | 0.01 |
| Denosumab and Teriparatide | 0.06 |
| Substance | Relationship Strength | Studies | Trials | Classes | Roles |
|---|---|---|---|---|---|
| betaine glycine betaine : The amino acid betaine derived from glycine. | 3.23 | 1 | 0 | amino-acid betaine; glycine derivative | fundamental metabolite |
| bupropion Bupropion: A propiophenone-derived antidepressant and antismoking agent that inhibits the uptake of DOPAMINE.. bupropion : An aromatic ketone that is propiophenone carrying a tert-butylamino group at position 2 and a chloro substituent at position 3 on the phenyl ring. | 3.23 | 1 | 0 | aromatic ketone; monochlorobenzenes; secondary amino compound | antidepressant; environmental contaminant; xenobiotic |
| aminocaproic acid Aminocaproic Acid: An antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties.. 6-aminohexanoic acid : An epsilon-amino acid comprising hexanoic acid carrying an amino substituent at position C-6. Used to control postoperative bleeding, and to treat overdose effects of the thrombolytic agents streptokinase and tissue plasminogen activator. | 3.23 | 1 | 0 | amino acid zwitterion; epsilon-amino acid; omega-amino fatty acid | antifibrinolytic drug; hematologic agent; metabolite |
| niacin Niacin: A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has PELLAGRA-curative, vasodilating, and antilipemic properties.. vitamin B3 : Any member of a group of vitamers that belong to the chemical structural class called pyridines that exhibit biological activity against vitamin B3 deficiency. Vitamin B3 deficiency causes a condition known as pellagra whose symptoms include depression, dermatitis and diarrhea. The vitamers include nicotinic acid and nicotinamide (and their ionized and salt forms).. nicotinic acid : A pyridinemonocarboxylic acid that is pyridine in which the hydrogen at position 3 is replaced by a carboxy group. | 3.23 | 1 | 0 | pyridine alkaloid; pyridinemonocarboxylic acid; vitamin B3 | antidote; antilipemic drug; EC 3.5.1.19 (nicotinamidase) inhibitor; Escherichia coli metabolite; human urinary metabolite; metabolite; mouse metabolite; plant metabolite; vasodilator agent |
| pyrazinamide pyrazinecarboxamide : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of pyrazinoic acid (pyrazine-2-carboxylic acid) with ammonia. A prodrug for pyrazinoic acid, pyrazinecarboxamide is used as part of multidrug regimens for the treatment of tuberculosis. | 3.23 | 1 | 0 | monocarboxylic acid amide; N-acylammonia; pyrazines | antitubercular agent; prodrug |
| pyridoxine 4,5-bis(hydroxymethyl)-2-methylpyridin-3-ol: structure in first source. vitamin B6 : Any member of the group of pyridines that exhibit biological activity against vitamin B6 deficiency. Vitamin B6 deficiency is associated with microcytic anemia, electroencephalographic abnormalities, dermatitis with cheilosis (scaling on the lips and cracks at the corners of the mouth) and glossitis (swollen tongue), depression and confusion, and weakened immune function. Vitamin B6 consists of the vitamers pyridoxine, pyridoxal, and pyridoxamine and their respective 5'-phosphate esters (and includes their corresponding ionized and salt forms). | 3.23 | 1 | 0 | hydroxymethylpyridine; methylpyridines; monohydroxypyridine; vitamin B6 | cofactor; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| thiamine thiamine(1+) : A primary alcohol that is 1,3-thiazol-3-ium substituted by (4-amino-2-methylpyrimidin-5-yl)methyl, methyl and 2-hydroxyethyl groups at positions 3, 4 and 5, respectively. | 3.23 | 1 | 0 | primary alcohol; vitamin B1 | Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| phenytoin [no description available] | 3.23 | 1 | 0 | imidazolidine-2,4-dione | anticonvulsant; drug allergen; sodium channel blocker; teratogenic agent |
| acebutolol Acebutolol: A cardioselective beta-1 adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm, as well as weak inherent sympathomimetic action.. acebutolol : An ether that is the 2-acetyl-4-(butanoylamino)phenyl ether of the primary hydroxy group of 3-(propan-2-ylamino)propane-1,2-diol. | 3.23 | 1 | 0 | aromatic amide; ethanolamines; ether; monocarboxylic acid amide; propanolamine; secondary amino compound | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; sympathomimetic agent |
| acetaminophen Acetaminophen: Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage.. paracetamol : A member of the class of phenols that is 4-aminophenol in which one of the hydrogens attached to the amino group has been replaced by an acetyl group. | 3.23 | 1 | 0 | acetamides; phenols | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; cyclooxygenase 3 inhibitor; environmental contaminant; ferroptosis inducer; geroprotector; hepatotoxic agent; human blood serum metabolite; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| acetazolamide Acetazolamide: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337) | 3.23 | 1 | 0 | monocarboxylic acid amide; sulfonamide; thiadiazoles | anticonvulsant; diuretic; EC 4.2.1.1 (carbonic anhydrase) inhibitor |
| acetohydroxamic acid acetohydroxamic acid: urease inhibitor. oxime : Compounds of structure R2C=NOH derived from condensation of aldehydes or ketones with hydroxylamine. Oximes from aldehydes may be called aldoximes; those from ketones may be called ketoximes.. N-hydroxyacetimidic acid : A carbohydroximic acid consisting of acetimidic acid having a hydroxy group attached to the imide nitrogen.. acetohydroxamic acid : A member of the class of acetohydroxamic acids that is acetamide in which one of the amino hydrogens has been replaced by a hydroxy group. | 3.23 | 1 | 0 | acetohydroxamic acids; carbohydroximic acid | algal metabolite; EC 3.5.1.5 (urease) inhibitor |
| alaproclate alaproclate: specific 5-hydroxytryptamine uptake inhibitors; RN given refers to (DL)-isomer | 3.23 | 1 | 0 | alpha-amino acid ester | |
| albendazole [no description available] | 3.23 | 1 | 0 | aryl sulfide; benzimidazoles; benzimidazolylcarbamate fungicide; carbamate ester | anthelminthic drug; microtubule-destabilising agent; tubulin modulator |
| albuterol Albuterol: A short-acting beta-2 adrenergic agonist that is primarily used as a bronchodilator agent to treat ASTHMA. Albuterol is prepared as a racemic mixture of R(-) and S(+) stereoisomers. The stereospecific preparation of R(-) isomer of albuterol is referred to as levalbuterol.. albuterol : A member of the class of phenylethanolamines that is 4-(2-amino-1-hydroxyethyl)-2-(hydroxymethyl)phenol having a tert-butyl group attached to the nirogen atom. It acts as a beta-adrenergic agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD). | 3.23 | 1 | 0 | phenols; phenylethanolamines; secondary amino compound | beta-adrenergic agonist; bronchodilator agent; environmental contaminant; xenobiotic |
| alendronate alendronic acid : A 1,1-bis(phosphonic acid) that is methanebis(phosphonic acid) in which the two methylene hydrogens are replaced by hydroxy and 3-aminopropyl groups. | 3.23 | 1 | 0 | 1,1-bis(phosphonic acid); primary amino compound | bone density conservation agent; EC 2.5.1.1 (dimethylallyltranstransferase) inhibitor |
| alfuzosin alfuzosin: structure given in first source | 3.23 | 1 | 0 | monocarboxylic acid amide; quinazolines; tetrahydrofuranol | alpha-adrenergic antagonist; antihypertensive agent; antineoplastic agent |
| alosetron alosetron : A pyrido[4,3-b]indole compound having a 5-methyl-1H-imidazol-4-ylmethyl group at the 2-position. | 3.23 | 1 | 0 | imidazoles; pyridoindole | antiemetic; gastrointestinal drug; serotonergic antagonist |
| alprazolam Alprazolam: A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238). alprazolam : A member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug. | 3.23 | 1 | 0 | organochlorine compound; triazolobenzodiazepine | anticonvulsant; anxiolytic drug; GABA agonist; muscle relaxant; sedative; xenobiotic |
| altretamine Altretamine: A hexamethyl-2,4,6-triamine derivative of 1,3,5-triazine. | 3.23 | 1 | 0 | triamino-1,3,5-triazine | |
| am 251 AM 251: an analog of SR141716A; structure given in first source. AM-251 : A carbohydrazide obtained by formal condensation of the carboxy group of 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid with the amino group of 1-aminopiperidine. An antagonist at the CB1 cannabinoid receptor. | 3.15 | 1 | 0 | amidopiperidine; carbohydrazide; dichlorobenzene; organoiodine compound; pyrazoles | antidepressant; antineoplastic agent; apoptosis inducer; CB1 receptor antagonist |
| amantadine amant: an antiviral compound consisting of an adamantane derivative chemically linked to a water-solube polyanioic matrix; structure in first source | 3.23 | 1 | 0 | adamantanes; primary aliphatic amine | analgesic; antiparkinson drug; antiviral drug; dopaminergic agent; NMDA receptor antagonist; non-narcotic analgesic |
| ambenonium ambenonium : A symmetrical oxalamide-based bis-quaternary ammonium ion having ethyl and 2-chlorobenzyl groups attached to the nitrogens. | 3.23 | 1 | 0 | quaternary ammonium ion | EC 3.1.1.8 (cholinesterase) inhibitor |
| diatrizoic acid Diatrizoate: A commonly used x-ray contrast medium. As DIATRIZOATE MEGLUMINE and as Diatrizoate sodium, it is used for gastrointestinal studies, angiography, and urography.. amidotrizoic acid : A member of the class of benzoic acids that is benzoic acid having iodo substituents at the 2-, 4- and 6-positions and acetamido substituents at the 3- and 5-positions. It is used, mainly as its N-methylglucamine and sodium salts, as an X-ray contrast medium in gastrointestinal studies, angiography, and urography. | 3.23 | 1 | 0 | acetamides; benzoic acids; organoiodine compound | environmental contaminant; radioopaque medium; xenobiotic |
| amifostine anhydrous Amifostine: A phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia.. amifostine : An organic thiophosphate that is the S-phospho derivative of 2-[(3-aminopropyl)amino]ethanethiol. A prodrug for the free thiol, WR-1065, which is used as a cytoprotectant in cancer chemotherapy and radiotherapy. | 3.23 | 1 | 0 | diamine; organic thiophosphate | antioxidant; prodrug; radiation protective agent |
| p-aminohippuric acid p-Aminohippuric Acid: The glycine amide of 4-aminobenzoic acid. Its sodium salt is used as a diagnostic aid to measure effective renal plasma flow (ERPF) and excretory capacity.. p-aminohippurate : A hippurate that is the conjugate base of p-aminohippuric acid, arising from deprotonation of the carboxy group.. p-aminohippuric acid : An N-acylglycine that is the 4-amino derivative of hippuric acid; used as a diagnostic agent in the measurement of renal plasma flow. | 3.23 | 1 | 0 | N-acylglycine | Daphnia magna metabolite |
| theophylline [no description available] | 3.23 | 1 | 0 | dimethylxanthine | adenosine receptor antagonist; anti-asthmatic drug; anti-inflammatory agent; bronchodilator agent; drug metabolite; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; fungal metabolite; human blood serum metabolite; immunomodulator; muscle relaxant; vasodilator agent |
| amiodarone Amiodarone: An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.. amiodarone : A member of the class of 1-benzofurans that is 1-benzofuran substituted by a butyl group at position 2 and a 4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl group at position 3. It is a cardiovascular drug used for the treatment of cardiac dysrhythmias. | 3.23 | 1 | 0 | 1-benzofurans; aromatic ketone; organoiodine compound; tertiary amino compound | cardiovascular drug |
| amitriptyline Amitriptyline: Tricyclic antidepressant with anticholinergic and sedative properties. It appears to prevent the re-uptake of norepinephrine and serotonin at nerve terminals, thus potentiating the action of these neurotransmitters. Amitriptyline also appears to antagonize cholinergic and alpha-1 adrenergic responses to bioactive amines.. amitriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(dimethylamino)propylidene group at position 5. | 3.23 | 1 | 0 | carbotricyclic compound; tertiary amine | adrenergic uptake inhibitor; antidepressant; environmental contaminant; tropomyosin-related kinase B receptor agonist; xenobiotic |
| amlodipine Amlodipine: A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.. amlodipine : A fully substituted dialkyl 1,4-dihydropyridine-3,5-dicarboxylate derivative, which is used for the treatment of hypertension, chronic stable angina and confirmed or suspected vasospastic angina. | 3.23 | 1 | 0 | dihydropyridine; ethyl ester; methyl ester; monochlorobenzenes; primary amino compound | antihypertensive agent; calcium channel blocker; vasodilator agent |
| amoxapine Amoxapine: The N-demethylated derivative of the antipsychotic agent LOXAPINE that works by blocking the reuptake of norepinephrine, serotonin, or both; it also blocks dopamine receptors. Amoxapine is used for the treatment of depression.. amoxapine : A dibenzooxazepine compound having a chloro substituent at the 2-position and a piperazin-1-yl group at the 11-position. | 3.23 | 1 | 0 | dibenzooxazepine | adrenergic uptake inhibitor; antidepressant; dopaminergic antagonist; geroprotector; serotonin uptake inhibitor |
| anastrozole [no description available] | 3.23 | 1 | 0 | nitrile; triazoles | antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor |
| aspirin Aspirin: The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5). acetylsalicylate : A benzoate that is the conjugate base of acetylsalicylic acid, arising from deprotonation of the carboxy group.. acetylsalicylic acid : A member of the class of benzoic acids that is salicylic acid in which the hydrogen that is attached to the phenolic hydroxy group has been replaced by an acetoxy group. A non-steroidal anti-inflammatory drug with cyclooxygenase inhibitor activity. | 3.23 | 1 | 0 | benzoic acids; phenyl acetates; salicylates | anticoagulant; antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; EC 1.1.1.188 (prostaglandin-F synthase) inhibitor; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug; plant activator; platelet aggregation inhibitor; prostaglandin antagonist; teratogenic agent |
| atenolol Atenolol: A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.. atenolol : An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent. | 3.23 | 1 | 0 | ethanolamines; monocarboxylic acid amide; propanolamine | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; environmental contaminant; sympatholytic agent; xenobiotic |
| azathioprine Azathioprine: An immunosuppressive agent used in combination with cyclophosphamide and hydroxychloroquine in the treatment of rheumatoid arthritis. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance has been listed as a known carcinogen. (Merck Index, 11th ed). azathioprine : A thiopurine that is 6-mercaptopurine in which the mercapto hydrogen is replaced by a 1-methyl-4-nitroimidazol-5-yl group. It is a prodrug for mercaptopurine and is used as an immunosuppressant, prescribed for the treatment of inflammatory conditions and after organ transplantation and also for treatment of Crohn's didease and MS. | 3.23 | 1 | 0 | aryl sulfide; C-nitro compound; imidazoles; thiopurine | antimetabolite; antineoplastic agent; carcinogenic agent; DNA synthesis inhibitor; hepatotoxic agent; immunosuppressive agent; prodrug |
| baclofen [no description available] | 3.23 | 1 | 0 | amino acid zwitterion; gamma-amino acid; monocarboxylic acid; monochlorobenzenes; primary amino compound | central nervous system depressant; GABA agonist; muscle relaxant |
| bendazac bendazac : A monocarboxylic acid that is glycolic acid in which the hydrogen attached to the 2-hydroxy group is replaced by a 1-benzyl-1H-indazol-3-yl group. Although it has anti-inflammatory, antinecrotic, choleretic and antilipidaemic properties and has been used for the treatment of various inflammatory skin disorders, its principal effect is to inhibit the denaturation of proteins. Its lysine salt is used in the management of cataracts. | 3.23 | 1 | 0 | indazoles; monocarboxylic acid | non-steroidal anti-inflammatory drug; radical scavenger |
| bendroflumethiazide Bendroflumethiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. It has been used in the treatment of familial hyperkalemia, hypertension, edema, and urinary tract disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p810). bendroflumethiazide : A sulfonamide consisting of 7-sulfamoyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide in which the hydrogen at position 6 is substituted by a trifluoromethyl group and that at position 3 is substituted by a benzyl group. | 3.23 | 1 | 0 | benzothiadiazine; sulfonamide | antihypertensive agent; diuretic |
| benzbromarone Benzbromarone: Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout.. benzbromarone : 1-Benzofuran substituted at C-2 and C-3 by an ethyl group and a 3,5-dibromo-4-hydroxybenzoyl group respectively. An inhibitor of CYP2C9, it is used as an anti-gout medication. | 3.23 | 1 | 0 | 1-benzofurans; aromatic ketone | uricosuric drug |
| betaxolol [no description available] | 3.23 | 1 | 0 | propanolamine | antihypertensive agent; beta-adrenergic antagonist; sympatholytic agent |
| bethanechol Bethanechol: A slowly hydrolyzing muscarinic agonist with no nicotinic effects. Bethanechol is generally used to increase smooth muscle tone, as in the GI tract following abdominal surgery or in urinary retention in the absence of obstruction. It may cause hypotension, HEART RATE changes, and BRONCHIAL SPASM.. bethanechol : The carbamic acid ester of 2-methylcholine. A slowly hydrolysed muscarinic agonist with no nicotinic effects, it is used as its chloride salt to increase smooth muscle tone, as in the gastrointestinal tract following abdominal surgery, treatment of gastro-oesophageal reflux disease, and as an alternative to catheterisation in the treatment of non-obstructive urinary retention. | 3.23 | 1 | 0 | carbamate ester; quaternary ammonium ion | muscarinic agonist |
| bicalutamide bicalutamide: approved for treatment of advanced prostate cancer. N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide : A member of the class of (trifluoromethyl)benzenes that is 4-amino-2-(trifluoromethyl)benzonitrile in which one of the amino hydrogens is substituted by a 3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanoyl group.. bicalutamide : A racemate comprising of equal amounts of (R)-bicalutamide and (S)-bicalutamide. It is an oral non-steroidal antiandrogen used in the treatment of prostate cancer and hirsutism. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; monocarboxylic acid amide; monofluorobenzenes; nitrile; sulfone; tertiary alcohol | |
| biperiden Biperiden: A muscarinic antagonist that has effects in both the central and peripheral nervous systems. It has been used in the treatment of arteriosclerotic, idiopathic, and postencephalitic parkinsonism. It has also been used to alleviate extrapyramidal symptoms induced by phenothiazine derivatives and reserpine.. biperiden : A member of the class of piperidines that is N-propylpiperidine in which the methyl hydrogens have been replaced by hydroxy, phenyl, and 5-norbornen-2-yl groups. A muscarinic antagonist affecting both the central and peripheral nervous systems, it is used in the treatment of all forms of Parkinson's disease. | 3.23 | 1 | 0 | piperidines; tertiary alcohol; tertiary amino compound | antidote to sarin poisoning; antidyskinesia agent; antiparkinson drug; muscarinic antagonist; parasympatholytic |
| bisacodyl Bisacodyl: A diphenylmethane stimulant laxative used for the treatment of CONSTIPATION and for bowel evacuation. (From Martindale, The Extra Pharmacopoeia, 30th ed, p871) | 3.23 | 1 | 0 | diarylmethane | |
| bisoprolol Bisoprolol: A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS. | 3.23 | 1 | 0 | secondary alcohol; secondary amine | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; sympatholytic agent |
| bumetanide [no description available] | 3.23 | 1 | 0 | amino acid; benzoic acids; sulfonamide | diuretic; EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor |
| buspirone Buspirone: An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.. buspirone : An azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N(4) position. | 3.23 | 1 | 0 | azaspiro compound; N-alkylpiperazine; N-arylpiperazine; organic heteropolycyclic compound; piperidones; pyrimidines | anxiolytic drug; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; sedative; serotonergic agonist |
| busulfan [no description available] | 3.23 | 1 | 0 | methanesulfonate ester | alkylating agent; antineoplastic agent; carcinogenic agent; insect sterilant; teratogenic agent |
| secbutabarbital secbutabarbital: Butabarbital (a synonym for Secbutabarbital) should be distinguished from Butobarbital | 3.23 | 1 | 0 | barbiturates | |
| caffeine [no description available] | 3.23 | 1 | 0 | purine alkaloid; trimethylxanthine | adenosine A2A receptor antagonist; adenosine receptor antagonist; adjuvant; central nervous system stimulant; diuretic; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; environmental contaminant; food additive; fungal metabolite; geroprotector; human blood serum metabolite; mouse metabolite; mutagen; plant metabolite; psychotropic drug; ryanodine receptor agonist; xenobiotic |
| verapamil Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group. | 3.23 | 1 | 0 | aromatic ether; nitrile; polyether; tertiary amino compound | |
| candesartan candesartan: a nonpeptide angiotensin II receptor antagonist. candesartan : A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension. | 3.23 | 1 | 0 | benzimidazolecarboxylic acid; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| carbamazepine Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.. carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant. | 3.23 | 1 | 0 | dibenzoazepine; ureas | analgesic; anticonvulsant; antimanic drug; drug allergen; EC 3.5.1.98 (histone deacetylase) inhibitor; environmental contaminant; glutamate transporter activator; mitogen; non-narcotic analgesic; sodium channel blocker; xenobiotic |
| carbinoxamine carbinoxamine: Note: tradenames that start with Histex refer to more than one drug. carbinoxamine : An organochlorine compound that is 2-(4-chlorobenzyl)pyridine in which one of the benzylic hydrogens is substituted by 2-(dimethylamino)ethoxy group. It is an ethanolamine-type antihistamine, used as its maleate salt for treating hay fever, as well as mild cases of Parkinson's disease. | 3.23 | 1 | 0 | monochlorobenzenes; pyridines; tertiary amino compound | anti-allergic agent; antiparkinson drug; H1-receptor antagonist; muscarinic antagonist |
| carisoprodol Carisoprodol: A centrally acting skeletal muscle relaxant whose mechanism of action is not completely understood but may be related to its sedative actions. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1202). carisoprodol : A carbamate ester that is the mono-N-isopropyl derivative of meprobamate (which is a significant metabolite). Carisoprodol interrupts neuronal communication within the reticular formation and spinal cord, resulting in sedation and alteration in pain perception. It is used as a muscle relaxant in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. | 3.23 | 1 | 0 | carbamate ester | muscle relaxant |
| carvedilol [no description available] | 3.23 | 1 | 0 | carbazoles; secondary alcohol; secondary amino compound | alpha-adrenergic antagonist; antihypertensive agent; beta-adrenergic antagonist; cardiovascular drug; vasodilator agent |
| celecoxib [no description available] | 3.23 | 1 | 0 | organofluorine compound; pyrazoles; sulfonamide; toluenes | cyclooxygenase 2 inhibitor; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| cetirizine Cetirizine: A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.. cetirizine : A member of the class of piperazines that is piperazine in which the hydrogens attached to nitrogen are replaced by a (4-chlorophenyl)(phenyl)methyl and a 2-(carboxymethoxy)ethyl group respectively. | 3.23 | 1 | 0 | ether; monocarboxylic acid; monochlorobenzenes; piperazines | anti-allergic agent; environmental contaminant; H1-receptor antagonist; xenobiotic |
| chlorambucil Chlorambucil: A nitrogen mustard alkylating agent used as antineoplastic for chronic lymphocytic leukemia, Hodgkin's disease, and others. Although it is less toxic than most other nitrogen mustards, it has been listed as a known carcinogen in the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (Merck Index, 11th ed). chlorambucil : A monocarboxylic acid that is butanoic acid substituted at position 4 by a 4-[bis(2-chloroethyl)amino]phenyl group. A chemotherapy drug that can be used in combination with the antibody obinutuzumab for the treatment of chronic lymphocytic leukemia. | 3.23 | 1 | 0 | aromatic amine; monocarboxylic acid; nitrogen mustard; organochlorine compound; tertiary amino compound | alkylating agent; antineoplastic agent; carcinogenic agent; drug allergen; immunosuppressive agent |
| chlorcyclizine chlorcyclizine: was heading 1964-94 (Prov 1964-73); CHLOROCYCLIZINE & HISTACHLORAZINE were see CHLORCYCLIZINE 1977-94; use PIPERAZINES to search CHLORCYCLIZINE 1966-94; histamine H1-blocker used both orally and topically in allergies and also for the prevention of motion sickness | 3.23 | 1 | 0 | diarylmethane | |
| chlordiazepoxide Chlordiazepoxide: An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.. chlordiazepoxide : A benzodiazepine that is 3H-1,4-benzodiazepine 4-oxide substituted by a chloro group at position 7, a phenyl group at position 5 and a methylamino group at position 2. | 3.23 | 1 | 0 | benzodiazepine | |
| chlormezanone Chlormezanone: A non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm.. chlormezanone : A 1,3-thiazine that is 1,3-thiazinan-4-one S,S-dioxide in which a hydrogen at position 2 is substituted by a 4-chlorophenyl group and the hydrogen attached to the nitrogen is substituted by methyl. A non-benzodiazepine muscle relaxant, it was used in the management of anxiety and in the treatment of muscle spasms until being discontinued worldwide by its manufacturer in 1996, due to rare but serious cutaneous reactions. | 3.23 | 1 | 0 | 1,3-thiazine; lactam; monochlorobenzenes; sulfone | antipsychotic agent; anxiolytic drug; muscle relaxant |
| chloroquine Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis. | 3.23 | 1 | 0 | aminoquinoline; organochlorine compound; secondary amino compound; tertiary amino compound | anticoronaviral agent; antimalarial; antirheumatic drug; autophagy inhibitor; dermatologic drug |
| chlorothiazide Chlorothiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p812). thiazide : Heterocyclic compound with sulfur and nitrogen in the ring.. chlorothiazide : 4H-1,2,4-benzothiadiazine 1,1-dioxide in which the hydrogen at position is substituted by chlorine and that at position 7 is substituted by a sulfonamide group. A diuretic, it is used for treatment of oedema and hypertension. | 3.23 | 1 | 0 | benzothiadiazine | antihypertensive agent; diuretic |
| chlorpheniramine Chlorpheniramine: A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than PROMETHAZINE.. chlorphenamine : A tertiary amino compound that is propylamine which is substituted at position 3 by a pyridin-2-yl group and a p-chlorophenyl group and in which the hydrogens attached to the nitrogen are replaced by methyl groups. A histamine H1 antagonist, it is used to relieve the symptoms of hay fever, rhinitis, urticaria, and asthma. | 3.23 | 1 | 0 | monochlorobenzenes; pyridines; tertiary amino compound | anti-allergic agent; antidepressant; antipruritic drug; H1-receptor antagonist; histamine antagonist; serotonin uptake inhibitor |
| chlorpromazine Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup.. chlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety. | 3.23 | 1 | 0 | organochlorine compound; phenothiazines; tertiary amine | anticoronaviral agent; antiemetic; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; phenothiazine antipsychotic drug |
| chlorpropamide Chlorpropamide: A sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277). chlorpropamide : An N-sulfonylurea that is urea in which a hydrogen attached to one of the nitrogens is substituted by 4-chlorobenzenesulfonyl group and a hydrogen attached to the other nitrogen is substituted by propyl group. Chlorpropamide is a hypoglycaemic agent used in the treatment of type 2 (non-insulin-dependent) diabetes mellitus not responding to dietary modification. | 3.23 | 1 | 0 | monochlorobenzenes; N-sulfonylurea | hypoglycemic agent; insulin secretagogue |
| chlorthalidone Chlorthalidone: A benzenesulfonamide-phthalimidine that tautomerizes to a BENZOPHENONES form. It is considered a thiazide-like diuretic. | 3.23 | 1 | 0 | isoindoles; monochlorobenzenes; sulfonamide | |
| chlorzoxazone Chlorzoxazone: A centrally acting central muscle relaxant with sedative properties. It is claimed to inhibit muscle spasm by exerting an effect primarily at the level of the spinal cord and subcortical areas of the brain. (From Martindale, The Extra Pharmacopoea, 30th ed, p1202). chlorzoxazone : A member of the class of 1,3-benzoxazoles that is 1,3-benzoxazol-2-ol in which the hydrogen atom at position 5 is substituted by chlorine. A centrally acting muscle relaxant with sedative properties, it is used for the symptomatic treatment of painful muscle spasm. | 3.23 | 1 | 0 | 1,3-benzoxazoles; heteroaryl hydroxy compound; organochlorine compound | muscle relaxant; sedative |
| cilostazol [no description available] | 3.23 | 1 | 0 | lactam; tetrazoles | anticoagulant; bronchodilator agent; EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor; fibrin modulating drug; neuroprotective agent; platelet aggregation inhibitor; vasodilator agent |
| cimetidine Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.. cimetidine : A member of the class of guanidines that consists of guanidine carrying a methyl substituent at position 1, a cyano group at position 2 and a 2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl group at position 3. It is a H2-receptor antagonist that inhibits the production of acid in stomach. | 3.23 | 1 | 0 | aliphatic sulfide; guanidines; imidazoles; nitrile | adjuvant; analgesic; anti-ulcer drug; H2-receptor antagonist; P450 inhibitor |
| ciprofloxacin Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.. ciprofloxacin : A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively. | 3.23 | 1 | 0 | aminoquinoline; cyclopropanes; fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone; zwitterion | antibacterial drug; antiinfective agent; antimicrobial agent; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; environmental contaminant; topoisomerase IV inhibitor; xenobiotic |
| citalopram Citalopram: A furancarbonitrile that is one of the serotonin uptake inhibitors used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from TARDIVE DYSKINESIA in preference to tricyclic antidepressants, which aggravate dyskinesia.. citalopram : A racemate comprising equimolar amounts of (R)-citalopram and its enantiomer, escitalopram. It is used as an antidepressant, although only escitalopram is active.. 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile : A nitrile that is 1,3-dihydro-2-benzofuran-5-carbonitrile in which one of the hydrogens at position 1 is replaced by a p-fluorophenyl group, while the other is replaced by a 3-(dimethylamino)propyl group. | 3.23 | 1 | 0 | 2-benzofurans; cyclic ether; nitrile; organofluorine compound; tertiary amino compound | |
| clofibrate angiokapsul: contains clofibrate & insoitolnicotinate | 3.23 | 1 | 0 | aromatic ether; ethyl ester; monochlorobenzenes | anticholesteremic drug; antilipemic drug; geroprotector; PPARalpha agonist |
| clomiphene [no description available] | 3.23 | 1 | 0 | tertiary amine | estrogen antagonist; estrogen receptor modulator |
| clomipramine Clomipramine: A tricyclic antidepressant similar to IMIPRAMINE that selectively inhibits the uptake of serotonin in the brain. It is readily absorbed from the gastrointestinal tract and demethylated in the liver to form its primary active metabolite, desmethylclomipramine.. clomipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine which is substituted by chlorine at position 3 and in which the hydrogen attached to the nitrogen is replaced by a 3-(dimethylamino)propyl group. One of the more sedating tricyclic antidepressants, it is used as the hydrochloride salt for the treatment of depression as well as obsessive-compulsive disorder and phobias. | 3.23 | 1 | 0 | dibenzoazepine | anticoronaviral agent; antidepressant; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; serotonergic antagonist; serotonergic drug; serotonin uptake inhibitor |
| clonazepam Clonazepam: An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of GAMMA-AMINOBUTYRIC ACID receptor responses.. clonazepam : 1,3-Dihydro-2H-1,4-benzodiazepin-2-one in which the hydrogens at positions 5 and 7 are substituted by 2-chlorophenyl and nitro groups, respectively. It is used in the treatment of all types of epilepsy and seizures, as well as myoclonus and associated abnormal movements, and panic disorders. However, its use can be limited by the development of tolerance and by sedation. | 3.23 | 1 | 0 | 1,4-benzodiazepinone; monochlorobenzenes | anticonvulsant; anxiolytic drug; GABA modulator |
| clonidine Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.. clonidine (amino form) : A clonidine that is 4,5-dihydro-1H-imidazol-2-amine in which one of the amino hydrogens is replaced by a 2,6-dichlorophenyl group. | 3.23 | 1 | 0 | clonidine; imidazoline | |
| chlorazepate clorazepic acid : A 1,4-benzodiazepinone in which the oxo group is at position 2, and which is substituted at positions 3, 5, and 7 by carboxy, phenyl and chloro groups, respectively. | 3.23 | 1 | 0 | 1,4-benzodiazepinone | anticonvulsant; anxiolytic drug; GABA modulator; prodrug |
| clotrimazole [no description available] | 3.23 | 1 | 0 | conazole antifungal drug; imidazole antifungal drug; imidazoles; monochlorobenzenes | antiinfective agent; environmental contaminant; xenobiotic |
| cyclobenzaprine cyclobenzaprine: RN given refers to parent cpd; Lisseril is synonymous for HCl; structure. cyclobenzaprine : 5-Methylidene-5H-dibenzo[a,d]cycloheptene in which one of the hydrogens of the methylidene group is substituted by a 2-(dimethylamino)ethyl group. A centrally acting skeletal muscle relaxant, it is used as its hydrochloride salt in the symptomatic treatment of painful muscle spasm. | 3.23 | 1 | 0 | carbotricyclic compound | antidepressant; muscle relaxant; tranquilizing drug |
| cyclofenil Cyclofenil: A gonadal stimulant and inducer of ovulation. It is used in the treatment of infertility and amenorrhea, but is thought to be less effective than CLOMIPHENE. | 3.23 | 1 | 0 | organic molecular entity | |
| cyproheptadine Cyproheptadine: A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.. cyproheptadine : The product resulting from the formal oxidative coupling of position 5 of 5H-dibenzo[a,d]cycloheptene with position 4 of 1-methylpiperidine resulting in the formation of a double bond between the two fragments. It is a sedating antihistamine with antimuscarinic and calcium-channel blocking actions. It is used (particularly as the hydrochloride sesquihydrate) for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia. | 3.23 | 1 | 0 | piperidines; tertiary amine | anti-allergic agent; antipruritic drug; gastrointestinal drug; H1-receptor antagonist; serotonergic antagonist |
| dapsone [no description available] | 3.23 | 1 | 0 | substituted aniline; sulfone | anti-inflammatory drug; antiinfective agent; antimalarial; leprostatic drug |
| deferoxamine Deferoxamine: Natural product isolated from Streptomyces pilosus. It forms iron complexes and is used as a chelating agent, particularly in the mesylate form.. desferrioxamine B : An acyclic desferrioxamine that is butanedioic acid in which one of the carboxy groups undergoes formal condensation with the primary amino group of N-(5-aminopentyl)-N-hydroxyacetamide and the second carboxy group undergoes formal condensation with the hydroxyamino group of N(1)-(5-aminopentyl)-N(1)-hydroxy-N(4)-[5-(hydroxyamino)pentyl]butanediamide. It is a siderophore native to Streptomyces pilosus biosynthesised by the DesABCD enzyme cluster as a high affinity Fe(III) chelator. | 3.23 | 1 | 0 | acyclic desferrioxamine | bacterial metabolite; ferroptosis inhibitor; iron chelator; siderophore |
| desipramine Desipramine: A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors.. desipramine : A dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group. | 3.23 | 1 | 0 | dibenzoazepine; secondary amino compound | adrenergic uptake inhibitor; alpha-adrenergic antagonist; antidepressant; cholinergic antagonist; drug allergen; EC 3.1.4.12 (sphingomyelin phosphodiesterase) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; H1-receptor antagonist; serotonin uptake inhibitor |
| amphetamine Amphetamine: A powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l- and the d,l-forms are included here. The l-form has less central nervous system activity but stronger cardiovascular effects. The d-form is DEXTROAMPHETAMINE.. 1-phenylpropan-2-amine : A primary amine that is isopropylamine in which a hydrogen attached to one of the methyl groups has been replaced by a phenyl group.. amphetamine : A racemate comprising equimolar amounts of (R)-amphetamine (also known as levamphetamine or levoamphetamine) and (S)-amphetamine (also known as dexamfetamine or dextroamphetamine. | 3.23 | 1 | 0 | primary amine | |
| diazepam Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5. | 3.23 | 1 | 0 | 1,4-benzodiazepinone; organochlorine compound | anticonvulsant; anxiolytic drug; environmental contaminant; sedative; xenobiotic |
| diazoxide Diazoxide: A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group.. diazoxide : A benzothiadiazine that is the S,S-dioxide of 2H-1,2,4-benzothiadiazine which is substituted at position 3 by a methyl group and at position 7 by chlorine. A peripheral vasodilator, it increases the concentration of glucose in the plasma and inhibits the secretion of insulin by the beta- cells of the pancreas. It is used orally in the management of intractable hypoglycaemia and intravenously in the management of hypertensive emergencies. | 3.23 | 1 | 0 | benzothiadiazine; organochlorine compound; sulfone | antihypertensive agent; beta-adrenergic agonist; bronchodilator agent; cardiotonic drug; diuretic; K-ATP channel agonist; sodium channel blocker; sympathomimetic agent; vasodilator agent |
| diclofenac Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.. diclofenac : A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position. | 3.23 | 1 | 0 | amino acid; aromatic amine; dichlorobenzene; monocarboxylic acid; secondary amino compound | antipyretic; drug allergen; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| dichlorphenamide Dichlorphenamide: A carbonic anhydrase inhibitor that is used in the treatment of glaucoma.. diclofenamide : A sulfonamide that is benzene-1,3-disulfonamide in which the hydrogens at positions 4 and 5 are substituted by chlorine. An oral carbonic anhydrase inhibitor, it partially suppresses the secretion (inflow) of aqueous humor in the eye and so reduces intraocular pressure. It is used for the treatment of glaucoma. | 3.23 | 1 | 0 | dichlorobenzene; sulfonamide | antiglaucoma drug; EC 4.2.1.1 (carbonic anhydrase) inhibitor; ophthalmology drug |
| dicyclomine Dicyclomine: A muscarinic antagonist used as an antispasmodic and in urinary incontinence. It has little effect on glandular secretion or the cardiovascular system. It does have some local anesthetic properties and is used in gastrointestinal, biliary, and urinary tract spasms.. dicyclomine : The ester resulting from the formal condensation of 1-cyclohexylcyclohexanecarboxylic acid with 2-(diethylamino)ethanol. An anticholinergic, it is used as the hydrochloride to treat or prevent spasm in the muscles of the gastrointestinal tract, particularly that associated with irritable bowel syndrome. | 3.23 | 1 | 0 | carboxylic ester; tertiary amine | antispasmodic drug; muscarinic antagonist; parasympatholytic |
| pentetic acid Pentetic Acid: An iron chelating agent with properties like EDETIC ACID. DTPA has also been used as a chelator for other metals, such as plutonium. | 3.23 | 1 | 0 | pentacarboxylic acid | copper chelator |
| diflunisal Diflunisal: A salicylate derivative and anti-inflammatory analgesic with actions and side effects similar to those of ASPIRIN.. diflunisal : An organofluorine compound comprising salicylic acid having a 2,4-difluorophenyl group at the 5-position. | 3.23 | 1 | 0 | monohydroxybenzoic acid; organofluorine compound | non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| dimercaprol Dimercaprol: An anti-gas warfare agent that is effective against Lewisite (dichloro(2-chlorovinyl)arsine) and formerly known as British Anti-Lewisite or BAL. It acts as a chelating agent and is used in the treatment of arsenic, gold, and other heavy metal poisoning.. dimercaprol : A dithiol that is propane-1,2-dithiol in which one of the methyl hydrogens is replaced by a hydroxy group. a chelating agent originally developed during World War II as an experimental antidote against the arsenic-based poison gas Lewisite, it has been used clinically since 1949 for the treatment of poisoning by arsenic, mercury and gold. It can also be used for treatment of poisoning by antimony, bismuth and possibly thallium, and (with sodium calcium edetate) in cases of acute leaad poisoning. Administration is by (painful) intramuscular injection of a suspension of dimercaprol in peanut oil, typically every 4 hours for 2-10 days depending on the toxicity. In the past, dimercaprol was also used for the treatment of Wilson's disease, a severely debilitating genetic disorder in which the body tends to retain copper, with resultant liver and brain injury. | 3.23 | 1 | 0 | dithiol; primary alcohol | chelator |
| diphenhydramine Diphenhydramine: A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects.. diphenhydramine : An ether that is the benzhydryl ether of 2-(dimethylamino)ethanol. It is a H1-receptor antagonist used as a antipruritic and antitussive drug.. antitussive : An agent that suppresses cough. Antitussives have a central or a peripheral action on the cough reflex, or a combination of both. Compare with expectorants, which are considered to increase the volume of secretions in the respiratory tract, so facilitating their removal by ciliary action and coughing, and mucolytics, which decrease the viscosity of mucus, facilitating its removal by ciliary action and expectoration. | 3.23 | 1 | 0 | ether; tertiary amino compound | anti-allergic agent; antidyskinesia agent; antiemetic; antiparkinson drug; antipruritic drug; antitussive; H1-receptor antagonist; local anaesthetic; muscarinic antagonist; oneirogen; sedative |
| dipyridamole Dipyridamole: A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752). dipyridamole : A pyrimidopyrimidine that is 2,2',2'',2'''-(pyrimido[5,4-d]pyrimidine-2,6-diyldinitrilo)tetraethanol substituted by piperidin-1-yl groups at positions 4 and 8 respectively. A vasodilator agent, it inhibits the formation of blood clots. | 3.23 | 1 | 0 | piperidines; pyrimidopyrimidine; tertiary amino compound; tetrol | adenosine phosphodiesterase inhibitor; EC 3.5.4.4 (adenosine deaminase) inhibitor; platelet aggregation inhibitor; vasodilator agent |
| disopyramide Disopyramide: A class I anti-arrhythmic agent (one that interferes directly with the depolarization of the cardiac membrane and thus serves as a membrane-stabilizing agent) with a depressant action on the heart similar to that of guanidine. It also possesses some anticholinergic and local anesthetic properties.. disopyramide : A monocarboxylic acid amide that is butanamide substituted by a diisopropylamino group at position 4, a phenyl group at position 2 and a pyridin-2-yl group at position 2. It is used as a anti-arrhythmia drug. | 3.23 | 1 | 0 | monocarboxylic acid amide; pyridines; tertiary amino compound | anti-arrhythmia drug |
| disulfiram [no description available] | 3.23 | 1 | 0 | organic disulfide; organosulfur acaricide | angiogenesis inhibitor; antineoplastic agent; apoptosis inducer; EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor; EC 3.1.1.1 (carboxylesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; EC 5.99.1.2 (DNA topoisomerase) inhibitor; ferroptosis inducer; fungicide; NF-kappaB inhibitor |
| valproic acid Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem. | 3.23 | 1 | 0 | branched-chain fatty acid; branched-chain saturated fatty acid | anticonvulsant; antimanic drug; EC 3.5.1.98 (histone deacetylase) inhibitor; GABA agent; neuroprotective agent; psychotropic drug; teratogenic agent |
| donepezil Donepezil: An indan and piperidine derivative that acts as a selective and reversible inhibitor of ACETYLCHOLINESTERASE. Donepezil is highly selective for the central nervous system and is used in the management of mild to moderate DEMENTIA in ALZHEIMER DISEASE.. donepezil : A racemate comprising equimolar amounts of (R)- and (S)-donepezil. A centrally acting reversible acetylcholinesterase inhibitor, its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.. 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one : A member of the class of indanones that is 5,6-dimethoxyindan-1-one which is substituted at position 2 by an (N-benzylpiperidin-4-yl)methyl group. | 3.23 | 1 | 0 | aromatic ether; indanones; piperidines; racemate | EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; nootropic agent |
| doxapram Doxapram: A central respiratory stimulant with a brief duration of action. (From Martindale, The Extra Pharmocopoeia, 30th ed, p1225). doxapram : A member of the class of pyrrolidin-2-ones that is N-ethylpyrrolidin-2-one in which both of the hydrogens at the 3 position (adjacent to the carbonyl group) are substituted by phenyl groups, and one of the hydrogens at the 4 position is substituted by a 2-(morpholin-4-yl)ethyl group. A central and respiratory stimulant with a brief duration of action, it is used (generally as the hydrochloride or the hydrochloride hydrate) as a temporary treatment of acute respiratory failure, particularly when superimposed on chronic obstructive pulmonary disease, and of postoperative respiratory depression. It has also been used for treatment of postoperative shivering. | 3.23 | 1 | 0 | morpholines; pyrrolidin-2-ones | central nervous system stimulant |
| doxazosin Doxazosin: A prazosin-related compound that is a selective alpha-1-adrenergic blocker.. doxazosin : A member of the class of quinazolines that is quinazoline substituted by an amino group at position 4, methoxy groups at positions 6 and 7 and a piperazin-1-yl group at position 2 which in turn is substituted by a 2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl group at position 4. An antihypertensive agent, it is used in the treatment of high blood pressure. | 3.23 | 1 | 0 | aromatic amine; benzodioxine; monocarboxylic acid amide; N-acylpiperazine; N-arylpiperazine; quinazolines | alpha-adrenergic antagonist; antihyperplasia drug; antihypertensive agent; antineoplastic agent; vasodilator agent |
| doxepin Doxepin: A dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors.. doxepin : A dibenzooxepine that is 6,11-dihydrodibenzo[b,e]oxepine substituted by a 3-(dimethylamino)propylidene group at position 11. It is used as an antidepressant drug. | 3.23 | 1 | 0 | dibenzooxepine; tertiary amino compound | antidepressant |
| doxylamine Doxylamine: Histamine H1 antagonist with pronounced sedative properties. It is used in allergies and as an antitussive, antiemetic, and hypnotic. Doxylamine has also been administered in veterinary applications and was formerly used in PARKINSONISM. | 3.23 | 1 | 0 | pyridines; tertiary amine | anti-allergic agent; antiemetic; antitussive; cholinergic antagonist; H1-receptor antagonist; histamine antagonist; sedative |
| droperidol Droperidol: A butyrophenone with general properties similar to those of HALOPERIDOL. It is used in conjunction with an opioid analgesic such as FENTANYL to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon. It is also used as a premedicant, as an antiemetic, and for the control of agitation in acute psychoses. (From Martindale, The Extra Pharmacopoeia, 29th ed, p593). droperidol : An organofluorine compound that is haloperidol in which the hydroxy group has been eliminated with the introduction of a double bond in the piperidine ring, and the 4-chlorophenyl group has been replaced by a benzimidazol-2-on-1-yl group. It is used in the management of chemotherapy-induced nausea and vomiting, and in conjunction with an opioid analgesic such as fentanyl to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon. | 3.23 | 1 | 0 | aromatic ketone; benzimidazoles; organofluorine compound | anaesthesia adjuvant; antiemetic; dopaminergic antagonist; first generation antipsychotic |
| dyphylline Dyphylline: A THEOPHYLLINE derivative with broncho- and vasodilator properties. It is used in the treatment of asthma, cardiac dyspnea, and bronchitis.. dyphylline : An oxopurine that is theophylline bearing a 2,3-dihydroxypropyl group at the 7 position. It has broncho- and vasodilator properties, and is used in the treatment of asthma, cardiac dyspnea, and bronchitis. It is also an ingredient in preparations that have been promoted for coughs. | 3.23 | 1 | 0 | oxopurine; propane-1,2-diols | bronchodilator agent; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; muscle relaxant; vasodilator agent |
| edrophonium Edrophonium: A rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles.. edrophonium : A quaternary ammonium ion that is N-ethyl-N,N-dimethylanilinium in which one of the meta positions is substituted by a hydroxy group. It is a reversible inhibitor of cholinesterase, with a rapid onset (30-60 seconds after injection) but a short duration of action (5-15 minutes). The chloride salt is used in myasthenia gravis both diagnostically and to distinguish between under- or over-treatment with other anticholinesterases. It has also been used for the reversal of neuromuscular blockade in anaesthesia, and for the management of poisoning due to tetrodotoxin, a neuromuscular blocking toxin found in puffer fish and other marine animals. | 3.23 | 1 | 0 | phenols; quaternary ammonium ion | antidote; diagnostic agent; EC 3.1.1.8 (cholinesterase) inhibitor |
| estazolam Estazolam: A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than DIAZEPAM or NITRAZEPAM.. estazolam : A triazolo[4,3-a][1,4]benzodiazepine having a phenyl group at position 6 and a chloro substituent at position 8. A short-acting benzodiazepine with general properties similar to diazepam, it is given by mouth as a hypnotic in the short-term management of insomnia. | 3.23 | 1 | 0 | triazoles; triazolobenzodiazepine | anticonvulsant; anxiolytic drug; GABA modulator |
| ethacrynic acid Ethacrynic Acid: A compound that inhibits symport of sodium, potassium, and chloride primarily in the ascending limb of Henle, but also in the proximal and distal tubules. This pharmacological action results in excretion of these ions, increased urinary output, and reduction in extracellular fluid. This compound has been classified as a loop or high ceiling diuretic.. etacrynic acid : An aromatic ether that is phenoxyacetic acid in which the phenyl ring is substituted by chlorines at positions 2 and 3, and by a 2-methylidenebutanoyl group at position 4. It is a loop diuretic used to treat high blood pressure resulting from diseases such as congestive heart failure, liver failure, and kidney failure. It is also a glutathione S-transferase (EC 2.5.1.18) inhibitor. | 3.23 | 1 | 0 | aromatic ether; aromatic ketone; dichlorobenzene; monocarboxylic acid | EC 2.5.1.18 (glutathione transferase) inhibitor; ion transport inhibitor; loop diuretic |
| ethosuximide Ethosuximide: An anticonvulsant especially useful in the treatment of absence seizures unaccompanied by other types of seizures.. ethosuximide : A dicarboximide that is pyrrolidine-2,5-dione in which the hydrogens at position 3 are substituted by one methyl and one ethyl group. An antiepileptic, it is used in the treatment of absence seizures and may be used for myoclonic seizures, but is ineffective against tonic-clonic seizures. | 3.23 | 1 | 0 | dicarboximide; pyrrolidinone | anticonvulsant; geroprotector; T-type calcium channel blocker |
| ethotoin ethotoin: was heading 1966-94 (see under HYDANTOINS 1966-90); use HYDANTOINS to search ETHOTOIN 1966-94. ethotoin : An imidazolidine-2,4-dione that is hydantoin substituted by ethyl and phenyl at positions 3 and 5, respectively. An antiepileptic, it is less toxic than phenytoin but also less effective. | 3.23 | 1 | 0 | imidazolidine-2,4-dione | anticonvulsant |
| etidronate Etidronic Acid: A diphosphonate which affects calcium metabolism. It inhibits ectopic calcification and slows down bone resorption and bone turnover.. etidronic acid : A 1,1-bis(phosphonic acid) that is (ethane-1,1-diyl)bis(phosphonic acid) having a hydroxy substituent at the 1-position. It inhibits the formation, growth, and dissolution of hydroxyapatite crystals by chemisorption to calcium phosphate surfaces. | 3.23 | 1 | 0 | 1,1-bis(phosphonic acid) | antineoplastic agent; bone density conservation agent; chelator |
| etodolac Etodolac: A non-steroidal anti-inflammatory agent and cyclooxygenase-2 (COX-2) inhibitor with potent analgesic and anti-arthritic properties. It has been shown to be effective in the treatment of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; ANKYLOSING SPONDYLITIS; and in the alleviation of postoperative pain (PAIN, POSTOPERATIVE).. etodolac : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is substituted by a 1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indol-1-yl moiety. A preferential inhibitor of cyclo-oxygenase 2 and non-steroidal anti-inflammatory, it is used for the treatment of rheumatoid arthritis and osteoarthritis, and for the alleviation of postoperative pain. Administered as the racemate, only the (S)-enantiomer is active. | 3.23 | 1 | 0 | monocarboxylic acid; organic heterotricyclic compound | antipyretic; cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| brl 42810 [no description available] | 3.23 | 1 | 0 | 2-aminopurines; acetate ester | antiviral drug; prodrug |
| felbamate Felbamate: A PEGylated phenylcarbamate derivative that acts as an antagonist of NMDA RECEPTORS. It is used as an anticonvulsant, primarily for the treatment of SEIZURES in severe refractory EPILEPSY.. felbamate : The bis(carbamate ester) of 2-phenylpropane-1,3-diol. An anticonvulsant, it is used in the treatment of epilepsy. | 3.23 | 1 | 0 | carbamate ester | anticonvulsant; neuroprotective agent |
| felodipine Felodipine: A dihydropyridine calcium antagonist with positive inotropic effects. It lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels.. felodipine : The mixed (methyl, ethyl) diester of 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid. A calcium-channel blocker, it lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels. It is used in the management of hypertension and angina pectoris. | 3.23 | 1 | 0 | dichlorobenzene; dihydropyridine; ethyl ester; methyl ester | anti-arrhythmia drug; antihypertensive agent; calcium channel blocker; vasodilator agent |
| fenofibrate Pharmavit: a polyvitamin product, comprising vitamins A, D2, B1, B2, B6, C, E, nicotinamide, & calcium pantothene; may be a promising agent for application to human populations exposed to carcinogenic and genetic hazards of ionizing radiation; RN from CHEMLINE | 3.23 | 1 | 0 | aromatic ether; chlorobenzophenone; isopropyl ester; monochlorobenzenes | antilipemic drug; environmental contaminant; geroprotector; xenobiotic |
| fenoldopam Fenoldopam: A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation. | 3.23 | 1 | 0 | benzazepine | alpha-adrenergic agonist; antihypertensive agent; dopamine agonist; dopaminergic antagonist; vasodilator agent |
| fenoprofen Fenoprofen: A propionic acid derivative that is used as a non-steroidal anti-inflammatory agent.. fenoprofen : A monocarboxylic acid that is propanoic acid in which one of the hydrogens at position 2 is substituted by a 3-phenoxyphenyl group. A non-steroidal anti-inflammatory drug, the dihydrate form of the calcium salt is used for the management of mild to moderate pain and for the relief of pain and inflammation associated with disorders such as arthritis. It is pharmacologically similar to aspirin, but causes less gastrointestinal bleeding. | 3.23 | 1 | 0 | monocarboxylic acid | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| fexofenadine fexofenadine: a second generation antihistamine; metabolite of the antihistaminic drug terfenadine; structure in first source; RN refers to HCl. fexofenadine : A piperidine-based anti-histamine compound. | 3.23 | 1 | 0 | piperidines; tertiary amine | anti-allergic agent; H1-receptor antagonist |
| fipexide fipexide: regulates dopaminergic systems at macromolecular level | 3.23 | 1 | 0 | benzodioxoles | |
| flavoxate Flavoxate: A drug that has been used in various urinary syndromes and as an antispasmodic. Its therapeutic usefulness and its mechanism of action are not clear. It may have local anesthetic activity and direct relaxing effects on smooth muscle as well as some activity as a muscarinic antagonist.. flavoxate : A carboxylic ester resulting from the formal condensation of 3-methylflavone-8-carboxylic acid with 2-(1-piperidinyl)ethanol. | 3.23 | 1 | 0 | carboxylic ester; flavones; piperidines; tertiary amino compound | antispasmodic drug; muscarinic antagonist; parasympatholytic |
| flecainide Flecainide: A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial ARRHYTHMIAS and TACHYCARDIAS.. flecainide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid with the primary amino group of piperidin-2-ylmethylamine. An antiarrhythmic agent used (in the form of its acetate salt) to prevent and treat tachyarrhythmia (abnormal fast rhythm of the heart). | 3.23 | 1 | 0 | aromatic ether; monocarboxylic acid amide; organofluorine compound; piperidines | anti-arrhythmia drug |
| fluconazole Fluconazole: Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.. fluconazole : A member of the class of triazoles that is propan-2-ol substituted at position 1 and 3 by 1H-1,2,4-triazol-1-yl groups and at position 2 by a 2,4-difluorophenyl group. It is an antifungal drug used for the treatment of mucosal candidiasis and for systemic infections including systemic candidiasis, coccidioidomycosis, and cryptococcosis. | 3.23 | 1 | 0 | conazole antifungal drug; difluorobenzene; tertiary alcohol; triazole antifungal drug | environmental contaminant; P450 inhibitor; xenobiotic |
| flucytosine Flucytosine: A fluorinated cytosine analog that is used as an antifungal agent.. flucytosine : An organofluorine compound that is cytosine that is substituted at position 5 by a fluorine. A prodrug for the antifungal 5-fluorouracil, it is used for the treatment of systemic fungal infections. | 3.23 | 1 | 0 | aminopyrimidine; nucleoside analogue; organofluorine compound; pyrimidine antifungal drug; pyrimidone | prodrug |
| fluphenazine [no description available] | 3.23 | 1 | 0 | N-alkylpiperazine; organofluorine compound; phenothiazines | anticoronaviral agent; dopaminergic antagonist; phenothiazine antipsychotic drug |
| flumazenil Flumazenil: A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.. flumazenil : An organic heterotricyclic compound that is 5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted at positions 3, 5, 6, and 8 by ethoxycarbonyl, methyl, oxo, and fluoro groups, respectively. It is used as an antidote to benzodiazepine overdose. | 3.23 | 1 | 0 | ethyl ester; imidazobenzodiazepine; organofluorine compound | antidote to benzodiazepine poisoning; GABA antagonist |
| fluorescite fluorescein (acid form) : A xanthene dye that is highly fluorescent and commonly used as a fluorescent tracer. | 3.23 | 1 | 0 | benzoic acids; cyclic ketone; hydroxy monocarboxylic acid; organic heterotricyclic compound; phenols; xanthene dye | fluorescent dye; radioopaque medium |
| fluorouracil Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth. | 3.23 | 1 | 0 | nucleobase analogue; organofluorine compound | antimetabolite; antineoplastic agent; environmental contaminant; immunosuppressive agent; radiosensitizing agent; xenobiotic |
| fluoxetine Fluoxetine: The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.. fluoxetine : A racemate comprising equimolar amounts of (R)- and (S)-fluoxetine. A selective serotonin reuptake inhibitor (SSRI), it is used (generally as the hydrochloride salt) for the treatment of depression (and the depressive phase of bipolar disorder), bullimia nervosa, and obsessive-compulsive disorder.. N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine : An aromatic ether consisting of 4-trifluoromethylphenol in which the hydrogen of the phenolic hydroxy group is replaced by a 3-(methylamino)-1-phenylpropyl group. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; aromatic ether; secondary amino compound | |
| flurazepam Flurazepam: A benzodiazepine derivative used mainly as a hypnotic.. flurazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a 2-(diethylamino)ethyl group, 2-fluorophenyl group and chloro group at positions 1, 5 and 7, respectively. It is a partial agonist of GABAA receptors and used for the treatment of insomnia. | 3.23 | 1 | 0 | 1,4-benzodiazepinone; monofluorobenzenes; organochlorine compound; tertiary amino compound | anticonvulsant; anxiolytic drug; GABAA receptor agonist; sedative |
| flurbiprofen Flurbiprofen: An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.. flurbiprofen : A monocarboxylic acid that is a 2-fluoro-[1,1'-biphenyl-4-yl] moiety linked to C-2 of propionic acid. A non-steroidal anti-inflammatory, analgesic and antipyretic, it is used as a pre-operative anti-miotic as well as orally for arthritis or dental pain. | 3.23 | 1 | 0 | fluorobiphenyl; monocarboxylic acid | antipyretic; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| flutamide Flutamide: An antiandrogen with about the same potency as cyproterone in rodent and canine species. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; monocarboxylic acid amide | androgen antagonist; antineoplastic agent |
| fomepizole Fomepizole: A pyrazole and competitive inhibitor of ALCOHOL DEHYDROGENASE that is used for the treatment of poisoning by ETHYLENE GLYCOL or METHANOL.. fomepizole : A member of the class of pyrazoles that is 1H-pyrazole substituted by a methyl group at position 4. | 3.23 | 1 | 0 | pyrazoles | antidote; EC 1.1.1.1 (alcohol dehydrogenase) inhibitor; protective agent |
| foscarnet Foscarnet: An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.. phosphonoformic acid : Phosphoric acid in which one of the hydroxy groups is replaced by a carboxylic acid group. It is used as the trisodium salt as an antiviral agent in the treatment of cytomegalovirus retinitis (CMV retinitis, an inflamation of the retina that can lead to blindness) and as an alternative to ganciclovir for AIDS patients who require concurrent antiretroviral therapy but are unable to tolerate ganciclovir due to haematological toxicity. | 3.23 | 1 | 0 | carboxylic acid; one-carbon compound; phosphonic acids | antiviral drug; geroprotector; HIV-1 reverse transcriptase inhibitor; sodium-dependent Pi-transporter inhibitor |
| furosemide Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure. | 3.23 | 1 | 0 | chlorobenzoic acid; furans; sulfonamide | environmental contaminant; loop diuretic; xenobiotic |
| gabapentin Gabapentin: A cyclohexane-gamma-aminobutyric acid derivative that is used for the treatment of PARTIAL SEIZURES; NEURALGIA; and RESTLESS LEGS SYNDROME.. gabapentin : A gamma-amino acid that is cyclohexane substituted at position 1 by aminomethyl and carboxymethyl groups. Used for treatment of neuropathic pain and restless legs syndrome. | 3.23 | 1 | 0 | gamma-amino acid | anticonvulsant; calcium channel blocker; environmental contaminant; xenobiotic |
| gemfibrozil [no description available] | 3.23 | 1 | 0 | aromatic ether | antilipemic drug |
| glafenine Glafenine: An anthranilic acid derivative with analgesic properties used for the relief of all types of pain.. glafenine : A carboxylic ester that is 2,3-dihydroxypropyl anthranilate in which the amino group is substituted by a 7-chloroquinolin-4-yl group. A non-steroidal anti-inflammatory drug, glafenine and its hydrochloride salt were used for the relief of all types of pain, but high incidence of anaphylactic reactions resulted in their withdrawal from the market. | 3.23 | 1 | 0 | aminoquinoline; carboxylic ester; glycol; organochlorine compound; secondary amino compound | inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| glimepiride glimepiride: structure given in first source | 3.23 | 1 | 0 | sulfonamide | |
| glipizide Glipizide: An oral hypoglycemic agent which is rapidly absorbed and completely metabolized.. glipizide : An N-sulfonylurea that is glyburide in which the (5-chloro-2-methoxybenzoyl group is replaced by a (5-methylpyrazin-2-yl)carbonyl group. An oral hypoglycemic agent, it is used in the treatment of type 2 diabetes mellitus. | 3.23 | 1 | 0 | aromatic amide; monocarboxylic acid amide; N-sulfonylurea; pyrazines | EC 2.7.1.33 (pantothenate kinase) inhibitor; hypoglycemic agent; insulin secretagogue |
| glyburide Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide. glyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group. | 3.23 | 1 | 0 | monochlorobenzenes; N-sulfonylurea | anti-arrhythmia drug; EC 2.7.1.33 (pantothenate kinase) inhibitor; EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor; hypoglycemic agent |
| 2-cyclopentyl-2-hydroxy-2-phenylacetic acid (1,1-dimethyl-3-pyrrolidin-1-iumyl) ester [no description available] | 3.23 | 1 | 0 | benzenes | |
| granisetron [no description available] | 3.23 | 1 | 0 | aromatic amide; indazoles | |
| guaifenesin Guaifenesin: An expectorant that also has some muscle relaxing action. It is used in many cough preparations. | 3.23 | 1 | 0 | methoxybenzenes | |
| guanethidine Guanethidine: An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues.. guanethidine : A member of the class of guanidines in which one of the hydrogens of the amino group has been replaced by a 2-azocan-1-ylethyl group.. guanethidine sulfate : A organic sulfate salt composed of two molecules of guanethidine and one of sulfuric acid. | 3.23 | 1 | 0 | azocanes; guanidines | adrenergic antagonist; antihypertensive agent; sympatholytic agent |
| guanfacine Guanfacine: A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS. | 3.23 | 1 | 0 | acetamides | |
| guanidine Guanidine: A strong organic base existing primarily as guanidium ions at physiological pH. It is found in the urine as a normal product of protein metabolism. It is also used in laboratory research as a protein denaturant. (From Martindale, the Extra Pharmacopoeia, 30th ed and Merck Index, 12th ed) It is also used in the treatment of myasthenia and as a fluorescent probe in HPLC.. guanidine : An aminocarboxamidine, the parent compound of the guanidines. | 3.23 | 1 | 0 | carboxamidine; guanidines; one-carbon compound | |
| haloperidol Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety. | 3.23 | 1 | 0 | aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol | antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist |
| hydralazine Hydralazine: A direct-acting vasodilator that is used as an antihypertensive agent.. hydralazine : The 1-hydrazino derivative of phthalazine; a direct-acting vasodilator that is used as an antihypertensive agent. | 3.23 | 1 | 0 | azaarene; hydrazines; ortho-fused heteroarene; phthalazines | antihypertensive agent; vasodilator agent |
| hydrochlorothiazide Hydrochlorothiazide: A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It is used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism.. hydrochlorothiazide : A benzothiadiazine that is 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide substituted by a chloro group at position 6 and a sulfonamide at 7. It is diuretic used for the treatment of hypertension and congestive heart failure. | 3.23 | 1 | 0 | benzothiadiazine; organochlorine compound; sulfonamide | antihypertensive agent; diuretic; environmental contaminant; xenobiotic |
| hydroflumethiazide Hydroflumethiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p822). hydroflumethiazide : A benzothiadiazine consisting of a 3,4-dihydro-HH-1,2,4-benzothiadiazine bicyclic system dioxygenated on sulfur and carrying trifluoromethyl and aminosulfonyl groups at positions 6 and 7 respectively. A diuretic with actions and uses similar to those of hydrochlorothiazide. | 3.23 | 1 | 0 | benzothiadiazine; thiazide | antihypertensive agent; diuretic |
| hydroxychloroquine Hydroxychloroquine: A chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa. It inhibits plasmodial heme polymerase. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p970). hydroxychloroquine : An aminoquinoline that is chloroquine in which one of the N-ethyl groups is hydroxylated at position 2. An antimalarial with properties similar to chloroquine that acts against erythrocytic forms of malarial parasites, it is mainly used as the sulfate salt for the treatment of lupus erythematosus, rheumatoid arthritis, and light-sensitive skin eruptions. | 3.23 | 1 | 0 | aminoquinoline; organochlorine compound; primary alcohol; secondary amino compound; tertiary amino compound | anticoronaviral agent; antimalarial; antirheumatic drug; dermatologic drug |
| hydroxyurea [no description available] | 3.23 | 1 | 0 | one-carbon compound; ureas | antimetabolite; antimitotic; antineoplastic agent; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; genotoxin; immunomodulator; radical scavenger; teratogenic agent |
| hydroxyzine Hydroxyzine: A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.. hydroxyzine : A N-alkylpiperazine that is piperzine in which the nitrogens atoms are substituted by 2-(2-hydroxyethoxy)ethyl and (4-chlorophenyl)(phenyl)methyl groups respectively. | 3.23 | 1 | 0 | hydroxyether; monochlorobenzenes; N-alkylpiperazine | anticoronaviral agent; antipruritic drug; anxiolytic drug; dermatologic drug; H1-receptor antagonist |
| ibuprofen Midol: combination of cinnamedrine, phenacetin, aspirin & caffeine | 3.23 | 1 | 0 | monocarboxylic acid | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; environmental contaminant; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug; radical scavenger; xenobiotic |
| phenelzine Phenelzine: One of the MONOAMINE OXIDASE INHIBITORS used to treat DEPRESSION; PHOBIC DISORDERS; and PANIC. | 3.23 | 1 | 0 | primary amine | |
| lidocaine Lidocaine: A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.. lidocaine : The monocarboxylic acid amide resulting from the formal condensation of N,N-diethylglycine with 2,6-dimethylaniline. | 3.23 | 1 | 0 | benzenes; monocarboxylic acid amide; tertiary amino compound | anti-arrhythmia drug; drug allergen; environmental contaminant; local anaesthetic; xenobiotic |
| ifosfamide [no description available] | 3.23 | 1 | 0 | ifosfamides | alkylating agent; antineoplastic agent; environmental contaminant; immunosuppressive agent; xenobiotic |
| imipramine Imipramine: The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group.. imipramine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)propyl group at the nitrogen atom. | 3.23 | 1 | 0 | dibenzoazepine | adrenergic uptake inhibitor; antidepressant; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor |
| amrinone Amrinone: A positive inotropic cardiotonic (CARDIOTONIC AGENTS) with vasodilator properties, phosphodiesterase 3 inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell.. amrinone : A 3,4'-bipyridine substituted at positions 5 and 6 by an amino group and a keto function respectively. A pyridine phosphodiesterase 3 inhibitor, it is a drug that may improve the prognosis in patients with congestive heart failure. | 3.23 | 1 | 0 | bipyridines | EC 3.1.4.* (phosphoric diester hydrolase) inhibitor |
| indapamide Indapamide: A benzamide-sulfonamide-indole derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. indapamide : A sulfonamide formed by condensation of the carboxylic group of 4-chloro-3-sulfamoylbenzoic acid with the amino group of 2-methyl-2,3-dihydro-1H-indol-1-amine. | 3.23 | 1 | 0 | indoles; organochlorine compound; sulfonamide | antihypertensive agent; diuretic |
| indomethacin Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.. indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis. | 3.23 | 1 | 0 | aromatic ether; indole-3-acetic acids; monochlorobenzenes; N-acylindole | analgesic; drug metabolite; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; gout suppressant; non-steroidal anti-inflammatory drug; xenobiotic metabolite; xenobiotic |
| ioversol [no description available] | 3.23 | 1 | 0 | amidobenzoic acid | |
| iproniazid [no description available] | 3.23 | 1 | 0 | carbohydrazide; pyridines | |
| avapro Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. | 3.23 | 1 | 0 | azaspiro compound; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| isocarboxazid Isocarboxazid: An MAO inhibitor that is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It also is useful in the treatment of panic disorder and the phobic disorders. (From AMA, Drug Evaluations Annual, 1994, p311) | 3.23 | 1 | 0 | benzenes | |
| isoniazid Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals.. hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC). | 3.23 | 1 | 0 | carbohydrazide | antitubercular agent; drug allergen |
| isoproterenol Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.. isoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders. | 3.23 | 1 | 0 | catechols; secondary alcohol; secondary amino compound | beta-adrenergic agonist; bronchodilator agent; cardiotonic drug; sympathomimetic agent |
| isoxsuprine Isoxsuprine: A beta-adrenergic agonist that causes direct relaxation of uterine and vascular smooth muscle. Its vasodilating actions are greater on the arteries supplying skeletal muscle than on those supplying skin. It is used in the treatment of peripheral vascular disease and in premature labor. | 3.23 | 1 | 0 | alkylbenzene | |
| isradipine Isradipine: A potent antagonist of CALCIUM CHANNELS that is highly selective for VASCULAR SMOOTH MUSCLE. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure. | 3.23 | 1 | 0 | benzoxadiazole; dihydropyridine; isopropyl ester; methyl ester | |
| itraconazole [no description available] | 3.23 | 1 | 0 | piperazines | |
| ketamine Ketamine: A cyclohexanone derivative used for induction of anesthesia. Its mechanism of action is not well understood, but ketamine can block NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE) and may interact with sigma receptors.. ketamine : A member of the class of cyclohexanones in which one of the hydrogens at position 2 is substituted by a 2-chlorophenyl group, while the other is substituted by a methylamino group. | 3.23 | 1 | 0 | cyclohexanones; monochlorobenzenes; secondary amino compound | analgesic; environmental contaminant; intravenous anaesthetic; neurotoxin; NMDA receptor antagonist; xenobiotic |
| ketoconazole 1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively. | 3.23 | 1 | 0 | dichlorobenzene; dioxolane; ether; imidazoles; N-acylpiperazine; N-arylpiperazine | |
| ketoprofen Ketoprofen: An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It is used in the treatment of rheumatoid arthritis and osteoarthritis.. ketoprofen : An oxo monocarboxylic acid that consists of propionic acid substituted by a 3-benzoylphenyl group at position 2. | 3.23 | 1 | 0 | benzophenones; oxo monocarboxylic acid | antipyretic; drug allergen; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; non-steroidal anti-inflammatory drug; xenobiotic |
| ketorolac Ketorolac: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed). ketorolac : A racemate comprising equimolar amounts of (R)-(+)- and (S)-(-)-5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid. While only the (S)-(-) enantiomer is a COX1 and COX2 inhibitor, the (R)-(+) enantiomer exhibits potent analgesic activity. A non-steroidal anti-inflammatory drug, ketorolac is mainly used (generally as the tromethamine salt) for its potent analgesic properties in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis. It was withdrawn from the market in many countries in 1993 following association with haemorrhage and renal failure.. 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid : A member of the class of pyrrolizines that is 2,3-dihydro-1H-pyrrolizine which is substituted at positions 1 and 5 by carboxy and benzoyl groups, respectively. | 3.23 | 1 | 0 | amino acid; aromatic ketone; monocarboxylic acid; pyrrolizines; racemate | analgesic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| labetalol Labetalol: A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS.. labetalol : A diastereoisomeric mixture of approximately equal amounts of all four possible stereoisomers ((R,S)-labetolol, (S,R)-labetolol, (S,S)-labetalol and (R,R)-labetalol). It is an adrenergic antagonist used to treat high blood pressure.. 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide : A member of the class of benzamides that is benzamide substituted by a hydroxy group at position 2 and by a 1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl group at position 5. | 3.23 | 1 | 0 | benzamides; benzenes; phenols; primary carboxamide; salicylamides; secondary alcohol; secondary amino compound | |
| lamotrigine [no description available] | 3.23 | 1 | 0 | 1,2,4-triazines; dichlorobenzene; primary arylamine | anticonvulsant; antidepressant; antimanic drug; calcium channel blocker; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; excitatory amino acid antagonist; geroprotector; non-narcotic analgesic; xenobiotic |
| lansoprazole Lansoprazole: A 2,2,2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a racemic mixture of (R)- and (S)-isomers. | 3.23 | 1 | 0 | benzimidazoles; pyridines; sulfoxide | anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor |
| leflunomide Leflunomide: An isoxazole derivative that inhibits dihydroorotate dehydrogenase, the fourth enzyme in the pyrimidine biosynthetic pathway. It is used an immunosuppressive agent in the treatment of RHEUMATOID ARTHRITIS and PSORIATIC ARTHRITIS.. leflunomide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-methyl-1,2-oxazole-4-carboxylic acid with the anilino group of 4-(trifluoromethyl)aniline. The prodrug of teriflunomide. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; isoxazoles; monocarboxylic acid amide | antineoplastic agent; antiparasitic agent; EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor; EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor; hepatotoxic agent; immunosuppressive agent; non-steroidal anti-inflammatory drug; prodrug; pyrimidine synthesis inhibitor; tyrosine kinase inhibitor |
| letrozole [no description available] | 3.23 | 1 | 0 | nitrile; triazoles | antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor |
| lomefloxacin lomefloxacin: structure given in first source. lomefloxacin : A fluoroquinolone antibiotic, used (generally as the hydrochloride salt) to treat bacterial infections including bronchitis and urinary tract infections. It is also used to prevent urinary tract infections prior to surgery. | 3.23 | 1 | 0 | fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antimicrobial agent; antitubercular agent; photosensitizing agent |
| lomustine [no description available] | 3.23 | 1 | 0 | N-nitrosoureas; organochlorine compound | alkylating agent; antineoplastic agent |
| loperamide Loperamide: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.. loperamide : A synthetic piperidine derivative, effective against diarrhoea resulting from gastroenteritis or inflammatory bowel disease. | 3.23 | 1 | 0 | monocarboxylic acid amide; monochlorobenzenes; piperidines; tertiary alcohol | anticoronaviral agent; antidiarrhoeal drug; mu-opioid receptor agonist |
| loratadine Loratadine: A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.. loratadine : A benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders. | 3.23 | 1 | 0 | benzocycloheptapyridine; ethyl ester; N-acylpiperidine; organochlorine compound; tertiary carboxamide | anti-allergic agent; cholinergic antagonist; geroprotector; H1-receptor antagonist |
| lorazepam Lorazepam: A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent. | 3.23 | 1 | 0 | benzodiazepine | |
| losartan Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position | 3.23 | 1 | 0 | biphenylyltetrazole; imidazoles | angiotensin receptor antagonist; anti-arrhythmia drug; antihypertensive agent; endothelin receptor antagonist |
| loxapine Loxapine: An antipsychotic agent used in SCHIZOPHRENIA. | 3.23 | 1 | 0 | dibenzooxazepine | antipsychotic agent; dopaminergic antagonist |
| maprotiline Maprotiline: A bridged-ring tetracyclic antidepressant that is both mechanistically and functionally similar to the tricyclic antidepressants, including side effects associated with its use. | 3.23 | 1 | 0 | anthracenes | |
| mebendazole Mebendazole: A benzimidazole that acts by interfering with CARBOHYDRATE METABOLISM and inhibiting polymerization of MICROTUBULES.. mebendazole : A carbamate ester that is methyl 1H-benzimidazol-2-ylcarbamate substituted by a benzoyl group at position 5. | 3.23 | 1 | 0 | aromatic ketone; benzimidazoles; carbamate ester | antinematodal drug; microtubule-destabilising agent; tubulin modulator |
| mecamylamine Mecamylamine: A nicotinic antagonist that is well absorbed from the gastrointestinal tract and crosses the blood-brain barrier. Mecamylamine has been used as a ganglionic blocker in treating hypertension, but, like most ganglionic blockers, is more often used now as a research tool. | 3.23 | 1 | 0 | primary aliphatic amine | |
| mechlorethamine nitrogen mustard : Compounds having two beta-haloalkyl groups bound to a nitrogen atom, as in (X-CH2-CH2)2NR. | 3.23 | 1 | 0 | nitrogen mustard; organochlorine compound | alkylating agent |
| meclizine Meclizine: A histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness. | 3.23 | 1 | 0 | diarylmethane | |
| meclofenamic acid Meclofenamic Acid: A non-steroidal anti-inflammatory agent with antipyretic and antigranulation activities. It also inhibits prostaglandin biosynthesis.. meclofenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,6-dichloro-3-methylphenyl group. A non-steroidal anti-inflammatory drug, it is used as the sodium salt for the treatment of dysmenorrhoea (painful periods), osteoarthritis and rheumatoid arthritis. | 3.23 | 1 | 0 | aminobenzoic acid; organochlorine compound; secondary amino compound | analgesic; anticonvulsant; antineoplastic agent; antipyretic; antirheumatic drug; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-steroidal anti-inflammatory drug |
| mefenamic acid Mefenamic Acid: A non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory, and antipyretic properties. It is an inhibitor of cyclooxygenase.. mefenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,3-dimethylphenyl group. Although classed as a non-steroidal anti-inflammatory drug, its anti-inflammatory properties are considered to be minor. It is used to relieve mild to moderate pain, including headaches, dental pain, osteoarthritis and rheumatoid arthritis. | 3.23 | 1 | 0 | aminobenzoic acid; secondary amino compound | analgesic; antipyretic; antirheumatic drug; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; non-steroidal anti-inflammatory drug; xenobiotic |
| memantine [no description available] | 3.23 | 1 | 0 | adamantanes; primary aliphatic amine | antidepressant; antiparkinson drug; dopaminergic agent; neuroprotective agent; NMDA receptor antagonist |
| mepenzolate mepenzolic acid: anticholinergic, antispasmodic agent; RN given refers to parent cpd; structure | 3.23 | 1 | 0 | diarylmethane | |
| meperidine Meperidine: A narcotic analgesic that can be used for the relief of most types of moderate to severe pain, including postoperative pain and the pain of labor. Prolonged use may lead to dependence of the morphine type; withdrawal symptoms appear more rapidly than with morphine and are of shorter duration.. pethidine : A piperidinecarboxylate ester that is piperidine which is substituted by a methyl group at position 1 and by phenyl and ethoxycarbonyl groups at position 4. It is an analgesic which is used for the treatment of moderate to severe pain, including postoperative pain and labour pain. | 3.23 | 1 | 0 | ethyl ester; piperidinecarboxylate ester; tertiary amino compound | antispasmodic drug; kappa-opioid receptor agonist; mu-opioid receptor agonist; opioid analgesic |
| mephenytoin Mephenytoin: An anticonvulsant effective in tonic-clonic epilepsy (EPILEPSY, TONIC-CLONIC). It may cause blood dyscrasias.. mephenytoin : An imidazolidine-2,4-dione (hydantoin) in which the imidazolidine nucleus carries a methyl group at N-3 and has ethyl and phenyl substituents at C-5. An anticonvulsant, it is no longer available in the USA or the UK but is still studied largely because of its interesting hydroxylation polymorphism. | 3.23 | 1 | 0 | imidazolidine-2,4-dione | anticonvulsant |
| mepivacaine Mepivacaine: A local anesthetic that is chemically related to BUPIVACAINE but pharmacologically related to LIDOCAINE. It is indicated for infiltration, nerve block, and epidural anesthesia. Mepivacaine is effective topically only in large doses and therefore should not be used by this route. (From AMA Drug Evaluations, 1994, p168). mepivacaine : A piperidinecarboxamide in which N-methylpipecolic acid and 2,6-dimethylaniline have combined to form the amide bond. It is used as a local amide-type anaesthetic. | 3.23 | 1 | 0 | piperidinecarboxamide | drug allergen; local anaesthetic |
| meprobamate Meprobamate: A carbamate with hypnotic, sedative, and some muscle relaxant properties, although in therapeutic doses reduction of anxiety rather than a direct effect may be responsible for muscle relaxation. Meprobamate has been reported to have anticonvulsant actions against petit mal seizures, but not against grand mal seizures (which may be exacerbated). It is used in the treatment of ANXIETY DISORDERS, and also for the short-term management of INSOMNIA but has largely been superseded by the BENZODIAZEPINES. (From Martindale, The Extra Pharmacopoeia, 30th ed, p603) | 3.23 | 1 | 0 | organic molecular entity | |
| mesalamine Mesalamine: An anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE. (From Martindale, The Extra Pharmacopoeia, 30th ed). mesalamine : A monohydroxybenzoic acid that is salicylic acid substituted by an amino group at the 5-position. | 3.23 | 1 | 0 | amino acid; aromatic amine; monocarboxylic acid; monohydroxybenzoic acid; phenols | non-steroidal anti-inflammatory drug |
| mesoridazine Mesoridazine: A phenothiazine antipsychotic with effects similar to CHLORPROMAZINE.. mesoridazine : A phenothiazine substituted at position 2 (para to the S atom) by a methylsulfinyl group, and on the nitrogen by a 2-(1-methylpiperidin-2-yl)ethyl group. | 3.23 | 1 | 0 | phenothiazines; sulfoxide; tertiary amino compound | dopaminergic antagonist; first generation antipsychotic |
| metaproterenol Metaproterenol: A beta-2 adrenergic agonist used in the treatment of ASTHMA and BRONCHIAL SPASM.. orciprenaline : A racemate composed of equimolar amounts of (R)- and (S)-orciprenaline. Used (as its sulfate salt) to relax the airway muscles and improve breathing for patients suffering from asthma or bronchitis.. 5-[1-hydroxy-2-(isopropanylamino)ethyl]benzene-1,3-diol : A member of the class of resorcinols bearing an additional 1-hydroxy-2-(isopropanylamino)ethyl substituent at position 5 of resorcinol itself. | 3.23 | 1 | 0 | aralkylamino compound; phenylethanolamines; resorcinols; secondary alcohol; secondary amino compound | |
| metformin Metformin: A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289). metformin : A member of the class of guanidines that is biguanide the carrying two methyl substituents at position 1. | 3.23 | 1 | 0 | guanidines | environmental contaminant; geroprotector; hypoglycemic agent; xenobiotic |
| methadone Methadone: A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3). methadone : A racemate comprising equimolar amounts of dextromethadone and levomethadone. It is a opioid analgesic which is used as a painkiller and as a substitute for heroin in the treatment of heroin addiction.. 6-(dimethylamino)-4,4-diphenylheptan-3-one : A ketone that is heptan-3-one substituted by a dimethylamino group at position 6 and two phenyl groups at position 4. | 3.23 | 1 | 0 | benzenes; diarylmethane; ketone; tertiary amino compound | |
| methazolamide Methazolamide: A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma. | 3.23 | 1 | 0 | sulfonamide; thiadiazoles | |
| methocarbamol Methocarbamol: A centrally acting muscle relaxant whose mode of action has not been established. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1206). methocarbamol : A racemate comprising equimolar amounts of (R)- and (S)-methocarbamol. A centrally acting skeletal muscle relaxant, it is used as an adjunct in the short-term symptomatic treatment of painful muscle spasm. The (R)-enantiomer is more active than the (S)-enantiomer.. 2-hydroxy-3-(2-methoxyphenoxy)propyl carbamate : A carbamate ester that is glycerol in which one of the primary alcohol groups has been converted to its 2-methoxyphenyl ether while the other has been converted to the corresponding carbamate ester. | 3.23 | 1 | 0 | aromatic ether; carbamate ester; secondary alcohol | |
| methoxsalen Methoxsalen: A naturally occurring furocoumarin compound found in several species of plants, including Psoralea corylifolia. It is a photoactive substance that forms DNA ADDUCTS in the presence of ultraviolet A irradiation.. methoxsalen : A member of the class of psoralens that is 7H-furo[3,2-g]chromen-7-one in which the 9 position is substituted by a methoxy group. It is a constituent of the fruits of Ammi majus. Like other psoralens, trioxsalen causes photosensitization of the skin. It is administered topically or orally in conjunction with UV-A for phototherapy treatment of vitiligo and severe psoriasis. | 3.23 | 1 | 0 | aromatic ether; psoralens | antineoplastic agent; cross-linking reagent; dermatologic drug; photosensitizing agent; plant metabolite |
| methyclothiazide Methyclothiazide: A thiazide diuretic with properties similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p825) | 3.23 | 1 | 0 | benzothiadiazine | |
| methylphenidate Methylphenidate: A central nervous system stimulant used most commonly in the treatment of ATTENTION DEFICIT DISORDER in children and for NARCOLEPSY. Its mechanisms appear to be similar to those of DEXTROAMPHETAMINE. The d-isomer of this drug is referred to as DEXMETHYLPHENIDATE HYDROCHLORIDE.. methylphenidate : A racemate comprising equimolar amounts of the two threo isomers of methyl phenyl(piperidin-2-yl)acetate. A central stimulant and indirect-acting sympathomimetic, is used (generally as the hydrochloride salt) in the treatment of hyperactivity disorders in children and for the treatment of narcolepsy.. methyl phenyl(piperidin-2-yl)acetate : A amino acid ester that is methyl phenylacetate in which one of the hydrogens alpha to the carbonyl group is replaced by a piperidin-2-yl group. | 3.23 | 1 | 0 | beta-amino acid ester; methyl ester; piperidines | |
| metoclopramide Metoclopramide: A dopamine D2 antagonist that is used as an antiemetic.. metoclopramide : A member of the class of benzamides resulting from the formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with the primary amino group of N,N-diethylethane-1,2-diamine. | 3.23 | 1 | 0 | benzamides; monochlorobenzenes; substituted aniline; tertiary amino compound | antiemetic; dopaminergic antagonist; environmental contaminant; gastrointestinal drug; xenobiotic |
| metolazone Metolazone: A quinazoline-sulfonamide derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. metolazone : A quinazoline that consists of 1,2,3,4-tetrahydroquinazolin-4-one bearing additional methyl, 2-tolyl, sulfamyl and chloro substituents at positions 2, 3, 6 and 7 respectively. A quinazoline diuretic, with properties similar to thiazide diuretics. | 3.23 | 1 | 0 | organochlorine compound; quinazolines; sulfonamide | antihypertensive agent; diuretic; ion transport inhibitor |
| metoprolol Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.. metoprolol : A propanolamine that is 1-(propan-2-ylamino)propan-2-ol substituted by a 4-(2-methoxyethyl)phenoxy group at position 1. | 3.23 | 1 | 0 | aromatic ether; propanolamine; secondary alcohol; secondary amino compound | antihypertensive agent; beta-adrenergic antagonist; environmental contaminant; geroprotector; xenobiotic |
| metronidazole Metronidazole: A nitroimidazole used to treat AMEBIASIS; VAGINITIS; TRICHOMONAS INFECTIONS; GIARDIASIS; ANAEROBIC BACTERIA; and TREPONEMAL INFECTIONS.. metronidazole : A member of the class of imidazoles substituted at C-1, -2 and -5 with 2-hydroxyethyl, nitro and methyl groups respectively. It has activity against anaerobic bacteria and protozoa, and has a radiosensitising effect on hypoxic tumour cells. It may be given by mouth in tablets, or as the benzoate in an oral suspension. The hydrochloride salt can be used in intravenous infusions. Metronidazole is a prodrug and is selective for anaerobic bacteria due to their ability to intracellularly reduce the nitro group of metronidazole to give nitroso-containing intermediates. These can covalently bind to DNA, disrupting its helical structure, inducing DNA strand breaks and inhibiting bacterial nucleic acid synthesis, ultimately resulting in bacterial cell death. | 3.23 | 1 | 0 | C-nitro compound; imidazoles; primary alcohol | antiamoebic agent; antibacterial drug; antimicrobial agent; antiparasitic agent; antitrichomonal drug; environmental contaminant; prodrug; radiosensitizing agent; xenobiotic |
| metyrapone Metyrapone: An inhibitor of the enzyme STEROID 11-BETA-MONOOXYGENASE. It is used as a test of the feedback hypothalamic-pituitary mechanism in the diagnosis of CUSHING SYNDROME.. metyrapone : An aromatic ketone that is 3,3-dimethylbutan-2-one in which the methyl groups at positions 1 and 4 are replaced by pyridin-3-yl groups. A steroid 11beta-monooxygenase (EC 1.14.15.4) inhibitor, it is used in the diagnosis of adrenal insufficiency. | 3.23 | 1 | 0 | aromatic ketone | antimetabolite; diagnostic agent; EC 1.14.15.4 (steroid 11beta-monooxygenase) inhibitor |
| mexiletine Mexiletine: Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties.. mexiletine : An aromatic ether which is 2,6-dimethylphenyl ether of 2-aminopropan-1-ol. | 3.23 | 1 | 0 | aromatic ether; primary amino compound | anti-arrhythmia drug |
| midazolam Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively. | 3.23 | 1 | 0 | imidazobenzodiazepine; monofluorobenzenes; organochlorine compound | anticonvulsant; antineoplastic agent; anxiolytic drug; apoptosis inducer; central nervous system depressant; GABAA receptor agonist; general anaesthetic; muscle relaxant; sedative |
| midodrine Midodrine: An ethanolamine derivative that is an adrenergic alpha-1 agonist. It is used as a vasoconstrictor agent in the treatment of HYPOTENSION.. midodrine : An aromatic ether that is 1,4-dimethoxybenzene which is substituted at position 2 by a 2-(glycylamino)-1-hydroxyethyl group. A direct-acting sympathomimetic with selective alpha-adrenergic agonist activity, it is used (generally as its hydrochloride salt) as a peripheral vasoconstrictor in the treatment of certain hypotensive states. The main active moiety is its major metabolite, deglymidodrine. | 3.23 | 1 | 0 | amino acid amide; aromatic ether; secondary alcohol | alpha-adrenergic agonist; prodrug; sympathomimetic agent; vasoconstrictor agent |
| milrinone [no description available] | 3.23 | 1 | 0 | bipyridines; nitrile; pyridone | cardiotonic drug; EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor; platelet aggregation inhibitor; vasodilator agent |
| minoxidil Minoxidil: A potent direct-acting peripheral vasodilator (VASODILATOR AGENTS) that reduces peripheral resistance and produces a fall in BLOOD PRESSURE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p371). minoxidil : A pyrimidine N-oxide that is pyrimidine-2,4-diamine 3-oxide substituted by a piperidin-1-yl group at position 6. | 3.23 | 1 | 0 | dialkylarylamine; tertiary amino compound | |
| mirtazapine Mirtazapine: A piperazinoazepine tetracyclic compound that enhances the release of NOREPINEPHRINE and SEROTONIN through blockage of presynaptic ALPHA-2 ADRENERGIC RECEPTORS. It also blocks both 5-HT2 and 5-HT3 serotonin receptors and is a potent HISTAMINE H1 RECEPTOR antagonist. It is used for the treatment of depression, and may also be useful for the treatment of anxiety disorders. | 3.23 | 1 | 0 | benzazepine; tetracyclic antidepressant | alpha-adrenergic antagonist; anxiolytic drug; H1-receptor antagonist; histamine antagonist; oneirogen; serotonergic antagonist |
| mitotane Mitotane: A derivative of the insecticide DICHLORODIPHENYLDICHLOROETHANE that specifically inhibits cells of the adrenal cortex and their production of hormones. It is used to treat adrenocortical tumors and causes CNS damage, but no bone marrow depression. | 3.23 | 1 | 0 | diarylmethane | |
| mitoxantrone Mitoxantrone: An anthracenedione-derived antineoplastic agent.. mitoxantrone : A dihydroxyanthraquinone that is 1,4-dihydroxy-9,10-anthraquinone which is substituted by 6-hydroxy-1,4-diazahexyl groups at positions 5 and 8. | 3.23 | 1 | 0 | dihydroxyanthraquinone | analgesic; antineoplastic agent |
| modafinil Modafinil: A benzhydryl acetamide compound, central nervous system stimulant, and CYP3A4 inducing agent that is used in the treatment of NARCOLEPSY and SLEEP WAKE DISORDERS.. modafinil : A racemate comprising equimolar amounts of armodafinil and (S)-modafinil. A central nervous system stimulant, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. The optical enantiomers of modafinil have similar pharmacological actions in animals.. 2-[(diphenylmethyl)sulfinyl]acetamide : A sulfoxide that is dimethylsulfoxide in which two hydrogens attached to one of the methyl groups are replaced by phenyl groups, while one hydrogen attached to the other methyl group is replaced by a carbamoyl (aminocarbonyl) group. | 3.23 | 1 | 0 | monocarboxylic acid amide; sulfoxide | |
| moxisylyte Moxisylyte: An alpha-adrenergic blocking agent that is used in Raynaud's disease. It is also used locally in the eye to reverse the mydriasis caused by phenylephrine and other sympathomimetic agents. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1312) | 3.23 | 1 | 0 | monoterpenoid | |
| nabumetone Nabumetone: A butanone non-steroidal anti-inflammatory drug and cyclooxygenase-2 (COX2) inhibitor that is used in the management of pain associated with OSTEOARTHRITIS and RHEUMATOID ARTHRITIS.. nabumetone : A methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthylacetic acid, following oral administration. It is shown to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs. | 3.23 | 1 | 0 | methoxynaphthalene; methyl ketone | cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug |
| nadolol [no description available] | 3.23 | 1 | 0 | tetralins | |
| nalidixic acid [no description available] | 3.23 | 1 | 0 | 1,8-naphthyridine derivative; monocarboxylic acid; quinolone antibiotic | antibacterial drug; antimicrobial agent; DNA synthesis inhibitor |
| naratriptan naratriptan: structure given in first source | 3.23 | 1 | 0 | heteroarylpiperidine; sulfonamide; tryptamines | serotonergic agonist; vasoconstrictor agent |
| nefazodone nefazodone: may be useful as an opiate adjunct | 3.23 | 1 | 0 | aromatic ether; monochlorobenzenes; N-alkylpiperazine; N-arylpiperazine; triazoles | alpha-adrenergic antagonist; analgesic; antidepressant; serotonergic antagonist; serotonin uptake inhibitor |
| nevirapine Nevirapine: A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.. nevirapine : A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection. | 3.23 | 1 | 0 | cyclopropanes; dipyridodiazepine | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| nialamide Nialamide: An MAO inhibitor that is used as an antidepressive agent. | 3.23 | 1 | 0 | organonitrogen compound; organooxygen compound | |
| nicardipine Nicardipine: A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.. nicardipine : A racemate comprising equimolar amounts of (R)- and (S)-nicardipine. It is a calcium channel blocker which is used to treat hypertension.. 2-[benzyl(methyl)amino]ethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine substituted by a methyl, {2-[benzyl(methyl)amino]ethoxy}carbonyl, 3-nitrophenyl, methoxycarbonyl and methyl groups at positions 2, 3, 4, 5 and 6, respectively. | 3.23 | 1 | 0 | benzenes; C-nitro compound; diester; dihydropyridine; methyl ester; tertiary amino compound | |
| nifedipine Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure. | 3.23 | 1 | 0 | C-nitro compound; dihydropyridine; methyl ester | calcium channel blocker; human metabolite; tocolytic agent; vasodilator agent |
| nilutamide [no description available] | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; C-nitro compound; imidazolidinone | androgen antagonist; antineoplastic agent |
| nimesulide nimesulide: structure. nimesulide : An aromatic ether having phenyl and 2-methylsulfonamido-5-nitrophenyl as the two aryl groups. | 3.23 | 1 | 0 | aromatic ether; C-nitro compound; sulfonamide | cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| nimodipine Nimodipine: A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure.. nimodipine : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a (2-methoxyethoxy)carbonyl group at position 3, a m-nitrophenyl group at position 4, and an isopropoxycarbonyl group at position 5. An L-type calcium channel blocker, it acts particularly on cerebral circulation, and is used both orally and intravenously for the prevention and treatment of subarachnoid hemorrhage from ruptured intracranial aneurysm. | 3.23 | 1 | 0 | 2-methoxyethyl ester; C-nitro compound; dicarboxylic acids and O-substituted derivatives; diester; dihydropyridine; isopropyl ester | antihypertensive agent; calcium channel blocker; cardiovascular drug; vasodilator agent |
| nisoldipine Nisoldipine: A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.. nisoldipine : A racemate consisting of equimolar amounts of (R)- and (S)-nisoldipine. A calcium channel blocker, it is used in the treatment of hypertension and angina pectoris.. methyl 2-methylpropyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a methoxycarbonyl group at position 3, an o-nitrophenyl group at position 4, and an isobutoxycarbonyl group at position 5. The racemate, a calcium channel blocker, is used in the treatment of hypertension and angina pectoris. | 3.23 | 1 | 0 | C-nitro compound; dicarboxylic acids and O-substituted derivatives; diester; dihydropyridine; methyl ester | |
| nitroglycerin Nitroglycerin: A volatile vasodilator which relieves ANGINA PECTORIS by stimulating GUANYLATE CYCLASE and lowering cytosolic calcium. It is also sometimes used for TOCOLYSIS and explosives.. nitroglycerol : A nitrate ester that is glycerol in which nitro group(s) replace the hydrogen(s) attached to one or more of the hydroxy groups.. nitroglycerin : A nitroglycerol that is glycerol in which the hydrogen atoms of all three hydroxy groups are replaced by nitro groups. It acts as a prodrug, releasing nitric oxide to open blood vessels and so alleviate heart pain. | 3.23 | 1 | 0 | nitroglycerol | explosive; muscle relaxant; nitric oxide donor; prodrug; tocolytic agent; vasodilator agent; xenobiotic |
| nizatidine [no description available] | 3.23 | 1 | 0 | 1,3-thiazoles; C-nitro compound; carboxamidine; organic sulfide; tertiary amino compound | anti-ulcer drug; cholinergic drug; H2-receptor antagonist |
| nomifensine Nomifensine: An isoquinoline derivative that prevents dopamine reuptake into synaptosomes. The maleate was formerly used in the treatment of depression. It was withdrawn worldwide in 1986 due to the risk of acute hemolytic anemia with intravascular hemolysis resulting from its use. In some cases, renal failure also developed. (From Martindale, The Extra Pharmacopoeia, 30th ed, p266). nomifensine : An N-methylated tetrahydroisoquinoline carrying phenyl and amino substituents at positions C-4 and C-8, respectively. | 3.23 | 1 | 0 | isoquinolines | dopamine uptake inhibitor |
| norfloxacin Norfloxacin: A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.. norfloxacin : A quinolinemonocarboxylic acid with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase. | 3.23 | 1 | 0 | fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antibacterial drug; DNA synthesis inhibitor; environmental contaminant; xenobiotic |
| nortriptyline Nortriptyline: A metabolite of AMITRIPTYLINE that is also used as an antidepressive agent. Nortriptyline is used in major depression, dysthymia, and atypical depressions.. nortriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(methylamino)propylidene group at position 5. It is an active metabolite of amitriptyline. | 3.23 | 1 | 0 | organic tricyclic compound; secondary amine | adrenergic uptake inhibitor; analgesic; antidepressant; antineoplastic agent; apoptosis inducer; drug metabolite |
| ofloxacin Ofloxacin: A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.. 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid : An oxazinoquinoline that is 2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinolin-7-one substituted by methyl, carboxy, fluoro, and 4-methylpiperazin-1-yl groups at positions 3, 6, 9, and 10, respectively.. ofloxacin : A racemate comprising equimolar amounts of levofloxacin and dextrofloxacin. It is a synthetic fluoroquinolone antibacterial agent which inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication. | 3.23 | 1 | 0 | 3-oxo monocarboxylic acid; N-arylpiperazine; N-methylpiperazine; organofluorine compound; oxazinoquinoline | |
| omeprazole Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5. | 3.23 | 1 | 0 | aromatic ether; benzimidazoles; pyridines; sulfoxide | |
| ondansetron Ondansetron: A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties. | 3.23 | 1 | 0 | carbazoles | |
| orphenadrine Orphenadrine: A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.. orphenadrine : A tertiary amino compound which is the phenyl-o-tolylmethyl ether of 2-(dimethylamino)ethanol. | 3.23 | 1 | 0 | ether; tertiary amino compound | antidyskinesia agent; antiparkinson drug; H1-receptor antagonist; muscarinic antagonist; muscle relaxant; NMDA receptor antagonist; parasympatholytic |
| oxaprozin Oxaprozin: An oxazole-propionic acid derivative, cyclooxygenase inhibitor, and non-steroidal anti-inflammatory drug that is used in the treatment of pain and inflammation associated with of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; and ARTHRITIS, JUVENILE.. oxaprozin : A monocarboxylic acid that is a propionic acid derivative having a 4,5-diphenyl-1,3-oxazol-2-yl substituent at position 3. It is non-steroidal anti-inflammatory drug commonly used to relieve the pain and inflammatory responses associated with osteoarthritis and rheumatoid arthritis. | 3.23 | 1 | 0 | 1,3-oxazoles; monocarboxylic acid | analgesic; non-steroidal anti-inflammatory drug |
| oxazepam Oxazepam: A benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia.. oxazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a hydroxy group at position 3 and phenyl group at position 5. | 3.23 | 1 | 0 | 1,4-benzodiazepinone; organochlorine compound | anxiolytic drug; environmental contaminant; xenobiotic |
| oxybutynin oxybutynin: RN given refers to parent cpd. oxybutynin : A racemate comprising equimolar amounts of (R)-oxybutynin and esoxybutynin. An antispasmodic used for the treatment of overactive bladder. | 3.23 | 1 | 0 | acetylenic compound; carboxylic ester; racemate; tertiary alcohol; tertiary amino compound | antispasmodic drug; calcium channel blocker; local anaesthetic; muscarinic antagonist; muscle relaxant; parasympatholytic |
| aminosalicylic acid Aminosalicylic Acid: An antitubercular agent often administered in association with ISONIAZID. The sodium salt of the drug is better tolerated than the free acid.. 4-aminosalicylic acid : An aminobenzoic acid that is salicylic acid substituted by an amino group at position 4. | 3.23 | 1 | 0 | aminobenzoic acid; phenols | antitubercular agent |
| pamidronate [no description available] | 3.23 | 1 | 0 | phosphonoacetic acid | |
| pantoprazole Pantoprazole: 2-pyridinylmethylsulfinylbenzimidazole proton pump inhibitor that is used in the treatment of GASTROESOPHAGEAL REFLUX and PEPTIC ULCER.. pantoprazole : A member of the class of benzimidazoles that is 1H-benzimidazole substituted by a difluoromethoxy group at position 5 and a [(3,4-dimethoxypyridin-2-yl)methyl]sulfinyl group at position 2. | 3.23 | 1 | 0 | aromatic ether; benzimidazoles; organofluorine compound; pyridines; sulfoxide | anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor; environmental contaminant; xenobiotic |
| papaverine Papaverine: An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels.. papaverine : A benzylisoquinoline alkaloid that is isoquinoline substituted by methoxy groups at positions 6 and 7 and a 3,4-dimethoxybenzyl group at position 1. It has been isolated from Papaver somniferum. | 3.23 | 1 | 0 | benzylisoquinoline alkaloid; dimethoxybenzene; isoquinolines | antispasmodic drug; vasodilator agent |
| pemoline Pemoline: A central nervous system stimulant used in fatigue and depressive states and to treat hyperkinetic disorders in children.. pemoline : A member of the class of 1,3-oxazoles that is 1,3-oxazol-4(5H)-one which is substituted by an amino group at position 2 and by a phenyl group at position 5. A central nervous system stimulant, it was used to treat hyperactivity disorders in children, but withdrawn from use following reports of serious hepatotoxicity. | 3.23 | 1 | 0 | 1,3-oxazoles | central nervous system stimulant |
| pentamidine Pentamidine: Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.. pentamidine : A diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease. | 3.23 | 1 | 0 | aromatic ether; carboxamidine; diether | anti-inflammatory agent; antifungal agent; calmodulin antagonist; chemokine receptor 5 antagonist; EC 2.3.1.48 (histone acetyltransferase) inhibitor; NMDA receptor antagonist; S100 calcium-binding protein B inhibitor; trypanocidal drug; xenobiotic |
| pentobarbital Pentobarbital: A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236). pentobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and sec-pentyl groups. | 3.23 | 1 | 0 | barbiturates | GABAA receptor agonist |
| pentoxifylline [no description available] | 3.23 | 1 | 0 | oxopurine | |
| perhexiline Perhexiline: 2-(2,2-Dicyclohexylethyl)piperidine. Coronary vasodilator used especially for angina of effort. It may cause neuropathy and hepatitis. | 3.23 | 1 | 0 | piperidines | cardiovascular drug |
| perphenazine Perphenazine: An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.. perphenazine : A phenothiazine derivative in which the phenothiazine tricycle carries a chloro substituent at the 2-position and a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at N-10. | 3.23 | 1 | 0 | N-(2-hydroxyethyl)piperazine; N-alkylpiperazine; organochlorine compound; phenothiazines | antiemetic; dopaminergic antagonist; phenothiazine antipsychotic drug |
| phenobarbital Phenobarbital: A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations.. phenobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and phenyl groups. | 3.23 | 1 | 0 | barbiturates | anticonvulsant; drug allergen; excitatory amino acid antagonist; sedative |
| phenoxybenzamine Phenoxybenzamine: An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator. | 3.23 | 1 | 0 | aromatic amine | |
| phentermine Phentermine: A central nervous system stimulant and sympathomimetic with actions and uses similar to those of DEXTROAMPHETAMINE. It has been used most frequently in the treatment of obesity. | 3.23 | 1 | 0 | primary amine | adrenergic agent; appetite depressant; central nervous system drug; central nervous system stimulant; dopaminergic agent; sympathomimetic agent |
| 4-phenylbutyric acid 4-phenylbutyric acid: RN refers to the parent cpd. 4-phenylbutyric acid : A monocarboxylic acid the structure of which is that of butyric acid substituted with a phenyl group at C-4. It is a histone deacetylase inhibitor that displays anticancer activity. It inhibits cell proliferation, invasion and migration and induces apoptosis in glioma cells. It also inhibits protein isoprenylation, depletes plasma glutamine, increases production of foetal haemoglobin through transcriptional activation of the gamma-globin gene and affects hPPARgamma activation. | 3.23 | 1 | 0 | monocarboxylic acid | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor; prodrug |
| pindolol Pindolol: A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638). pindolol : A member of the class of indols which is the 2-hydroxy-3-(isopropylamino)propyl ether derivative of 1H-indol-4-ol. | 3.23 | 1 | 0 | indoles; secondary amine | antiglaucoma drug; antihypertensive agent; beta-adrenergic antagonist; serotonergic antagonist; vasodilator agent |
| pioglitazone Pioglitazone: A thiazolidinedione and PPAR GAMMA agonist that is used in the treatment of TYPE 2 DIABETES MELLITUS.. pioglitazone : A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity. | 3.23 | 1 | 0 | aromatic ether; pyridines; thiazolidinediones | antidepressant; cardioprotective agent; EC 2.7.1.33 (pantothenate kinase) inhibitor; EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; geroprotector; hypoglycemic agent; insulin-sensitizing drug; PPARgamma agonist; xenobiotic |
| polythiazide [no description available] | 3.23 | 1 | 0 | benzothiadiazine | |
| duodote duodote: consists of atropine and pralidoxime chloride; for treating those exposed to organophosphorus-containing nerve agents | 3.23 | 1 | 0 | pyridinium ion | antidote to organophosphate poisoning; antidote to sarin poisoning; cholinergic drug; cholinesterase reactivator |
| praziquantel azinox: Russian drug | 3.23 | 1 | 0 | isoquinolines | |
| prazosin Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.. prazosin : A member of the class of piperazines that is piperazine substituted by a furan-2-ylcarbonyl group and a 4-amino-6,7-dimethoxyquinazolin-2-yl group at positions 1 and 4 respectively. | 3.23 | 1 | 0 | aromatic ether; furans; monocarboxylic acid amide; piperazines; quinazolines | alpha-adrenergic antagonist; antihypertensive agent; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor |
| primaquine Primaquine: An aminoquinoline that is given by mouth to produce a radical cure and prevent relapse of vivax and ovale malarias following treatment with a blood schizontocide. It has also been used to prevent transmission of falciparum malaria by those returning to areas where there is a potential for re-introduction of malaria. Adverse effects include anemias and GI disturbances. (From Martindale, The Extra Pharmacopeia, 30th ed, p404). primaquine : An N-substituted diamine that is pentane-1,4-diamine substituted by a 6-methoxyquinolin-8-yl group at the N(4) position. It is a drug used in the treatment of malaria and Pneumocystis pneumonia. | 3.23 | 1 | 0 | aminoquinoline; aromatic ether; N-substituted diamine | antimalarial |
| primidone Primidone: A barbiturate derivative that acts as a GABA modulator and anti-epileptic agent. It is partly metabolized to PHENOBARBITAL in the body and owes some of its actions to this metabolite.. primidone : A pyrimidone that is dihydropyrimidine-4,6(1H,5H)-dione substituted by an ethyl and a phenyl group at position 5. It is used as an anticonvulsant for treatment of various types of seizures. | 3.23 | 1 | 0 | pyrimidone | anticonvulsant; environmental contaminant; xenobiotic |
| probenecid Probenecid: The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.. probenecid : A sulfonamide in which the nitrogen of 4-sulfamoylbenzoic acid is substituted with two propyl groups. | 3.23 | 1 | 0 | benzoic acids; sulfonamide | uricosuric drug |
| procainamide Procainamide: A class Ia antiarrhythmic drug that is structurally-related to PROCAINE.. procainamide : A benzamide that is 4-aminobenzamide substituted on the amide N by a 2-(diethylamino)ethyl group. It is a pharmaceutical antiarrhythmic agent used for the medical treatment of cardiac arrhythmias. | 3.23 | 1 | 0 | benzamides | anti-arrhythmia drug; platelet aggregation inhibitor; sodium channel blocker |
| procarbazine Procarbazine: An antineoplastic agent used primarily in combination with mechlorethamine, vincristine, and prednisone (the MOPP protocol) in the treatment of Hodgkin's disease.. procarbazine : A benzamide obtained by formal condensation of the carboxy group of 4-[(2-methylhydrazino)methyl]benzoic acid with the amino group of isopropylamine. An antineoplastic chemotherapy drug used for treatment of Hodgkin's lymphoma. Metabolism yields azo-procarbazine and hydrogen peroxide, which results in the breaking of DNA strands. | 3.23 | 1 | 0 | benzamides; hydrazines | antineoplastic agent |
| prochlorperazine Prochlorperazine: A phenothiazine antipsychotic used principally in the treatment of NAUSEA; VOMITING; and VERTIGO. It is more likely than CHLORPROMAZINE to cause EXTRAPYRAMIDAL DISORDERS. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612). prochlorperazine : A member of the class of phenothiazines that is 10H-phenothiazine having a chloro substituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at the N-10 position. | 3.23 | 1 | 0 | N-alkylpiperazine; N-methylpiperazine; organochlorine compound; phenothiazines | alpha-adrenergic antagonist; antiemetic; cholinergic antagonist; dopamine receptor D2 antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; first generation antipsychotic |
| procyclidine Procyclidine: A muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in parkinsonism.. procyclidine : A tertiary alcohol that consists of propan-1-ol substituted by a cyclohexyl and a phenyl group at position 1 and a pyrrolidin-1-yl group at position 3. | 3.23 | 1 | 0 | pyrrolidines; tertiary alcohol | antidyskinesia agent; antiparkinson drug; muscarinic antagonist |
| promethazine Promethazine: A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals.. promethazine : A tertiary amine that is a substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropan-2-amine moiety. | 3.23 | 1 | 0 | phenothiazines; tertiary amine | anti-allergic agent; anticoronaviral agent; antiemetic; antipruritic drug; H1-receptor antagonist; local anaesthetic; sedative |
| propafenone Propafenone: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity.. propafenone : An aromatic ketone that is 3-(propylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is replaced by a 2-(3-phenylpropanoyl)phenyl group. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used as the hydrochloride salt in the management of supraventricular and ventricular arrhythmias. | 3.23 | 1 | 0 | aromatic ketone; secondary alcohol; secondary amino compound | anti-arrhythmia drug |
| propantheline Propantheline: A muscarinic antagonist used as an antispasmodic, in rhinitis, in urinary incontinence, and in the treatment of ulcers. At high doses it has nicotinic effects resulting in neuromuscular blocking. | 3.23 | 1 | 0 | xanthenes | |
| propofol Propofol: An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS.. propofol : A phenol resulting from the formal substitution of the hydrogen at the 2 position of 1,3-diisopropylbenzene by a hydroxy group. | 3.23 | 1 | 0 | phenols | anticonvulsant; antiemetic; intravenous anaesthetic; radical scavenger; sedative |
| propranolol Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3. | 3.23 | 1 | 0 | naphthalenes; propanolamine; secondary amine | anti-arrhythmia drug; antihypertensive agent; anxiolytic drug; beta-adrenergic antagonist; environmental contaminant; human blood serum metabolite; vasodilator agent; xenobiotic |
| protriptyline Protriptyline: Tricyclic antidepressant similar in action and side effects to IMIPRAMINE. It may produce excitation. | 3.23 | 1 | 0 | carbotricyclic compound | antidepressant |
| pyridostigmine [no description available] | 3.23 | 1 | 0 | pyridinium ion | |
| pyrimethamine Maloprim: contains above 2 cpds | 3.23 | 1 | 0 | aminopyrimidine; monochlorobenzenes | antimalarial; antiprotozoal drug; EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
| sch 16134 quazepam: structure given in first source | 3.23 | 1 | 0 | benzodiazepine | |
| quetiapine [no description available] | 3.23 | 1 | 0 | dibenzothiazepine; N-alkylpiperazine; N-arylpiperazine | adrenergic antagonist; dopaminergic antagonist; histamine antagonist; second generation antipsychotic; serotonergic antagonist |
| rabeprazole Rabeprazole: A 4-(3-methoxypropoxy)-3-methylpyridinyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. | 3.23 | 1 | 0 | benzimidazoles; pyridines; sulfoxide | anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor |
| raloxifene raloxifene : A member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogens at positions 2, 3, and 6 have been replaced by p-hydroxyphenyl, p-[2-(piperidin-1-yl)ethoxy]benzoyl, and hydroxy groups, respectively. | 3.23 | 1 | 0 | 1-benzothiophenes; aromatic ketone; N-oxyethylpiperidine; phenols | bone density conservation agent; estrogen antagonist; estrogen receptor modulator |
| riluzole Riluzole: A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS. | 3.23 | 1 | 0 | benzothiazoles | |
| rimantadine Rimantadine: An RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza. | 3.23 | 1 | 0 | alkylamine | |
| risperidone Risperidone: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.. risperidone : A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2. | 3.23 | 1 | 0 | 1,2-benzoxazoles; heteroarylpiperidine; organofluorine compound; pyridopyrimidine | alpha-adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; H1-receptor antagonist; psychotropic drug; second generation antipsychotic; serotonergic antagonist |
| rizatriptan rizatriptan: structure given in first source; RN given refers to benzoate | 3.23 | 1 | 0 | tryptamines | anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| ropinirole [no description available] | 3.23 | 1 | 0 | indolones; tertiary amine | antidyskinesia agent; antiparkinson drug; central nervous system drug; dopamine agonist |
| salicylsalicylic acid salicylsalicylic acid: structure. salsalate : A dimeric benzoate ester obtained by intermolecular condensation between the carboxy of one molecule of salicylic acid with the phenol group of a second. It is a prodrug for salycylic acid that is used for treatment of rheumatoid arthritis and osteoarthritis and also shows activity against type II diabetes. | 3.23 | 1 | 0 | benzoate ester; benzoic acids; phenols; salicylates | antineoplastic agent; antirheumatic drug; EC 3.5.2.6 (beta-lactamase) inhibitor; hypoglycemic agent; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug |
| secobarbital Secobarbital: A barbiturate that is used as a sedative. Secobarbital is reported to have no anti-anxiety activity.. secobarbital : A member of the class of barbiturates that is barbituric acid in which the hydrogens at position 5 are substituted by prop-2-en-1-yl and pentan-2-yl groups. | 3.23 | 1 | 0 | barbiturates | anaesthesia adjuvant; GABA modulator; sedative |
| sibutramine sibutramine: serotonin and norepinephrine transporter inhibitor; Meridia is tradename for sibutramine hydrochloride | 3.23 | 1 | 0 | organochlorine compound; tertiary amino compound | anti-obesity agent; serotonin uptake inhibitor |
| sulfadiazine Sulfadiazine: One of the short-acting SULFONAMIDES used in combination with PYRIMETHAMINE to treat toxoplasmosis in patients with acquired immunodeficiency syndrome and in newborns with congenital infections.. sulfadiazine : A sulfonamide consisting of pyrimidine with a 4-aminobenzenesulfonamido group at the 2-position.. diazine : The parent structure of the diazines. | 3.23 | 1 | 0 | pyrimidines; substituted aniline; sulfonamide antibiotic; sulfonamide | antiinfective agent; antimicrobial agent; antiprotozoal drug; coccidiostat; drug allergen; EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor; EC 2.5.1.15 (dihydropteroate synthase) inhibitor; environmental contaminant; xenobiotic |
| risedronic acid Risedronic Acid: A pyridine and diphosphonic acid derivative that acts as a CALCIUM CHANNEL BLOCKER and inhibits BONE RESORPTION. | 3.23 | 1 | 0 | pyridines | |
| sotalol Sotalol: An adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias.. sotalol : A sulfonamide that is N-phenylmethanesulfonamide in which the phenyl group is substituted at position 4 by a 1-hydroxy-2-(isopropylamino)ethyl group. It has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. It is used (usually as the hydrochloride salt) for the management of ventricular and supraventricular arrhythmias. | 3.23 | 1 | 0 | ethanolamines; secondary alcohol; secondary amino compound; sulfonamide | anti-arrhythmia drug; beta-adrenergic antagonist; environmental contaminant; xenobiotic |
| imatinib [no description available] | 3.23 | 1 | 0 | aromatic amine; benzamides; N-methylpiperazine; pyridines; pyrimidines | antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor |
| vorinostat Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL). | 3.23 | 1 | 0 | dicarboxylic acid diamide; hydroxamic acid | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor |
| succinylcholine Succinylcholine: A quaternary skeletal muscle relaxant usually used in the form of its bromide, chloride, or iodide. It is a depolarizing relaxant, acting in about 30 seconds and with a duration of effect averaging three to five minutes. Succinylcholine is used in surgical, anesthetic, and other procedures in which a brief period of muscle relaxation is called for.. succinylcholine : A quaternary ammonium ion that is the bis-choline ester of succinic acid. | 3.23 | 1 | 0 | quaternary ammonium ion; succinate ester | drug allergen; muscle relaxant; neuromuscular agent |
| sulfamethizole Sulfamethizole: A sulfathiazole antibacterial agent.. sulfamethizole : A sulfonamide consisting of a 1,3,4-thiadiazole nucleus with a methyl substituent at C-5 and a 4-aminobenzenesulfonamido group at C-2. | 3.23 | 1 | 0 | sulfonamide antibiotic; sulfonamide; thiadiazoles | antiinfective agent; antimicrobial agent; drug allergen; EC 2.5.1.15 (dihydropteroate synthase) inhibitor |
| sulfasalazine Sulfasalazine: A drug that is used in the management of inflammatory bowel diseases. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid (see MESALAMINE) released in the colon. (From Martindale, The Extra Pharmacopoeia, 30th ed, p907). sulfasalazine : An azobenzene consisting of diphenyldiazene having a carboxy substituent at the 4-position, a hydroxy substituent at the 3-position and a 2-pyridylaminosulphonyl substituent at the 4'-position. | 3.23 | 1 | 0 | ||
| sulfathiazole Sulfathiazole: A sulfathiazole compound that is used as a short-acting anti-infective agent. It is no longer commonly used systemically due to its toxicity, but may still be applied topically in combination with other drugs for the treatment of vaginal and skin infections, and is still used in veterinary medicine.. sulfathiazole : A 1,3-thiazole compound having a 4-aminobenzenesulfonamido group at the 2-position. | 3.23 | 1 | 0 | 1,3-thiazoles; substituted aniline; sulfonamide antibiotic; sulfonamide | antiinfective agent; drug allergen; EC 2.5.1.15 (dihydropteroate synthase) inhibitor; environmental contaminant; xenobiotic |
| 2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol [no description available] | 3.23 | 1 | 0 | alkylbenzene | |
| sumatriptan Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.. sumatriptan : A sulfonamide that consists of N,N-dimethyltryptamine bearing an additional (N-methylsulfamoyl)methyl substituent at position 5. Selective agonist for a vascular 5-HT1 receptor subtype (probably a member of the 5-HT1D family). Used (in the form of its succinate salt) for the acute treatment of migraine with or without aura in adults. | 3.23 | 1 | 0 | sulfonamide; tryptamines | serotonergic agonist; vasoconstrictor agent |
| temazepam Temazepam: A benzodiazepine that acts as a GAMMA-AMINOBUTYRIC ACID modulator and anti-anxiety agent. | 3.23 | 1 | 0 | benzodiazepine | |
| temozolomide [no description available] | 3.23 | 1 | 0 | imidazotetrazine; monocarboxylic acid amide; triazene derivative | alkylating agent; antineoplastic agent; prodrug |
| terazosin Terazosin: induces decreased blood pressure; used in the treatment of benign prostatic hyperplasia | 3.23 | 1 | 0 | furans; piperazines; primary amino compound; quinazolines | alpha-adrenergic antagonist; antihypertensive agent; antineoplastic agent |
| terbutaline Terbutaline: A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic.. terbutaline : A member of the class of phenylethanolamines that is catechol substituted at position 5 by a 2-(tert-butylamino)-1-hydroxyethyl group. | 3.23 | 1 | 0 | phenylethanolamines; resorcinols | anti-asthmatic drug; beta-adrenergic agonist; bronchodilator agent; EC 3.1.1.7 (acetylcholinesterase) inhibitor; hypoglycemic agent; sympathomimetic agent; tocolytic agent |
| thalidomide Thalidomide: A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, but withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of immunological and inflammatory disorders. Thalidomide displays immunosuppressive and anti-angiogenic activity. It inhibits release of TUMOR NECROSIS FACTOR-ALPHA from monocytes, and modulates other cytokine action.. thalidomide : A racemate comprising equimolar amounts of R- and S-thalidomide.. 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione : A dicarboximide that is isoindole-1,3(2H)-dione in which the hydrogen attached to the nitrogen is substituted by a 2,6-dioxopiperidin-3-yl group. | 3.23 | 1 | 0 | phthalimides; piperidones | |
| thiabendazole Tresaderm: dermatologic soln containing dexamethasone, thiabendazole & neomycin sulfate | 3.23 | 1 | 0 | 1,3-thiazoles; benzimidazole fungicide; benzimidazoles | antifungal agrochemical; antinematodal drug |
| thioridazine Thioridazine: A phenothiazine antipsychotic used in the management of PHYCOSES, including SCHIZOPHRENIA.. thioridazine : A phenothiazine derivative having a methylsulfanyl subsitituent at the 2-position and a (1-methylpiperidin-2-yl)ethyl] group at the N-10 position. | 3.23 | 1 | 0 | phenothiazines; piperidines | alpha-adrenergic antagonist; dopaminergic antagonist; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; first generation antipsychotic; H1-receptor antagonist; serotonergic antagonist |
| thiotepa Thiotepa: A very toxic alkylating antineoplastic agent also used as an insect sterilant. It causes skin, gastrointestinal, CNS, and bone marrow damage. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), thiotepa may reasonably be anticipated to be a carcinogen (Merck Index, 11th ed). | 3.23 | 1 | 0 | aziridines | |
| ticlopidine Ticlopidine: An effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES.. ticlopidine : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group. | 3.23 | 1 | 0 | monochlorobenzenes; thienopyridine | anticoagulant; fibrin modulating drug; hematologic agent; P2Y12 receptor antagonist; platelet aggregation inhibitor |
| tinidazole Tinidazole: A nitroimidazole alkylating agent that is used as an antitrichomonal agent against TRICHOMONAS VAGINALIS; ENTAMOEBA HISTOLYTICA; and GIARDIA LAMBLIA infections. It also acts as an antibacterial agent for the treatment of BACTERIAL VAGINOSIS and anaerobic bacterial infections.. tinidazole : 1H-imidazole substituted at C-1 by a (2-ethylsulfonyl)ethyl group, at C-2 by a methyl group and at C-5 by a nitro group. It is used as an antiprotozoal, antibacterial agent. | 3.23 | 1 | 0 | imidazoles | antiamoebic agent; antibacterial drug; antiparasitic agent; antiprotozoal drug |
| tiopronin Tiopronin: Sulfhydryl acylated derivative of GLYCINE. | 3.23 | 1 | 0 | N-acyl-amino acid | |
| tizanidine tizanidine: RN given refers to parent cpd; structure. tizanidine : 2,1,3-Benzothiadiazole substituted at C-4 by a Delta(1)-imidazolin-2-ylamino group and at C-4 by a chloro group. It is an agonist at alpha2-adrenergic receptor sites. | 3.23 | 1 | 0 | benzothiadiazole; imidazoles | alpha-adrenergic agonist; muscle relaxant |
| tolazamide Tolazamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE.. tolazamide : An N-sulfonylurea that is 1-tosylurea in which a hydrogen attached to the nitrogen at position 3 is replaced by an azepan-1-yl group. A hypoglycemic agent, it is used for the treatment of type 2 diabetes mellitus. | 3.23 | 1 | 0 | N-sulfonylurea | hypoglycemic agent; potassium channel blocker |
| tolbutamide Tolbutamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). tolbutamide : An N-sulfonylurea that consists of 1-butylurea having a tosyl group attached at the 3-position. | 3.23 | 1 | 0 | N-sulfonylurea | human metabolite; hypoglycemic agent; insulin secretagogue; potassium channel blocker |
| tolmetin Tolmetin: A non-steroidal anti-inflammatory agent (ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL) similar in mode of action to INDOMETHACIN.. tolmetin : A monocarboxylic acid that is (1-methylpyrrol-2-yl)acetic acid substituted at position 5 on the pyrrole ring by a 4-methylbenzoyl group. Used in the form of its sodium salt dihydrate as a nonselective nonsteroidal anti-inflammatory drug. | 3.23 | 1 | 0 | aromatic ketone; monocarboxylic acid; pyrroles | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-steroidal anti-inflammatory drug |
| ultram 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol : A tertiary alcohol that is cyclohexanol substituted at positions 1 and 2 by 3-methoxyphenyl and dimethylaminomethyl groups respectively. | 3.23 | 1 | 0 | aromatic ether; tertiary alcohol; tertiary amino compound | |
| tranexamic acid Tranexamic Acid: Antifibrinolytic hemostatic used in severe hemorrhage. | 3.23 | 1 | 0 | amino acid | |
| trazodone Trazodone: A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309). trazodone : An N-arylpiperazine in which one nitrogen is substituted by a 3-chlorophenyl group, while the other is substituted by a 3-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propyl group. | 3.23 | 1 | 0 | monochlorobenzenes; N-alkylpiperazine; N-arylpiperazine; triazolopyridine | adrenergic antagonist; antidepressant; anxiolytic drug; H1-receptor antagonist; sedative; serotonin uptake inhibitor |
| triamterene Triamterene: A pteridinetriamine compound that inhibits SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS.. triamterene : Pteridine substituted at positions 2, 4 and 7 with amino groups and at position 6 with a phenyl group. A sodium channel blocker, it is used as a diuretic in the treatment of hypertension and oedema. | 3.23 | 1 | 0 | pteridines | diuretic; sodium channel blocker |
| triazolam Triazolam: A short-acting benzodiazepine used in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries. | 3.23 | 1 | 0 | triazolobenzodiazepine | sedative |
| trifluoperazine [no description available] | 3.23 | 1 | 0 | N-alkylpiperazine; N-methylpiperazine; organofluorine compound; phenothiazines | antiemetic; calmodulin antagonist; dopaminergic antagonist; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor; phenothiazine antipsychotic drug |
| trihexyphenidyl Trihexyphenidyl: One of the centrally acting MUSCARINIC ANTAGONISTS used for treatment of PARKINSONIAN DISORDERS and drug-induced extrapyramidal movement disorders and as an antispasmodic. | 3.23 | 1 | 0 | amine | |
| trimethadione Trimethadione: An anticonvulsant effective in absence seizures, but generally reserved for refractory cases because of its toxicity. (From AMA Drug Evaluations Annual, 1994, p378). trimethadione : An oxazolidinone that is 1,3-oxazolidine-2,4-dione substituted by methyl groups at positions 3, 5 and 5. It is an antiepileptic agent. | 3.23 | 1 | 0 | oxazolidinone | anticonvulsant; geroprotector |
| trimethobenzamide trimethobenzamide: major descriptor (64-84); on-line search BENZAMIDES (64-84); Index Medicus search TRIMETHOBENZAMIDE (64-84); RN given refers to parent cpd. trimethobenzamide : The amide obtained by formal condensation of 3,4,5-trihydroxybenzoic acid with 4-[2-(N,N-dimethylamino)ethoxy]benzylamine. It is used to prevent nausea and vomitting in humans. | 3.23 | 1 | 0 | benzamides; tertiary amino compound | antiemetic |
| trimethoprim Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge. | 3.23 | 1 | 0 | aminopyrimidine; methoxybenzenes | antibacterial drug; diuretic; drug allergen; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; environmental contaminant; xenobiotic |
| trimetrexate Trimetrexate: A nonclassical folic acid inhibitor through its inhibition of the enzyme dihydrofolate reductase. It is being tested for efficacy as an antineoplastic agent and as an antiparasitic agent against PNEUMOCYSTIS PNEUMONIA in AIDS patients. Myelosuppression is its dose-limiting toxic effect. | 3.23 | 1 | 0 | ||
| trimipramine Trimipramine: Tricyclic antidepressant similar to IMIPRAMINE, but with more antihistaminic and sedative properties.. trimipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)-2-methylpropyl group at the nitrogen atom. It is used as an antidepressant. | 3.23 | 1 | 0 | dibenzoazepine; tertiary amino compound | antidepressant; environmental contaminant; xenobiotic |
| troglitazone Troglitazone: A chroman and thiazolidinedione derivative that acts as a PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS (PPAR) agonist. It was formerly used in the treatment of TYPE 2 DIABETES MELLITUS, but has been withdrawn due to hepatotoxicity. | 3.23 | 1 | 0 | chromanes; thiazolidinone | anticoagulant; anticonvulsant; antineoplastic agent; antioxidant; EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; hypoglycemic agent; platelet aggregation inhibitor; vasodilator agent |
| tyramine [no description available] | 3.23 | 1 | 0 | monoamine molecular messenger; primary amino compound; tyramines | EC 3.1.1.8 (cholinesterase) inhibitor; Escherichia coli metabolite; human metabolite; mouse metabolite; neurotransmitter |
| delavirdine Delavirdine: A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1.. delavirdine : The amide resulting from the formal condensation of 5-[(methylsulfonyl)amino]-1H-indole-2-carboxylic acid and 4-amino group of 1-[3-(isopropylamino)pyridin-2-yl]piperazine, delavirdine is a non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1. Viral resistance emerges rapidly when delavirdine is used alone, so it is therefore used (as the methanesulfonic acid salt) with other antiretrovirals for combination therapy of HIV infection. | 3.23 | 1 | 0 | aminopyridine; indolecarboxamide; N-acylpiperazine; sulfonamide | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| venlafaxine venlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-methoxyphenyl group. | 3.23 | 1 | 0 | cyclohexanols; monomethoxybenzene; tertiary alcohol; tertiary amino compound | adrenergic uptake inhibitor; analgesic; antidepressant; dopamine uptake inhibitor; environmental contaminant; serotonin uptake inhibitor; xenobiotic |
| vigabatrin [no description available] | 3.23 | 1 | 0 | gamma-amino acid | anticonvulsant; EC 2.6.1.19 (4-aminobutyrate--2-oxoglutarate transaminase) inhibitor |
| ici 204,219 zafirlukast: a leukotriene D4 receptor antagonist | 3.23 | 1 | 0 | carbamate ester; indoles; N-sulfonylcarboxamide | anti-asthmatic agent; leukotriene antagonist |
| zaleplon zaleplon: an azabicyclo(4.3.0)nonane; a nonbenzodiazepine; one of the so-called of Z drugs (zopiclone, eszopiclone, zolpidem, and zaleplon) for which there is some correlation with tumors; a hypnotic with less marked effect on psychomotor functions compared to lorazepam. zaleplon : A pyrazolo[1,5-a]pyrimidine having a nitrile group at position 3 and a 3-(N-ethylacetamido)phenyl substituent at the 7-position. | 3.23 | 1 | 0 | nitrile; pyrazolopyrimidine | anticonvulsant; anxiolytic drug; central nervous system depressant; sedative |
| zolpidem Zolpidem: An imidazopyridine derivative and short-acting GABA-A receptor agonist that is used for the treatment of INSOMNIA.. zolpidem : An imidazo[1,2-a]pyridine compound having a 4-tolyl group at the 2-position, an N,N-dimethylcarbamoylmethyl group at the 3-position and a methyl substituent at the 6-position. | 3.23 | 1 | 0 | imidazopyridine | central nervous system depressant; GABA agonist; sedative |
| zonisamide Zonisamide: A benzisoxazole and sulfonamide derivative that acts as a CALCIUM CHANNEL blocker. It is used primarily as an adjunctive antiepileptic agent for the treatment of PARTIAL SEIZURES, with or without secondary generalization.. zonisamide : A 1,2-benzoxazole compound having a sulfamoylmethyl substituent at the 3-position. | 3.23 | 1 | 0 | 1,2-benzoxazoles; sulfonamide | anticonvulsant; antioxidant; central nervous system drug; protective agent; T-type calcium channel blocker |
| cortisone acetate Cortisone Acetate: The acetate ester of cortisone that is used mainly for replacement therapy in adrenocortical insufficiency and in the treatment of many allergic and inflammatory disorders. | 3.23 | 1 | 0 | corticosteroid hormone | |
| mitomycin Mitomycin: An antineoplastic antibiotic produced by Streptomyces caespitosus. It is one of the bi- or tri-functional ALKYLATING AGENTS causing cross-linking of DNA and inhibition of DNA synthesis.. mitomycin : A family of aziridine-containing natural products isolated from Streptomyces caespitosus or Streptomyces lavendulae. | 3.23 | 1 | 0 | mitomycin | alkylating agent; antineoplastic agent |
| prednisolone Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone. | 3.23 | 1 | 0 | 11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | adrenergic agent; anti-inflammatory drug; antineoplastic agent; drug metabolite; environmental contaminant; immunosuppressive agent; xenobiotic |
| reserpine Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.. reserpine : An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. | 3.23 | 1 | 0 | alkaloid ester; methyl ester; yohimban alkaloid | adrenergic uptake inhibitor; antihypertensive agent; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; first generation antipsychotic; plant metabolite; xenobiotic |
| phentolamine Phentolamine: A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.. phentolamine : A substituted aniline that is 3-aminophenol in which the hydrogens of the amino group are replaced by 4-methylphenyl and 4,5-dihydro-1H-imidazol-2-ylmethyl groups respectively. An alpha-adrenergic antagonist, it is used for the treatment of hypertension. | 3.23 | 1 | 0 | imidazoles; phenols; substituted aniline; tertiary amino compound | alpha-adrenergic antagonist; vasodilator agent |
| sorbitol D-glucitol : The D-enantiomer of glucitol (also known as D-sorbitol). | 3.23 | 1 | 0 | glucitol | cathartic; Escherichia coli metabolite; food humectant; human metabolite; laxative; metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite; sweetening agent |
| thyroxine Thyroxine: The major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism.. thyroxine : An iodothyronine compound having iodo substituents at the 3-, 3'-, 5- and 5'-positions. | 3.23 | 1 | 0 | 2-halophenol; iodophenol; L-phenylalanine derivative; non-proteinogenic L-alpha-amino acid; thyroxine zwitterion; thyroxine | antithyroid drug; human metabolite; mouse metabolite; thyroid hormone |
| dextroamphetamine Dextroamphetamine: The d-form of AMPHETAMINE. It is a central nervous system stimulant and a sympathomimetic. It has also been used in the treatment of narcolepsy and of attention deficit disorders and hyperactivity in children. Dextroamphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulating release of monamines, and inhibiting monoamine oxidase. It is also a drug of abuse and a psychotomimetic.. (S)-amphetamine : A 1-phenylpropan-2-amine that has S configuration. | 3.23 | 1 | 0 | 1-phenylpropan-2-amine | adrenergic agent; adrenergic uptake inhibitor; dopamine uptake inhibitor; dopaminergic agent; neurotoxin; sympathomimetic agent |
| spironolactone Spironolactone: A potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827). spironolactone : A steroid lactone that is 17alpha-pregn-4-ene-21,17-carbolactone substituted by an oxo group at position 3 and an alpha-acetylsulfanyl group at position 7. | 3.23 | 1 | 0 | 3-oxo-Delta(4) steroid; oxaspiro compound; steroid lactone; thioester | aldosterone antagonist; antihypertensive agent; diuretic; environmental contaminant; xenobiotic |
| penicillamine Penicillamine: 3-Mercapto-D-valine. The most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.. penicillamine : An alpha-amino acid having the structure of valine substituted at the beta position with a sulfanyl group. | 3.23 | 1 | 0 | non-proteinogenic alpha-amino acid; penicillamine | antirheumatic drug; chelator; copper chelator; drug allergen |
| cysteine [no description available] | 3.23 | 1 | 0 | cysteine zwitterion; cysteine; L-alpha-amino acid; proteinogenic amino acid; serine family amino acid | EC 4.3.1.3 (histidine ammonia-lyase) inhibitor; flour treatment agent; human metabolite |
| prednisone Prednisone: A synthetic anti-inflammatory glucocorticoid derived from CORTISONE. It is biologically inert and converted to PREDNISOLONE in the liver.. prednisone : A synthetic glucocorticoid drug that is particularly effective as an immunosuppressant, and affects virtually all of the immune system. Prednisone is a prodrug that is converted by the liver into prednisolone (a beta-hydroxy group instead of the oxo group at position 11), which is the active drug and also a steroid. | 3.23 | 1 | 0 | 11-oxo steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | adrenergic agent; anti-inflammatory drug; antineoplastic agent; immunosuppressive agent; prodrug |
| estrone Hydroxyestrones: Estrone derivatives substituted with one or more hydroxyl groups in any position. They are important metabolites of estrone and other estrogens. | 3.23 | 1 | 0 | 17-oxo steroid; 3-hydroxy steroid; phenolic steroid; phenols | antineoplastic agent; bone density conservation agent; estrogen; human metabolite; mouse metabolite |
| oxandrolone Oxandrolone: A synthetic hormone with anabolic and androgenic properties. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo steroid; anabolic androgenic steroid; oxa-steroid | anabolic agent; androgen |
| penicillin g Penicillin G: A penicillin derivative commonly used in the form of its sodium or potassium salts in the treatment of a variety of infections. It is effective against most gram-positive bacteria and against gram-negative cocci. It has also been used as an experimental convulsant because of its actions on GAMMA-AMINOBUTYRIC ACID mediated synaptic transmission.. benzylpenicillin : A penicillin in which the substituent at position 6 of the penam ring is a phenylacetamido group. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug; drug allergen; epitope |
| pilocarpine Pilocarpine: A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.. (+)-pilocarpine : The (+)-enantiomer of pilocarpine. | 3.23 | 1 | 0 | pilocarpine | antiglaucoma drug |
| triiodothyronine Triiodothyronine: A T3 thyroid hormone normally synthesized and secreted by the thyroid gland in much smaller quantities than thyroxine (T4). Most T3 is derived from peripheral monodeiodination of T4 at the 5' position of the outer ring of the iodothyronine nucleus. The hormone finally delivered and used by the tissues is mainly T3.. 3,3',5-triiodo-L-thyronine : An iodothyronine compound having iodo substituents at the 3-, 3'- and 5-positions. Although some is produced in the thyroid, most of the 3,3',5-triiodo-L-thyronine in the body is generated by mono-deiodination of L-thyroxine in the peripheral tissues. Its metabolic activity is about 3 to 5 times that of L-thyroxine. The sodium salt is used in the treatment of hypothyroidism. | 3.23 | 1 | 0 | 2-halophenol; amino acid zwitterion; iodophenol; iodothyronine | human metabolite; mouse metabolite; thyroid hormone |
| chloramphenicol Amphenicol: Chloramphenicol and its derivatives. | 3.23 | 1 | 0 | C-nitro compound; carboxamide; diol; organochlorine compound | antibacterial drug; antimicrobial agent; Escherichia coli metabolite; geroprotector; Mycoplasma genitalium metabolite; protein synthesis inhibitor |
| glutamine Glutamine: A non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from GLUTAMIC ACID and AMMONIA. It is the principal carrier of NITROGEN in the body and is an important energy source for many cells.. L-glutamine : An optically active form of glutamine having L-configuration.. glutamine : An alpha-amino acid that consists of butyric acid bearing an amino substituent at position 2 and a carbamoyl substituent at position 4. | 3.23 | 1 | 0 | amino acid zwitterion; glutamine family amino acid; glutamine; L-alpha-amino acid; polar amino acid zwitterion; proteinogenic amino acid | EC 1.14.13.39 (nitric oxide synthase) inhibitor; Escherichia coli metabolite; human metabolite; metabolite; micronutrient; mouse metabolite; nutraceutical; Saccharomyces cerevisiae metabolite |
| vincristine [no description available] | 3.23 | 1 | 0 | acetate ester; formamides; methyl ester; organic heteropentacyclic compound; organic heterotetracyclic compound; tertiary alcohol; tertiary amino compound; vinca alkaloid | antineoplastic agent; drug; microtubule-destabilising agent; plant metabolite; tubulin modulator |
| physostigmine Physostigmine: A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity. | 3.23 | 1 | 0 | carbamate ester; indole alkaloid | antidote to curare poisoning; EC 3.1.1.8 (cholinesterase) inhibitor; miotic |
| apomorphine Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use. | 3.23 | 1 | 0 | aporphine alkaloid | alpha-adrenergic drug; antidyskinesia agent; antiparkinson drug; dopamine agonist; emetic; serotonergic drug |
| methyltestosterone Methyltestosterone: A synthetic hormone used for androgen replacement therapy and as an hormonal antineoplastic agent (ANTINEOPLASTIC AGENTS, HORMONAL).. methyltestosterone : A 17beta-hydroxy steroid that is testosterone bearing a methyl group at the 17alpha position. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; enone | anabolic agent; androgen; antineoplastic agent |
| tetrabenazine 9,10-dimethoxy-3-isobutyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one : A benzoquinolizine that is 1,2,3,4,4a,9,10,10a-octahydrophenanthrene in which the carbon at position 10a is replaced by a nitrogen and which is substituted by an isobutyl group at position 2, an oxo group at position 3, and methoxy groups at positions 6 and 7. | 3.23 | 1 | 0 | benzoquinolizine; cyclic ketone; tertiary amino compound | |
| kanamycin a Kanamycin: Antibiotic complex produced by Streptomyces kanamyceticus from Japanese soil. Comprises 3 components: kanamycin A, the major component, and kanamycins B and C, the minor components.. kanamycin : Kanamycin is a naturally occurring antibiotic complex from Streptomyces kanamyceticus that consists of several components: kanamycin A, the major component (also usually designated as kanamycin), and kanamycins B, C, D and X the minor components. | 3.23 | 1 | 0 | kanamycins | bacterial metabolite |
| edetic acid Edetic Acid: A chelating agent that sequesters a variety of polyvalent cations such as CALCIUM. It is used in pharmaceutical manufacturing and as a food additive. | 3.23 | 1 | 0 | ethylenediamine derivative; polyamino carboxylic acid; tetracarboxylic acid | anticoagulant; antidote; chelator; copper chelator; geroprotector |
| cysteamine Cysteamine: A mercaptoethylamine compound that is endogenously derived from the COENZYME A degradative pathway. The fact that cysteamine is readily transported into LYSOSOMES where it reacts with CYSTINE to form cysteine-cysteamine disulfide and CYSTEINE has led to its use in CYSTINE DEPLETING AGENTS for the treatment of CYSTINOSIS.. cysteamine : An amine that consists of an ethane skeleton substituted with a thiol group at C-1 and an amino group at C-2. | 3.23 | 1 | 0 | amine; thiol | geroprotector; human metabolite; mouse metabolite; radiation protective agent |
| acetylcholine chloride acetylcholine chloride : The chloride salt of acetylcholine, and a parasympatomimetic drug. | 3.23 | 1 | 0 | quaternary ammonium salt | |
| mepazine mepazine: major descriptor (66-85); on-line search PHENOTHIAZINES (66-85); Index Medicus search MEPAZINE (66-85); RN given refers to parent cpd. pacatal : A phenothiazine derivative in which 10H-phenothiazine has an N-methylpiperidin-4-ylmethyl substituent at the N-10 position. | 3.23 | 1 | 0 | phenothiazines | |
| cloxacillin Cloxacillin: A semi-synthetic antibiotic that is a chlorinated derivative of OXACILLIN.. cloxacillin : A semisynthetic penicillin antibiotic carrying a 3-(2-chlorophenyl)-5-methylisoxazole-4-carboxamido group at position 6. | 3.23 | 1 | 0 | penicillin allergen; penicillin; semisynthetic derivative | antibacterial agent; antibacterial drug |
| calcium acetate calcium acetate: a principal compound used as phosphate binders in patients with chronic renal failure; used like sevelamer. calcium acetate : The calcium salt of acetic acid. It is used, commonly as a hydrate, to treat hyperphosphataemia (excess phosphate in the blood) in patients with kidney disease: the calcium ion combines with dietary phosphate to form (insoluble) calcium phosphate, which is excreted in the faeces. | 3.23 | 1 | 0 | calcium salt | chelator |
| methionine Methionine: A sulfur-containing essential L-amino acid that is important in many body functions.. methionine : A sulfur-containing amino acid that is butyric acid bearing an amino substituent at position 2 and a methylthio substituent at position 4. | 3.23 | 1 | 0 | aspartate family amino acid; L-alpha-amino acid; methionine zwitterion; methionine; proteinogenic amino acid | antidote to paracetamol poisoning; human metabolite; micronutrient; mouse metabolite; nutraceutical |
| colchicine (S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions. | 3.23 | 1 | 0 | alkaloid; colchicine | anti-inflammatory agent; gout suppressant; mutagen |
| mebanazine mebanazine: RN given refers to parent cpd without isomeric designation; structure | 3.23 | 1 | 0 | benzenes | |
| oxacillin Oxacillin: An antibiotic similar to FLUCLOXACILLIN used in resistant staphylococci infections.. oxacillin : A penicillin antibiotic carrying a 5-methyl-3-phenylisoxazole-4-carboxamide group at position 6beta. | 3.23 | 1 | 0 | penicillin | antibacterial agent; antibacterial drug |
| cycloserine Cycloserine: Antibiotic substance produced by Streptomyces garyphalus.. D-cycloserine : A 4-amino-1,2-oxazolidin-3-one that has R configuration. It is an antibiotic produced by Streptomyces garyphalus or S. orchidaceus and is used as part of a multi-drug regimen for the treatment of tuberculosis when resistance to, or toxicity from, primary drugs has developed. An analogue of D-alanine, it interferes with bacterial cell wall synthesis in the cytoplasm by competitive inhibition of L-alanine racemase (which forms D-alanine from L-alanine) and D-alanine--D-alanine ligase (which incorporates D-alanine into the pentapeptide required for peptidoglycan formation and bacterial cell wall synthesis). | 3.23 | 1 | 0 | 4-amino-1,2-oxazolidin-3-one; organonitrogen heterocyclic antibiotic; organooxygen heterocyclic antibiotic; zwitterion | antiinfective agent; antimetabolite; antitubercular agent; metabolite; NMDA receptor agonist |
| benziodarone benziodarone: minor descriptor (75-89); on-line & INDEX MEDICUS search BENZOFURANS (68-89) & IODOBENZOATES (74) | 3.23 | 1 | 0 | aromatic ketone | |
| ampicillin Ampicillin: Semi-synthetic derivative of penicillin that functions as an orally active broad-spectrum antibiotic.. ampicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-phenylacetamido group. | 3.23 | 1 | 0 | beta-lactam antibiotic; penicillin allergen; penicillin | antibacterial drug |
| mannitol [no description available] | 3.23 | 1 | 0 | mannitol | allergen; antiglaucoma drug; compatible osmolytes; Escherichia coli metabolite; food anticaking agent; food bulking agent; food humectant; food stabiliser; food thickening agent; hapten; metabolite; osmotic diuretic; sweetening agent |
| cytarabine [no description available] | 3.23 | 1 | 0 | beta-D-arabinoside; monosaccharide derivative; pyrimidine nucleoside | antimetabolite; antineoplastic agent; antiviral agent; immunosuppressive agent |
| arginine Arginine: An essential amino acid that is physiologically active in the L-form.. arginine : An alpha-amino acid that is glycine in which the alpha-is substituted by a 3-guanidinopropyl group. | 3.23 | 1 | 0 | arginine; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid | biomarker; Escherichia coli metabolite; micronutrient; mouse metabolite; nutraceutical |
| perflutren Definity: a fluorocarbon-filled ultrasonic contrast agent; Definity is tradename. octafluoropropane : A fluorocarbon that is propane in which all of the hydrogens have been replaced by fluorines. | 3.23 | 1 | 0 | fluoroalkane; fluorocarbon | |
| fluoxymesterone Fluoxymesterone: An anabolic steroid that has been used in the treatment of male HYPOGONADISM, delayed puberty in males, and in the treatment of breast neoplasms in women. | 3.23 | 1 | 0 | 11beta-hydroxy steroid; 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; anabolic androgenic steroid; fluorinated steroid | anabolic agent; antineoplastic agent |
| methsuximide methsuximide: anticonvulsant effective in petit mal & psychomotor epilepsy; has a number of unpleasant & toxic side effects; minor descriptor (75-86); on-line & INDEX MEDICUS search SUCCINIMIDES (75-86); RN given refers to parent cpd without isomeric designation | 3.23 | 1 | 0 | organic molecular entity | |
| tromethamine Tromethamine: An organic amine proton acceptor. It is used in the synthesis of surface-active agents and pharmaceuticals; as an emulsifying agent for cosmetic creams and lotions, mineral oil and paraffin wax emulsions, as a biological buffer, and used as an alkalizer. (From Merck, 11th ed; Martindale, The Extra Pharmacopoeia, 30th ed, p1424) | 3.23 | 1 | 0 | primary amino compound; triol | buffer |
| methylprednisolone Methylprednisolone: A PREDNISOLONE derivative with similar anti-inflammatory action.. 6alpha-methylprednisolone : The 6alpha-stereoisomer of 6-methylprednisolone. | 3.23 | 1 | 0 | 6-methylprednisolone; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | adrenergic agent; anti-inflammatory drug; antiemetic; environmental contaminant; neuroprotective agent; xenobiotic |
| brompheniramine Brompheniramine: Histamine H1 antagonist used in treatment of allergies, rhinitis, and urticaria.. brompheniramine : Pheniramine in which the hydrogen at position 4 of the phenyl substituent is substituted by bromine. A histamine H1 receptor antagonist, brompheniramine is used (commonly as its maleate salt) for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis. | 3.23 | 1 | 0 | organobromine compound; pyridines | anti-allergic agent; H1-receptor antagonist |
| penicillin v Penicillin V: A broad-spectrum penicillin antibiotic used orally in the treatment of mild to moderate infections by susceptible gram-positive organisms.. phenoxymethylpenicillin : A penicillin compound having a 6beta-(phenoxyacetyl)amino side-chain. | 3.23 | 1 | 0 | penicillin allergen; penicillin | |
| isosorbide dinitrate Isosorbide Dinitrate: A vasodilator used in the treatment of ANGINA PECTORIS. Its actions are similar to NITROGLYCERIN but with a slower onset of action. | 3.23 | 1 | 0 | glucitol derivative; nitrate ester | nitric oxide donor; vasodilator agent |
| pseudoephedrine Pseudoephedrine: A phenethylamine that is an isomer of EPHEDRINE which has less central nervous system effects and usage is mainly for respiratory tract decongestion.. pseudoephedrine : A member of the class of the class of phenylethanolamines that is (1S)-2-(methylamino)-1-phenylethan-1-ol in which the pro-S hydrogen at position 2 is replaced by a methyl group. | 3.23 | 1 | 0 | phenylethanolamines; secondary alcohol; secondary amino compound | anti-asthmatic drug; bronchodilator agent; central nervous system drug; nasal decongestant; plant metabolite; sympathomimetic agent; vasoconstrictor agent; xenobiotic |
| diethylpropion Diethylpropion: A appetite depressant considered to produce less central nervous system disturbance than most drugs in this therapeutic category. It is also considered to be among the safest for patients with hypertension. (From AMA Drug Evaluations Annual, 1994, p2290). diethylpropion : An aromatic ketone that is propiophenone in which one of the hydrogens alpha- to the carbonyl is substituted by a diethylamino group. A central stimulant and indirect-acting sympathomimetic, it is an appetite depressant and is used as the hydrochloride as an anoretic in the short term management of obesity. | 3.23 | 1 | 0 | aromatic ketone; tertiary amine | appetite depressant |
| benzonatate benzonatate: structure in Merck Index, 9th ed, #1107. benzonatate : The ester obtained by formal condensation of 4-butylaminobenzoic acid with nonaethylene glycol monomethyl ether. Structurally related to procaine and benzocaine, it has an anaesthetic effect on the stretch sensors in the lungs, and is used as a non-narcotic cough suppressant. | 3.23 | 1 | 0 | benzoate ester; secondary amino compound; substituted aniline | anaesthetic; antitussive |
| methylergonovine Methylergonovine: A homolog of ERGONOVINE containing one more CH2 group. (Merck Index, 11th ed) | 3.23 | 1 | 0 | ergoline alkaloid | |
| cinchophen cinchophen: was heading 1963-94; ACIPHENOCHINOLIUM was see CHINOPHEN 1978-94; use QUINOLINES to search CINCHOPHEN 1966-94 | 3.23 | 1 | 0 | quinolines | |
| nafcillin Nafcillin: A semi-synthetic antibiotic related to penicillin.. nafcillin : A penicillin in which the substituent at position 6 of the penam ring is a (2-ethoxy-1-naphthoyl)amino group. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| methohexital Methohexital: An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia.. methohexital : A barbiturate, the structure of which is that of barbituric acid substituted at N-1 by a methyl group and at C-5 by allyl and 1-methylpent-2-ynyl groups. | 3.23 | 1 | 0 | acetylenic compound; barbiturates | drug allergen; intravenous anaesthetic |
| ephedrine Ephedrine: A phenethylamine found in EPHEDRA SINICA. PSEUDOEPHEDRINE is an isomer. It is an alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. It has been used for asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It has become less extensively used with the advent of more selective agonists.. (-)-ephedrine : A phenethylamine alkaloid that is 2-phenylethanamine substituted by a methyl group at the amino nitrogen and a methyl and a hydroxy group at position 2 and 1 respectively. | 3.23 | 1 | 0 | phenethylamine alkaloid; phenylethanolamines | bacterial metabolite; environmental contaminant; nasal decongestant; plant metabolite; sympathomimetic agent; vasoconstrictor agent; xenobiotic |
| aminophylline Aminophylline: A drug combination that contains THEOPHYLLINE and ethylenediamine. It is more soluble in water than theophylline but has similar pharmacologic actions. It's most common use is in bronchial asthma, but it has been investigated for several other applications.. aminophylline : A mixture comprising of theophylline and ethylenediamine in a 2:1 ratio. | 3.23 | 1 | 0 | mixture | bronchodilator agent; cardiotonic drug |
| azacitidine Azacitidine: A pyrimidine analogue that inhibits DNA methyltransferase, impairing DNA methylation. It is also an antimetabolite of cytidine, incorporated primarily into RNA. Azacytidine has been used as an antineoplastic agent.. 5-azacytidine : An N-glycosyl-1,3,5-triazine that is 4-amino-1,3,5-triazin-2(1H)-one substituted by a beta-D-ribofuranosyl residue via an N-glycosidic linkage. An antineoplastic agent, it is used in the treatment of myeloid leukaemia. | 3.23 | 1 | 0 | N-glycosyl-1,3,5-triazine; nucleoside analogue | antineoplastic agent |
| galantamine Galantamine: A benzazepine derived from norbelladine. It is found in GALANTHUS and other AMARYLLIDACEAE. It is a cholinesterase inhibitor that has been used to reverse the muscular effects of GALLAMINE TRIETHIODIDE and TUBOCURARINE and has been studied as a treatment for ALZHEIMER DISEASE and other central nervous system disorders.. galanthamine : A benzazepine alkaloid isolated from certain species of daffodils. | 3.23 | 1 | 0 | benzazepine alkaloid fundamental parent; benzazepine alkaloid; organic heterotetracyclic compound; tertiary amino compound | antidote to curare poisoning; cholinergic drug; EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; plant metabolite |
| nandrolone decanoate Nandrolone Decanoate: Decanoic acid ester of nandrolone that is used as an anabolic agent to prevent or treat WASTING SYNDROME associated with severe chronic illness or HIV infection (HIV WASTING SYNDROME). It may also be used in the treatment of POSTMENOPAUSAL OSTEOPOROSIS. | 3.23 | 1 | 0 | steroid ester | |
| dextropropoxyphene Dextropropoxyphene: A narcotic analgesic structurally related to METHADONE. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect.. propoxyphene : A racemate of the (1R,2R)- and (1S,2R)- diastereoisomers.. dextropropoxyphene : The (1S,2R)-(+)-diastereoisomer of propoxyphene. | 3.23 | 1 | 0 | 1-benzyl-3-(dimethylamino)-2-methyl-1-phenylpropyl propanoate | mu-opioid receptor agonist; opioid analgesic |
| chenodeoxycholic acid Chenodeoxycholic Acid: A bile acid, usually conjugated with either glycine or taurine. It acts as a detergent to solubilize fats for intestinal absorption and is reabsorbed by the small intestine. It is used as cholagogue, a choleretic laxative, and to prevent or dissolve gallstones.. chenodeoxycholic acid : A dihydroxy-5beta-cholanic acid that is (5beta)-cholan-24-oic acid substituted by hydroxy groups at positions 3 and 7 respectively.. chenodeoxycholate : Conjugate base of chenodeoxycholic acid; major species at pH 7.3. | 3.23 | 1 | 0 | bile acid; C24-steroid; dihydroxy-5beta-cholanic acid | human metabolite; mouse metabolite |
| 4-hydroxybutyric acid 4-hydroxybutyric acid: was an entry term to Sodium Oxybate (74-98). 4-hydroxybutyric acid : A 4-hydroxy monocarboxylic acid that is butyric acid in which one of the hydrogens at position 4 is replaced by a hydroxy group. | 3.23 | 1 | 0 | 4-hydroxy monocarboxylic acid; hydroxybutyric acid | general anaesthetic; GHB receptor agonist; neurotoxin; sedative |
| dihydroergotamine Dihydroergotamine: A 9,10alpha-dihydro derivative of ERGOTAMINE. It is used as a vasoconstrictor, specifically for the therapy of MIGRAINE DISORDERS.. dihydroergotamine : Ergotamine in which a single bond replaces the double bond between positions 9 and 10. A semisynthetic ergot alkaloid with weaker oxytocic and vasoconstrictor properties than ergotamine, it is used (as the methanesulfonic or tartaric acid salts) for the treatment of migraine and orthostatic hypotension. | 3.23 | 1 | 0 | ergot alkaloid; semisynthetic derivative | dopamine agonist; non-narcotic analgesic; serotonergic agonist; sympatholytic agent; vasoconstrictor agent |
| medroxyprogesterone [no description available] | 3.23 | 1 | 0 | 17alpha-hydroxy steroid; 20-oxo steroid; 3-oxo-Delta(4) steroid; tertiary alpha-hydroxy ketone | contraceptive drug; progestin; synthetic oral contraceptive |
| dimenhydrinate gravinol: has antioxidant and ant-inflammatory activities; structure in first source | 3.23 | 1 | 0 | diarylmethane | |
| methamphetamine Methamphetamine: A central nervous system stimulant and sympathomimetic with actions and uses similar to DEXTROAMPHETAMINE. The smokable form is a drug of abuse and is referred to as crank, crystal, crystal meth, ice, and speed.. methamphetamine : A member of the class of amphetamines in which the amino group of (S)-amphetamine carries a methyl substituent. | 3.23 | 1 | 0 | amphetamines; secondary amine | central nervous system stimulant; environmental contaminant; neurotoxin; psychotropic drug; xenobiotic |
| levocarnitine (R)-carnitine : The (R)-enantiomer of carnitine. | 3.23 | 1 | 0 | carnitine | antilipemic drug; nootropic agent; nutraceutical; Saccharomyces cerevisiae metabolite; water-soluble vitamin (role) |
| sulfanilylurea sulfanilylurea: antimicrobial agent; structure | 3.23 | 1 | 0 | benzenes; sulfonamide | |
| lactulose [no description available] | 3.23 | 1 | 0 | glycosylfructose | gastrointestinal drug; laxative |
| pamabrom [no description available] | 3.23 | 1 | 0 | ||
| acetylcysteine N-acetyl-L-cysteine : An N-acetyl-L-amino acid that is the N-acetylated derivative of the natural amino acid L-cysteine. | 3.23 | 1 | 0 | acetylcysteine; L-cysteine derivative; N-acetyl-L-amino acid | antidote to paracetamol poisoning; antiinfective agent; antioxidant; antiviral drug; ferroptosis inhibitor; geroprotector; human metabolite; mucolytic; radical scavenger; vulnerary |
| erythromycin Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively. | 3.23 | 1 | 0 | cyclic ketone; erythromycin | |
| levonorgestrel Levonorgestrel: A synthetic progestational hormone with actions similar to those of PROGESTERONE and about twice as potent as its racemic or (+-)-isomer (NORGESTREL). It is used for contraception, control of menstrual disorders, and treatment of endometriosis. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound | contraceptive drug; female contraceptive drug; progestin; synthetic oral contraceptive |
| diphenoxylate Diphenoxylate: A MEPERIDINE congener used as an antidiarrheal, usually in combination with ATROPINE. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity.. diphenoxylate : A piperidinecarboxylate ester that is the ethyl ester of difenoxin. | 3.23 | 1 | 0 | ethyl ester; nitrile; piperidinecarboxylate ester; tertiary amine | antidiarrhoeal drug |
| ethambutol Ethambutol: An antitubercular agent that inhibits the transfer of mycolic acids into the cell wall of the tubercle bacillus. It may also inhibit the synthesis of spermidine in mycobacteria. The action is usually bactericidal, and the drug can penetrate human cell membranes to exert its lethal effect. (From Smith and Reynard, Textbook of Pharmacology, 1992, p863). ethambutol : An ethylenediamine derivative that is ethane-1,2-diamine in which one hydrogen attached to each of the nitrogens is sutstituted by a 1-hydroxybutan-2-yl group (S,S-configuration). It is a bacteriostatic antimycobacterial drug, effective against Mycobacterium tuberculosis and some other mycobacteria. It is used (as the dihydrochloride salt) in combination with other antituberculous drugs in the treatment of pulmonary and extrapulmonary tuberculosis; resistant strains of M. tuberculosis are readily produced if ethambutol is used alone. | 3.23 | 1 | 0 | ethanolamines; ethylenediamine derivative | antitubercular agent; environmental contaminant; xenobiotic |
| vancomycin Vancomycin: Antibacterial obtained from Streptomyces orientalis. It is a glycopeptide related to RISTOCETIN that inhibits bacterial cell wall assembly and is toxic to kidneys and the inner ear.. vancomycin : A complex glycopeptide from Streptomyces orientalis. It inhibits a specific step in the synthesis of the peptidoglycan layer in the Gram-positive bacteria Staphylococcus aureus and Clostridium difficile. | 3.23 | 1 | 0 | glycopeptide | antibacterial drug; antimicrobial agent; bacterial metabolite |
| d-alpha tocopherol Vitamin E: A generic descriptor for all TOCOPHEROLS and TOCOTRIENOLS that exhibit ALPHA-TOCOPHEROL activity. By virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus, these compounds exhibit varying degree of antioxidant activity, depending on the site and number of methyl groups and the type of ISOPRENOIDS.. tocopherol : A collective name for a group of closely related lipids that contain a chroman-6-ol nucleus substituted at position 2 by a methyl group and by a saturated hydrocarbon chain consisting of three isoprenoid units. They are designated as alpha-, beta-, gamma-, and delta-tocopherol depending on the number and position of additional methyl substituents on the aromatic ring. Tocopherols occur in vegetable oils and vegetable oil products, almost exclusively with R,R,R configuration. Tocotrienols differ from tocopherols only in having three double bonds in the hydrocarbon chain.. vitamin E : Any member of a group of fat-soluble chromanols that exhibit biological activity against vitamin E deficiency. The vitamers in this class consists of a chroman-6-ol core which is substituted at position 2 by a methyl group and (also at position 2) either a saturated or a triply-unsaturated hydrocarbon chain consisting of three isoprenoid units. The major function of vitamin E is to act as a natural antioxidant by scavenging free radicals and molecular oxygen.. (R,R,R)-alpha-tocopherol : An alpha-tocopherol that has R,R,R configuration. The naturally occurring stereoisomer of alpha-tocopherol, it is found particularly in sunflower and olive oils. | 3.23 | 1 | 0 | alpha-tocopherol | algal metabolite; antiatherogenic agent; anticoagulant; antioxidant; antiviral agent; EC 2.7.11.13 (protein kinase C) inhibitor; immunomodulator; micronutrient; nutraceutical; plant metabolite |
| ibufenac ibufenac: used in the treatment of rheumatism; also possesses antipyretic properties; minor descriptor (75-84); on-line & Index Medicus search PHENYLACETATES (75-84); RN given refers to parent cpd. ibufenac : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is replaced by a 4-isobutylphenyl group. Although it was shown to be effective in treatment of rheumatoid arthritis, the clinical use of ibufenac was discontinued due to hepatotoxic side-effects. | 3.23 | 1 | 0 | monocarboxylic acid | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; hepatotoxic agent; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| metaxalone [no description available] | 3.23 | 1 | 0 | aromatic ether | |
| spectinomycin Spectinomycin: An antibiotic produced by Streptomyces spectabilis. It is active against gram-negative bacteria and used for the treatment of GONORRHEA.. spectinomycin dihydrochloride : A hydrochloride obtained by combining spectinomycin with two molar equivalents of hydrochloric acid. An antibiotic that is active against gram-negative bacteria and used (as its pentahydrate) to treat gonorrhea.. spectinomycin : A pyranobenzodioxin and antibiotic that is active against gram-negative bacteria and used (as its dihydrochloride pentahydrate) to treat gonorrhea. It is produced by the bacterium Streptomyces spectabilis. | 3.23 | 1 | 0 | cyclic acetal; cyclic hemiketal; cyclic ketone; pyranobenzodioxin; secondary alcohol; secondary amino compound | antibacterial drug; antimicrobial agent; bacterial metabolite |
| dronabinol Dronabinol: A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.. Delta(9)-tetrahydrocannabinol : A diterpenoid that is 6a,7,8,10a-tetrahydro-6H-benzo[c]chromene substituted at position 1 by a hydroxy group, positions 6, 6 and 9 by methyl groups and at position 3 by a pentyl group. The principal psychoactive constituent of the cannabis plant, it is used for treatment of anorexia associated with AIDS as well as nausea and vomiting associated with cancer chemotherapy. | 3.23 | 1 | 0 | benzochromene; diterpenoid; phytocannabinoid; polyketide | cannabinoid receptor agonist; epitope; hallucinogen; metabolite; non-narcotic analgesic |
| amiloride Amiloride: A pyrazine compound inhibiting SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with DIURETICS to spare POTASSIUM loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705). amiloride : A member of the class of pyrazines resulting from the formal monoacylation of guanidine with the carboxy group of 3,5-diamino-6-chloropyrazine-2-carboxylic acid. | 3.23 | 1 | 0 | aromatic amine; guanidines; organochlorine compound; pyrazines | diuretic; sodium channel blocker |
| pimozide Pimozide: A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403). pimozide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which one of the nitrogens is substituted by a piperidin-4-yl group, which in turn is substituted on the nitrogen by a 4,4-bis(p-fluorophenyl)butyl group. | 3.23 | 1 | 0 | benzimidazoles; heteroarylpiperidine; organofluorine compound | antidyskinesia agent; dopaminergic antagonist; first generation antipsychotic; H1-receptor antagonist; serotonergic antagonist |
| dexbrompheniramine dexbrompheniramine : The (pharmacologically active) (S)-(+)-enantiomer of brompheniramine. A histamine H1 receptor antagonist, it is used (commonly as its maleate salt) for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis. | 3.23 | 1 | 0 | brompheniramine | anti-allergic agent; H1-receptor antagonist |
| stavudine Stavudine: A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.. stavudine : A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase | 3.23 | 1 | 0 | dihydrofuran; nucleoside analogue; organic molecular entity | antimetabolite; antiviral agent; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| dicloxacillin Dicloxacillin: One of the PENICILLINS which is resistant to PENICILLINASE.. dicloxacillin : A penicillin that is 6-aminopenicillanic acid in which one of the amino hydrogens is replaced by a 3-(2,6-dichlorophenyl)-5-methyl-1,2-oxazol-4-yl]formyl group. | 3.23 | 1 | 0 | dichlorobenzene; penicillin | antibacterial drug |
| megestrol Megestrol: A progestational hormone used most commonly as the acetate ester. As the acetate, it is more potent than progesterone both as a progestagen and as an ovulation inhibitor. It has also been used in the palliative treatment of breast cancer.. megestrol : A 3-oxo Delta(4)-steroid that is pregna-4,6-diene-3,20-dione substituted by a methyl group at position 6 and a hydroxy group at position 17. | 3.23 | 1 | 0 | 17alpha-hydroxy steroid; 20-oxo steroid; 3-oxo-Delta(4) steroid; tertiary alpha-hydroxy ketone | antineoplastic agent; appetite enhancer; contraceptive drug; progestin; synthetic oral contraceptive |
| streptomycin [no description available] | 3.23 | 1 | 0 | antibiotic antifungal drug; antibiotic fungicide; streptomycins | antibacterial drug; antifungal agrochemical; antimicrobial agent; antimicrobial drug; bacterial metabolite; protein synthesis inhibitor |
| cladribine [no description available] | 3.23 | 1 | 0 | organochlorine compound; purine 2'-deoxyribonucleoside | antineoplastic agent; immunosuppressive agent |
| carbenicillin Carbenicillin: Broad-spectrum semisynthetic penicillin derivative used parenterally. It is susceptible to gastric juice and penicillinase and may damage platelet function.. carbenicillin : A penicillin antibiotic having a 6beta-2-carboxy-2-phenylacetamido side-chain. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| clomacran clomacran: RN given refers to parent cpd; structure | 3.23 | 1 | 0 | acridines | |
| methenamine hippurate methenamine hippurate: both parts of molecule contribute to its antibacterial action | 3.23 | 1 | 0 | N-acylglycine | |
| olsalazine olsalazine: cpd with 2 salicylate molecules linked together by an azo bond. olsalazine : An azobenzene that consists of two molecules of 4-aminosalicylic acid joined by an azo linkage. A prodrug for mesalazine, an anti-inflammatory drug, it is used (as the disodium salt) in the treatment of inflammatory bowel disease. | 3.23 | 1 | 0 | azobenzenes; dicarboxylic acid | non-steroidal anti-inflammatory drug; prodrug |
| sodium thiosulfate sodium thiosulfate: do not confuse synonym sodium hyposulfite with sodium hyposulfite, synonym for di-Na salt of dithionous acid. sodium thiosulfate : An inorganic sodium salt composed of sodium and thiosulfate ions in a 2:1 ratio. | 3.23 | 1 | 0 | inorganic sodium salt | antidote to cyanide poisoning; antifungal drug; nephroprotective agent |
| selegiline Selegiline: A selective, irreversible inhibitor of Type B monoamine oxidase that is used for the treatment of newly diagnosed patients with PARKINSON DISEASE, and for the treatment of depressive disorders. The compound without isomeric designation is Deprenyl. | 3.23 | 1 | 0 | selegiline; terminal acetylenic compound | geroprotector |
| clemastine Clemastine: A histamine H1 antagonist used as the hydrogen fumarate in hay fever, rhinitis, allergic skin conditions, and pruritus. It causes drowsiness.. clemastine : 2-[(2R)-1-Methylpyrrolidin-2-yl]ethanol in which the hydrogen of the hydroxy group is substituted by a 1-(4-chlorophenyl)-1-phenylethyl group (R configuration). An antihistamine with antimuscarinic and moderate sedative properties, it is used as its fumarate salt for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin conditions. | 3.23 | 1 | 0 | monochlorobenzenes; N-alkylpyrrolidine | anti-allergic agent; antipruritic drug; H1-receptor antagonist; muscarinic antagonist |
| cephalexin Cephalexin: A semisynthetic cephalosporin antibiotic with antimicrobial activity similar to that of CEPHALORIDINE or CEPHALOTHIN, but somewhat less potent. It is effective against both gram-positive and gram-negative organisms.. cephalexin : A semisynthetic first-generation cephalosporin antibiotic having methyl and beta-(2R)-2-amino-2-phenylacetamido groups at the 3- and 7- of the cephem skeleton, respectively. It is effective against both Gram-negative and Gram-positive organisms, and is used for treatment of infections of the skin, respiratory tract and urinary tract. | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin; semisynthetic derivative | antibacterial drug |
| danazol Danazol: A synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins. It possesses some androgenic properties. Danazol has been used in the treatment of endometriosis and some benign breast disorders. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; terminal acetylenic compound | anti-estrogen; estrogen antagonist; geroprotector |
| fenclozic acid fenclozic acid: an analgesic & antipyretic with anti-inflammatory properties; minor descriptor (75-86); on-line & INDEX MEDICUS search THIAZOLES (75-86); RN given refers to parent cpd | 3.23 | 1 | 0 | ||
| laxagetten 4,4'-diacetoxydiphenylpyridylemethane [no description available] | 3.23 | 1 | 0 | ||
| daunorubicin Daunorubicin: A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of LEUKEMIA and other NEOPLASMS.. anthracycline : Anthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine.. daunorubicin : A natural product found in Actinomadura roseola. | 3.23 | 1 | 0 | aminoglycoside antibiotic; anthracycline; p-quinones; tetracenequinones | antineoplastic agent; bacterial metabolite |
| fludarabine phosphate fludarabine phosphate: structure given in first source. fludarabine phosphate : A purine arabinonucleoside monophosphate having 2-fluoroadenine as the nucleobase. A prodrug, it is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. Once incorporated into DNA, 2-fluoro-ara-ATP functions as a DNA chain terminator. It is used for the treatment of adult patients with B-cell chronic lymphocytic leukemia (CLL) who have not responded to, or whose disease has progressed during, treatment with at least one standard alkylating-agent containing regimenas. | 3.23 | 1 | 0 | nucleoside analogue; organofluorine compound; purine arabinonucleoside monophosphate | antimetabolite; antineoplastic agent; antiviral agent; DNA synthesis inhibitor; immunosuppressive agent; prodrug |
| alclofenac alclofenac: was heading 1975-94 (was see under PHENYLACETATES 1975-90); use PHENYLACETATES to search ALCLOFENAC 1975-94; an anti-inflammatory agent used in the treatment of rheumatoid arthritis; acts also as an analgesic and an antipyretic. alclofenac : An aromatic ether in which the ether oxygen links an allyl group to the 4-position of (3-chlorophenyl)acetic acid.A non-steroidal anti-inflammatory drug, it was withdrawn from the UK market in 1979 due to concerns with its association with vasculitis and rash. | 3.23 | 1 | 0 | aromatic ether; monocarboxylic acid; monochlorobenzenes | drug allergen; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| bromocriptine Bromocriptine: A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion. | 3.23 | 1 | 0 | indole alkaloid | antidyskinesia agent; antiparkinson drug; dopamine agonist; hormone antagonist |
| oxyphenisatin [no description available] | 3.23 | 1 | 0 | indoles | |
| fludrocortisone Fludrocortisone: A synthetic mineralocorticoid with anti-inflammatory activity. | 3.23 | 1 | 0 | 11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid; fluorinated steroid; mineralocorticoid | adrenergic agent; anti-inflammatory drug |
| ursodeoxycholic acid Ursodeoxycholic Acid: An epimer of chenodeoxycholic acid. It is a mammalian bile acid found first in the bear and is apparently either a precursor or a product of chenodeoxycholate. Its administration changes the composition of bile and may dissolve gallstones. It is used as a cholagogue and choleretic.. ursodeoxycholic acid : A bile acid found in the bile of bears (Ursidae) as a conjugate with taurine. Used therapeutically, it prevents the synthesis and absorption of cholesterol and can lead to the dissolution of gallstones.. ursodeoxycholate : A bile acid anion that is the conjugate base of ursodeoxycholic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3. | 3.23 | 1 | 0 | bile acid; C24-steroid; dihydroxy-5beta-cholanic acid | human metabolite; mouse metabolite |
| dexchlorpheniramine dexchlorpheniramine: RN given refers to parent cpd(S)-isomer | 3.23 | 1 | 0 | chlorphenamine | |
| clometacin clometacin: structure | 3.23 | 1 | 0 | N-acylindole | |
| cefazolin Cefazolin: A semisynthetic cephalosporin analog with broad-spectrum antibiotic action due to inhibition of bacterial cell wall synthesis. It attains high serum levels and is excreted quickly via the urine.. cefazolin : A first-generation cephalosporin compound having [(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]methyl and (1H-tetrazol-1-ylacetyl)amino side-groups at positions 3 and 7 respectively. | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin; tetrazoles; thiadiazoles | antibacterial drug |
| amoxicillin Amoxicillin: A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.. amoxicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-(4-hydroxyphenyl)acetamido group. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| timolol (S)-timolol (anhydrous) : The (S)-(-) (more active) enantiomer of timolol. A beta-adrenergic antagonist, both the hemihydrate and the maleate salt are used in the mangement of glaucoma, hypertension, angina pectoris and myocardial infarction, and for the prevention of migraine. | 3.23 | 1 | 0 | timolol | anti-arrhythmia drug; antiglaucoma drug; antihypertensive agent; beta-adrenergic antagonist |
| oxcarbazepine Oxcarbazepine: A carbamazepine derivative that acts as a voltage-gated sodium channel blocker. It is used for the treatment of PARTIAL SEIZURES with or without secondary generalization. It is also an inducer of CYTOCHROME P-450 CYP3A4.. oxcarbazepine : A dibenzoazepine derivative, having a carbamoyl group at the ring nitrogen, substituted with an oxo group at C-4 of the azepeine ring which is also hydrogenated at C-4 and C-5. It is a anticholinergic anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy. | 3.23 | 1 | 0 | cyclic ketone; dibenzoazepine | anticonvulsant; drug allergen |
| carbidopa carbidopa (anhydrous) : 3-(3,4-Dihydroxyphenyl)propanoic acid in which the hydrogens alpha- to the carboxyl group are substituted by hydrazinyl and methyl groups (S-configuration). Carbidopa is a dopa decarboxylase inhibitor, so prevents conversion of levodopa to dopamine. It has no antiparkinson activity by itself, but is used (commonly as its hydrate) in the management of Parkinson's disease to reduce peripheral adverse effects of levodopa. | 3.23 | 1 | 0 | catechols; hydrazines; monocarboxylic acid | antiparkinson drug; dopaminergic agent; EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor |
| moricizine Moricizine: An antiarrhythmia agent used primarily for ventricular rhythm disturbances.. moricizine : A phenothiazine substituted on the nitrogen by a 3-(morpholin-4-yl)propanoyl group, and at position 2 by an (ethoxycarbonyl)amino group. | 3.23 | 1 | 0 | carbamate ester; morpholines; phenothiazines | anti-arrhythmia drug |
| amineptin amineptin: used in treatment of neuroses with psychoasthenic, anxio-phobic & depressive manifestations; synonym S 1694 refers to HCl; structure. amineptine : A carbocyclic fatty acid that is 5-aminoheptanoic acid in which one of the hydrogens attached to the nitrogen is replaced by a 10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-yl group. A tricyclic antidepressant, it was never approved in the US and was withdrawn from the French market in 1999 due to concerns over abuse, dependence and severe acne. | 3.23 | 1 | 0 | amino acid; carbocyclic fatty acid; carbotricyclic compound; secondary amino compound | antidepressant; dopamine uptake inhibitor |
| zidovudine Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.. zidovudine : A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase. | 3.23 | 1 | 0 | azide; pyrimidine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; HIV-1 reverse transcriptase inhibitor |
| pirprofen pirprofen: anti-inflammatory agent used in therapy of rheumatoid arthritis; prostaglandin synthetase inhibitor; more potent than indomethacin; structure | 3.23 | 1 | 0 | pyrroline | |
| paclitaxel Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL). | 3.23 | 1 | 0 | taxane diterpenoid; tetracyclic diterpenoid | antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent |
| etoposide [no description available] | 3.23 | 1 | 0 | beta-D-glucoside; furonaphthodioxole; organic heterotetracyclic compound | antineoplastic agent; DNA synthesis inhibitor |
| dobutamine Dobutamine: A catecholamine derivative with specificity for BETA-1 ADRENERGIC RECEPTORS. It is commonly used as a cardiotonic agent after CARDIAC SURGERY and during DOBUTAMINE STRESS ECHOCARDIOGRAPHY.. dobutamine : A catecholamine that is 4-(3-aminobutyl)phenol in which one of the hydrogens attached to the nitrogen is substituted by a 2-(3,4-dihydroxyphenyl)ethyl group. A beta1-adrenergic receptor agonist that has cardiac stimulant action without evoking vasoconstriction or tachycardia, it is used as the hydrochloride to increase the contractility of the heart in the management of acute heart failure. | 3.23 | 1 | 0 | catecholamine; secondary amine | beta-adrenergic agonist; cardiotonic drug; sympathomimetic agent |
| penbutolol Penbutolol: A nonselective beta-blocker used as an antihypertensive and an antianginal agent. | 3.23 | 1 | 0 | ethanolamines | |
| ribavirin Rebetron: Rebetron is tradename | 3.23 | 1 | 0 | 1-ribosyltriazole; aromatic amide; monocarboxylic acid amide; primary carboxamide | anticoronaviral agent; antiinfective agent; antimetabolite; antiviral agent; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| amikacin Amikacin: A broad-spectrum antibiotic derived from KANAMYCIN. It is reno- and oto-toxic like the other aminoglycoside antibiotics.. amikacin : An amino cyclitol glycoside that is kanamycin A acylated at the N-1 position by a 4-amino-2-hydroxybutyryl group. | 3.23 | 1 | 0 | alpha-D-glucoside; amino cyclitol glycoside; aminoglycoside; carboxamide | antibacterial drug; antimicrobial agent; nephrotoxin |
| cephradine Cephradine: A semi-synthetic cephalosporin antibiotic.. cephradine : A first-generation cephalosporin antibiotic with a methyl substituent at position 3, and a (2R)-2-amino-2-cyclohexa-1,4-dien-1-ylacetamido substituent at position 7, of the cephem skeleton. | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin | antibacterial drug |
| ticrynafen Ticrynafen: A novel diuretic with uricosuric action. It has been proposed as an antihypertensive agent.. tienilic acid : An aromatic ketone that is 2,3-dichlorophenoxyacetic acid in which the hydrogen at position 4 on the benzene ring is replaced by a thiophenecarbonyl group. A loop diuretic used to treat hypertension, it was withdrawn from the market in 1982 due to links with hepatitis. | 3.23 | 1 | 0 | aromatic ether; aromatic ketone; dichlorobenzene; monocarboxylic acid; thiophenes | antihypertensive agent; hepatotoxic agent; loop diuretic |
| methyldopa Methyldopa: An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent.. alpha-methyl-L-dopa : A derivative of L-tyrosine having a methyl group at the alpha-position and an additional hydroxy group at the 3-position on the phenyl ring. | 3.23 | 1 | 0 | L-tyrosine derivative; non-proteinogenic L-alpha-amino acid | alpha-adrenergic agonist; antihypertensive agent; hapten; peripheral nervous system drug; sympatholytic agent |
| diltiazem Diltiazem: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.. diltiazem : A 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate in which both stereocentres have S configuration. A calcium-channel blocker and vasodilator, it is used as the hydrochloride in the management of angina pectoris and hypertension. | 3.23 | 1 | 0 | 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate | antihypertensive agent; calcium channel blocker; vasodilator agent |
| vecuronium vecuronium : A 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidino- and 16beta-N-methylpiperidinium substituents. | 3.23 | 1 | 0 | acetate ester; androstane; quaternary ammonium ion | drug allergen; muscle relaxant; neuromuscular agent; nicotinic antagonist |
| benoxaprofen benoxaprofen: RN given refers to parent cpd; structure. benoxaprofen : A monocarboxylic acid that is propionic acid substituted at position 2 by a 2-(4-chlorophenyl)-1,3-benzoxazol-5-yl group. It was used as a non-steroidal anti-inflammatory drug until 1982 when it was withdrawn from the market due to adverse side-effects including liver necrosis, photosensitivity, and carcinogenicity in animals. | 3.23 | 1 | 0 | 1,3-benzoxazoles; monocarboxylic acid; monochlorobenzenes | antipsoriatic; antipyretic; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; hepatotoxic agent; nephrotoxin; non-narcotic analgesic; non-steroidal anti-inflammatory drug; protein kinase C agonist |
| exifone [no description available] | 3.23 | 1 | 0 | benzophenones | |
| mefloquine (-)-(11S,2'R)-erythro-mefloquine : An optically active form of [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol having (-)-(11S,2'R)-erythro-configuration. An antimalarial agent, used in racemic form, which acts as a blood schizonticide; its mechanism of action is unknown. | 3.23 | 1 | 0 | [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol | antimalarial |
| nitazoxanide nitazoxanide: a 5-nitrothiazolyl derivative used for a broad range of intestinal parasitic infections including CRYPTOSPORIDIUM and GIARDIA; it is a redox-active nitrothiazolyl-salicylamide prodrug | 3.23 | 1 | 0 | benzamides; carboxylic ester | |
| sufentanil Sufentanil: An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent.. sufentanil : An anilide resulting from the formal condensation of the aryl amino group of 4-(methoxymethyl)-N-phenyl-1-[2-(2-thienyl)ethyl]piperidin-4-amine with propanoic acid. | 3.23 | 1 | 0 | anilide; ether; piperidines; thiophenes | anaesthesia adjuvant; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic |
| acarbose [no description available] | 3.23 | 1 | 0 | tetrasaccharide derivative | EC 3.2.1.1 (alpha-amylase) inhibitor; EC 3.2.1.20 (alpha-glucosidase) inhibitor; geroprotector; hypoglycemic agent |
| torsemide Torsemide: A pyridine and sulfonamide derivative that acts as a sodium-potassium chloride symporter inhibitor (loop diuretic). It is used for the treatment of EDEMA associated with CONGESTIVE HEART FAILURE; CHRONIC RENAL INSUFFICIENCY; and LIVER DISEASES. It is also used for the management of HYPERTENSION.. torasemide : An N-sulfonylurea obtained by formal condensation of [(3-methylphenyl)amino]pyridine-3-sulfonic acid with the free amino group of N-isopropylurea. It is a potent loop diuretic used for the treatment of hypertension and edema in patients with congestive heart failure. | 3.23 | 1 | 0 | aminopyridine; N-sulfonylurea; secondary amino compound | antihypertensive agent; loop diuretic |
| epirubicin Epirubicin: An anthracycline which is the 4'-epi-isomer of doxorubicin. The compound exerts its antitumor effects by interference with the synthesis and function of DNA. | 3.23 | 1 | 0 | aminoglycoside; anthracycline antibiotic; anthracycline; deoxy hexoside; monosaccharide derivative; p-quinones; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | antimicrobial agent; antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor |
| idarubicin Idarubicin: An orally administered anthracycline antineoplastic. The compound has shown activity against BREAST NEOPLASMS; LYMPHOMA; and LEUKEMIA. | 3.23 | 1 | 0 | anthracycline antibiotic; deoxy hexoside; monosaccharide derivative | |
| piperacillin Piperacillin: Semisynthetic, broad-spectrum, AMPICILLIN derived ureidopenicillin antibiotic proposed for PSEUDOMONAS infections. It is also used in combination with other antibiotics.. piperacillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-[(4-ethyl-2,3-dioxopiperazin-1-yl)carboxamido]-2-phenylacetamido group. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| paroxetine Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.. paroxetine : A benzodioxole that consists of piperidine bearing 1,3-benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively; the (3S,4R)-diastereomer. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo. | 3.23 | 1 | 0 | aromatic ether; benzodioxoles; organofluorine compound; piperidines | antidepressant; anxiolytic drug; hepatotoxic agent; P450 inhibitor; serotonin uptake inhibitor |
| captopril Captopril: A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.. captopril : A L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group. It is used as an anti-hypertensive ACE inhibitor drug. | 3.23 | 1 | 0 | alkanethiol; L-proline derivative; N-acylpyrrolidine; pyrrolidinemonocarboxylic acid | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| cefoperazone Cefoperazone: Semisynthetic broad-spectrum cephalosporin with a tetrazolyl moiety that is resistant to beta-lactamase. It may be used to treat Pseudomonas infections.. cefoperazone : A semi-synthetic parenteral cephalosporin with a tetrazolyl moiety that confers beta-lactamase resistance. | 3.23 | 1 | 0 | cephalosporin | antibacterial drug |
| atracurium Atracurium: A non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.. atracurium : A diester compound consisting of pentane-1,5-diol with both hydroxyls bearing 3-[1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-2-methyl-3,4-dihydroisoquinolinium-2(1H)-yl]propanoyl groups. | 3.23 | 1 | 0 | diester; quaternary ammonium ion | muscle relaxant; nicotinic antagonist |
| pergolide Pergolide: A long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES.. pergolide : A diamine that is ergoline in which the beta-hydrogen at position 8 is replaced by a (methylthio)methyl group and the hydrogen attached to the piperidine nitrogen (position 6) is replaced by a propyl group. A dopamine D2 receptor agonist which also has D1 and D2 agonist properties, it is used as the mesylate salt in the management of Parkinson's disease, although it was withdrawn from the U.S. and Canadian markets in 2007 due to an increased risk of cardiac valve dysfunction. | 3.23 | 1 | 0 | diamine; methyl sulfide; organic heterotetracyclic compound | antiparkinson drug; dopamine agonist |
| cefadroxil anhydrous Cefadroxil: Long-acting, broad-spectrum, water-soluble, CEPHALEXIN derivative.. cefadroxil : A cephalosporin bearing methyl and (2R)-2-amino-2-(4-hydroxyphenyl)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. | 3.23 | 1 | 0 | cephalosporin | antibacterial drug |
| fialuridine [no description available] | 3.23 | 1 | 0 | ||
| cefaclor anhydrous Cefaclor: Semisynthetic, broad-spectrum antibiotic derivative of CEPHALEXIN.. cefaclor : A cephalosporin bearing chloro and (R)-2-amino-2-phenylacetamido groups at positions 3 and 7, respectively, of the cephem skeleton. | 3.23 | 1 | 0 | cephalosporin | antibacterial drug; drug allergen |
| alfentanil Alfentanil: A short-acting opioid anesthetic and analgesic derivative of FENTANYL. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients.. alfentanil : A member of the class of piperidines that is piperidine having a 2-(4-ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl group at the 1-position as well as N-phenylpropanamido- and methoxymethyl groups at the 4-position. | 3.23 | 1 | 0 | monocarboxylic acid amide; piperidines | central nervous system depressant; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic; peripheral nervous system drug |
| miglustat miglustat: a glucosylceramide synthase inhibitor. miglustat : A hydroxypiperidine that is deoxynojirimycin in which the amino hydrogen is replaced by a butyl group. | 3.23 | 1 | 0 | piperidines; tertiary amino compound | anti-HIV agent; EC 2.4.1.80 (ceramide glucosyltransferase) inhibitor |
| haloperidol decanoate [no description available] | 3.23 | 1 | 0 | organic molecular entity | |
| cefotetan Cefotetan: A semisynthetic cephamycin antibiotic that is administered intravenously or intramuscularly. The drug is highly resistant to a broad spectrum of beta-lactamases and is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative microorganisms.. cefotetan : A semi-synthetic second-generation cephamycin antibiotic with [(1-methyl-1H-tetrazol-5-yl)sulfanyl]methyl, methoxy and {[4-(2-amino-1-carboxy-2-oxoethylidene)-1,3-dithietan-2-yl]carbonyl}amino groups at the 3, 7alpha, and 7beta positions, respectively, of the cephem skeleton. It is resistant to a wide range of beta-lactamases and is active against a broad spectrum of aerobic and anaerobic Gram-positive and Gram-negative microorganisms. | 3.23 | 1 | 0 | ||
| lovastatin Lovastatin: A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver.. lovastatin : A fatty acid ester that is mevastatin carrying an additional methyl group on the carbobicyclic skeleton. It is used in as an anticholesteremic drug and has been found in fungal species such as Aspergillus terreus and Pleurotus ostreatus (oyster mushroom). | 3.23 | 1 | 0 | delta-lactone; fatty acid ester; hexahydronaphthalenes; polyketide; statin (naturally occurring) | anticholesteremic drug; antineoplastic agent; Aspergillus metabolite; prodrug |
| tolrestat tolrestat: RN & structure given in first source | 3.23 | 1 | 0 | naphthalenes | EC 1.1.1.21 (aldehyde reductase) inhibitor |
| simvastatin Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug. | 3.23 | 1 | 0 | delta-lactone; fatty acid ester; hexahydronaphthalenes; statin (semi-synthetic) | EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor; EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor; ferroptosis inducer; geroprotector; prodrug |
| balsalazide balsalazide: a mesalamine 5-aminosalicylate prodrug; 99% of ingested drug remains intact through the stomach and is delivered to and activated in the colon; used for inflammatory bowel disease, ulcerative colitis and radiation-induced proctosigmoiditis but avoided in patients with known hypersensitivity reaction to salicylates or mesalamine; structure in first source. balsalazide : A monohydroxybenzoic acid consisting of 5-aminosalicylic acid (mesalazine) linked to 4-aminobenzoyl-beta-alanine via an azo bond. | 3.23 | 1 | 0 | ||
| pravastatin Pravastatin: An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).. pravastatin : A carboxylic ester resulting from the formal condensation of (S)-2-methylbutyric acid with the hydroxy group adjacent to the ring junction of (3R,5R)-7-[(1S,2S,6S,8S,8aR)-6,8-dihydroxy-2-methyl-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid. Derived from microbial transformation of mevastatin, pravastatin is a reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA). The sodium salt is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin. | 3.23 | 1 | 0 | 3-hydroxy carboxylic acid; carbobicyclic compound; carboxylic ester; hydroxy monocarboxylic acid; secondary alcohol; statin (semi-synthetic) | anticholesteremic drug; environmental contaminant; metabolite; xenobiotic |
| cabergoline Cabergoline: An ergoline derivative and dopamine D2-agonist that inhibits PROLACTIN secretion. It is used in the management of HYPERPROLACTINEMIA, and to suppress lactation following childbirth for medical reasons. Cabergoline is also used in the management of PARKINSON DISEASE.. cabergoline : An N-acylurea that is (8R)-ergoline-8-carboxamide in which the hydrogen attached to the piperidine nitrogen (position 6) is substituted by an allyl group and the hydrogens attached to the carboxamide nitrogen are substituted by a 3-(dimethylamino)propyl group and an N-ethylcarbamoyl group. A dopamine D2 receptor agonist, cabergoline is used in the management of Parkinson's disease and of disorders associated with hyperprolactinaemia. | 3.23 | 1 | 0 | N-acylurea | antineoplastic agent; antiparkinson drug; dopamine agonist |
| atomoxetine atomoxetine : A secondary amino compound having methyl and 3-(2-methylphenoxy)-3-phenylpropan-1-yl substituents. | 3.23 | 1 | 0 | aromatic ether; secondary amino compound; toluenes | adrenergic uptake inhibitor; antidepressant; environmental contaminant; xenobiotic |
| quinapril Quinapril: A tetrahydroisoquinoline derivative and ANGIOTENSIN CONVERTING ENZYME inhibitor that is used in the treatment of HYPERTENSION and HEART FAILURE.. quinapril : A member of the class of isoquinolines that is (3S)-2-L-alanyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid in which the alpha-amino group of the alanyl residue has been substituted by a 1-ethoxycarbonyl-4-phenylbutan-2-yl group (the all-S isomer). A prodrug for quinaprilat (by hydrolysis of the ethyl ester to the corresponding carboxylic acid), it is used as an angiotensin-converting enzyme inhibitor (ACE inhibitor) used (generally as the hydrochloride salt) for the treatment of hypertension and congestive heart failure. | 3.23 | 1 | 0 | dicarboxylic acid monoester; ethyl ester; isoquinolines; tertiary carboxamide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug |
| alpidem [no description available] | 3.23 | 1 | 0 | imidazoles | |
| mifepristone Mifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME. | 3.23 | 1 | 0 | 3-oxo-Delta(4) steroid; acetylenic compound; tertiary amino compound | abortifacient; contraceptive drug; hormone antagonist; synthetic oral contraceptive |
| fosphenytoin fosphenytoin: structure given in first & second source | 3.23 | 1 | 0 | imidazolidine-2,4-dione | |
| ranolazine Ranolazine: An acetanilide and piperazine derivative that functions as a SODIUM CHANNEL BLOCKER and prevents the release of enzymes during MYOCARDIAL ISCHEMIA. It is used in the treatment of ANGINA PECTORIS.. N-(2,6-dimethylphenyl)-2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetamide : An aromatic amide obtained by formal condensation of the carboxy group of 2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetic acid with the amino group of 2,6-dimethylaniline.. ranolazine : A racemate comprising equal amounts of (R)- and (S)-ranolazine. Used for treatment of chronic angina. | 3.23 | 1 | 0 | aromatic amide; monocarboxylic acid amide; monomethoxybenzene; N-alkylpiperazine; secondary alcohol | |
| finasteride Finasteride: An orally active 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE inhibitor. It is used as a surgical alternative for treatment of benign PROSTATIC HYPERPLASIA.. finasteride : An aza-steroid that is a synthetic drug for the treatment of benign prostatic hyperplasia. | 3.23 | 1 | 0 | 3-oxo steroid; aza-steroid; delta-lactam | androgen antagonist; antihyperplasia drug; EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor |
| esmolol methyl 3-{4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl}propanoate : A methyl ester that is methyl 3-(4-hydroxyphenyl)propanoate in which the hydrogen attached to the phenolic hydroxy group is substituted by a 2-hydroxy-3-(isopropylamino)propyl group.. esmolol : A racemate comprising equimolar amounts of (R)- and (S)-esmolol. A cardioselective and short-acting beta1 receptor blocker with rapid onset but lacking intrinsic sympathomimetic and membrane-stabilising properties, it is used as the hydrochloride salt in the management of supraventricular arrhythmias, and for the control of hypertension and tachycardia during surgery. While the S enantiomer possesses all of the heart rate control, both enantiomers contribute to lowering blood pressure. | 3.23 | 1 | 0 | aromatic ether; ethanolamines; methyl ester; secondary alcohol; secondary amino compound | |
| adefovir adefovir: inhibitor of African swine fever virus. adefovir(1-) : A organophosphonate oxoanion obtained by removal of a proton from the phosphonate group of adefovir, a nucleoside reverse transcriptase inhibitor. It is the major microspecies at pH 7.3 (according to Marvin v 6.2.0.).. adefovir : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens has been replaced by a 2-(6-amino-9H-purin-9-yl)ethoxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(t-butoxycarbonyloxymethyl) ester (dipivoxil ester) prodrug is used to treat chronic hepatitis B viral infection. | 3.23 | 1 | 0 | 6-aminopurines; ether; phosphonic acids | antiviral drug; DNA synthesis inhibitor; drug metabolite; HIV-1 reverse transcriptase inhibitor; nephrotoxic agent |
| aromasil [no description available] | 3.23 | 1 | 0 | 17-oxo steroid; 3-oxo-Delta(1),Delta(4)-steroid | antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor; environmental contaminant; xenobiotic |
| zileuton [no description available] | 3.23 | 1 | 0 | 1-benzothiophenes; ureas | anti-asthmatic drug; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; ferroptosis inhibitor; leukotriene antagonist; non-steroidal anti-inflammatory drug |
| clopidogrel Clopidogrel: A ticlopidine analog and platelet purinergic P2Y receptor antagonist that inhibits adenosine diphosphate-mediated PLATELET AGGREGATION. It is used to prevent THROMBOEMBOLISM in patients with ARTERIAL OCCLUSIVE DISEASES; MYOCARDIAL INFARCTION; STROKE; or ATRIAL FIBRILLATION.. clopidogrel : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group, the methylene hydrogen of which is replaced by a methoxycarbonyl group (the S enantiomer). A P2Y12 receptor antagonist, it is used to inhibit blood clots and prevent heart attacks. | 3.23 | 1 | 0 | methyl ester; monochlorobenzenes; thienopyridine | anticoagulant; P2Y12 receptor antagonist; platelet aggregation inhibitor |
| cidofovir anhydrous Cidofovir: An acyclic nucleoside phosphonate that acts as a competitive inhibitor of viral DNA polymerases. It is used in the treatment of RETINITIS caused by CYTOMEGALOVIRUS INFECTIONS and may also be useful for treating HERPESVIRUS INFECTIONS.. cidofovir anhydrous : Cytosine substituted at the 1 position by a 3-hydroxy-2-(phosphonomethoxy)propyl group (S configuration). A nucleoside analogue, it is an injectable antiviral used for the treatment of cytomegalovirus (CMV) retinitis in AIDS patients. | 3.23 | 1 | 0 | phosphonic acids; pyrimidone | anti-HIV agent; antineoplastic agent; antiviral drug; photosensitizing agent |
| tiagabine Tiagabine: A nipecotic acid derivative that acts as a GABA uptake inhibitor and anticonvulsant agent. It is used in the treatment of EPILEPSY, for refractory PARTIAL SEIZURES.. tiagabine : A piperidinemonocarboxylic acid that is (R)-nipecotic acid in which the hydrogen attached to the nitrogen has been replaced by a 1,1-bis(3-methyl-2-thienyl)but-1-en-4-yl group. A GABA reuptake inhibitor, it is used (generally as the hydrochloride salt) for the treatment of epilepsy. | 3.23 | 1 | 0 | beta-amino acid; piperidinemonocarboxylic acid; tertiary amino compound; thiophenes | anticonvulsant; GABA reuptake inhibitor |
| topotecan Topotecan: An antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA TOPOISOMERASES, TYPE I.. topotecan : A pyranoindolizinoquinoline used as an antineoplastic agent. It is a derivative of camptothecin and works by binding to the topoisomerase I-DNA complex and preventing religation of these 328 single strand breaks. | 3.23 | 1 | 0 | pyranoindolizinoquinoline | antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor |
| bromfenac bromfenac: bromfenac sodium is the active cpd; structure in first source. bromfenac : Amfenac in which the the hydrogen at the 4 position of the benzoyl group is substituted by bromine. It is used for the management of ocular pain and treatment of postoperative inflammation in patients who have undergone cataract extraction. It was withdrawn from the US market in 1998, following concerns over off-label abuse and hepatic failure. | 3.23 | 1 | 0 | aromatic amino acid; benzophenones; organobromine compound; substituted aniline | non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| gemcitabine gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer. | 3.23 | 1 | 0 | organofluorine compound; pyrimidine 2'-deoxyribonucleoside | antimetabolite; antineoplastic agent; antiviral drug; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; environmental contaminant; immunosuppressive agent; photosensitizing agent; prodrug; radiosensitizing agent; xenobiotic |
| ibutilide ibutilide: RN & structure in first source; RN refers to the fumarate salt | 3.23 | 1 | 0 | benzenes; organic amino compound | |
| aripiprazole Aripiprazole: A piperazine and quinolone derivative that is used primarily as an antipsychotic agent. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A. It is used for the treatment of SCHIZOPHRENIA and BIPOLAR DISORDER, and as an adjunct therapy for the treatment of depression.. aripiprazole : An N-arylpiperazine that is piperazine substituted by a 4-[(2-oxo-1,2,3,4-tetrahydroquinolin-7-yl)oxy]butyl group at position 1 and by a 2,3-dichlorophenyl group at position 4. It is an antipsychotic drug used for the treatment of Schizophrenia, and other mood disorders. | 3.23 | 1 | 0 | aromatic ether; delta-lactam; dichlorobenzene; N-alkylpiperazine; N-arylpiperazine; quinolone | drug metabolite; H1-receptor antagonist; second generation antipsychotic; serotonergic agonist |
| remifentanil Remifentanil: A piperidine-propionate derivative and opioid analgesic structurally related to FENTANYL. It functions as a short-acting MU OPIOID RECEPTOR agonist, and is used as an analgesic during induction or maintenance of general anesthesia, following surgery, during childbirth, and in mechanically ventilated patients under intensive care.. remifentanil : A piperidinecarboxylate ester that is methyl piperidine-4-carboxylate in which the hydrogen attached to the nitrogen is substituted by a 3-methoxy-3-oxopropyl group and the hydrogen at position 4 is substituted the nitrogen of N-propanoylaniline. | 3.23 | 1 | 0 | alpha-amino acid ester; anilide; monocarboxylic acid amide; piperidinecarboxylate ester | intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic; sedative |
| atorvastatin [no description available] | 3.23 | 1 | 0 | aromatic amide; dihydroxy monocarboxylic acid; monofluorobenzenes; pyrroles; statin (synthetic) | environmental contaminant; xenobiotic |
| lamivudine [no description available] | 3.23 | 1 | 0 | monothioacetal; nucleoside analogue; oxacycle; primary alcohol | allergen; anti-HBV agent; antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor; HIV-1 reverse transcriptase inhibitor; prodrug |
| duloxetine [no description available] | 3.23 | 1 | 0 | duloxetine | |
| irinotecan [no description available] | 3.23 | 1 | 0 | carbamate ester; delta-lactone; N-acylpiperidine; pyranoindolizinoquinoline; ring assembly; tertiary alcohol; tertiary amino compound | antineoplastic agent; apoptosis inducer; EC 5.99.1.2 (DNA topoisomerase) inhibitor; prodrug |
| valsartan Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.. valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity. | 3.23 | 1 | 0 | biphenylyltetrazole; monocarboxylic acid amide; monocarboxylic acid | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| ibandronic acid Ibandronic Acid: Aminobisphosphonate that is a potent inhibitor of BONE RESORPTION. It is used in the treatment of HYPERCALCEMIA associated with malignancy, for the prevention of fracture and bone complications in patients with breast cancer and bone metastases, and for the treatment and prevention of POSTMENOPAUSAL OSTEOPOROSIS. | 3.23 | 1 | 0 | ||
| ziprasidone ziprasidone: a benzisothiazoylpiperazine derivative; has combined dopamine and serotonin receptor antagonist activity; structurally related to tiospirone. ziprasidone : A piperazine compound having 1,2-benzothiazol-3-yl- and 2-(6-chloro-1,3-dihydro-2-oxindol-5-yl)ethyl substituents attached to the nitrogen atoms. | 3.23 | 1 | 0 | 1,2-benzisothiazole; indolones; organochlorine compound; piperazines | antipsychotic agent; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; psychotropic drug; serotonergic antagonist |
| zolmitriptan zolmitriptan: an antimigraine compound; a serotonin (5HT)-1D receptor agonist. zolmitriptan : A member of the class of tryptamines that is N,N-dimethyltryptamine in which the hydrogen at position 5 of the indole ring has been replaced by a [(4S)-2-oxo-1,3-oxazolidin-4-yl]methyl group. A serotonin 5-HT1 B and D receptor agonist, it is used for the treatment of migraine. | 3.23 | 1 | 0 | oxazolidinone; tryptamines | anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| emtricitabine Emtricitabine: A deoxycytidine analog and REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B viruses. It is used to treat HIV INFECTIONS.. emtricitabine : An organofluorine compound that is 5-fluorocytosine substituted at the 1 position by a 2-(hydroxymethyl)-1,3-oxathiolan-5-yl group (2R,5S configuration). It is used in combination therapy for the treatment of HIV-1 infection. | 3.23 | 1 | 0 | monothioacetal; nucleoside analogue; organofluorine compound; pyrimidone | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| tasosartan tasosartan: angiotensin II antagonist; structure given in first source | 3.23 | 1 | 0 | biphenyls | |
| tiludronic acid tiludronic acid: a bone resorption inhibitor; an antihypercalcemic agent; used in the tratment of Paget's disease; used in the treatment and prevention of osteoporosis; structure given in first source | 3.23 | 1 | 0 | organochlorine compound | |
| tirofiban Tirofiban: Tyrosine analog and PLATELET GLYCOPROTEIN GPIIB-IIIA COMPLEX antagonist that inhibits PLATELET AGGREGATION and is used in the treatment of ACUTE CORONARY SYNDROME.. tirofiban : A member of the class of piperidines that is L-tyrosine in which a hydrogen attached to the amino group is replaced by a butylsulfonyl group and in which the hydrogen attached to the phenolic hydroxy group is replaced by a 4-(piperidin-4-yl)butyl group. | 3.23 | 1 | 0 | L-tyrosine derivative; piperidines; sulfonamide | anticoagulant; fibrin modulating drug; platelet glycoprotein-IIb/IIIa receptor antagonist |
| capecitabine Capecitabine: A deoxycytidine derivative and fluorouracil PRODRUG that is used as an ANTINEOPLASTIC ANTIMETABOLITE in the treatment of COLON CANCER; BREAST CANCER and GASTRIC CANCER.. capecitabine : A carbamate ester that is cytidine in which the hydrogen at position 5 is replaced by fluorine and in which the amino group attached to position 4 is converted into its N-(penyloxy)carbonyl derivative. Capecitabine is a antineoplastic agent used in the treatment of cancers. | 3.23 | 1 | 0 | carbamate ester; cytidines; organofluorine compound | antimetabolite; antineoplastic agent; prodrug |
| adenosine quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit | 3.23 | 1 | 0 | adenosines; purines D-ribonucleoside | analgesic; anti-arrhythmia drug; fundamental metabolite; human metabolite; vasodilator agent |
| trovafloxacin trovafloxacin: a trifluoronaphthyridone derivative of 7-(3-azabicyclo(3.1.0)hexyl)naphthyridone; has antineoplastic activity. trovafloxacin : A 1,8-naphthyridine derivative that is 4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid bearing additional 2,4-difluorophenyl, fluoro and 6-amino-3-azabicyclo[3.1.0]hex-3-yl substituents at positions 1, 6 and 7 respectively. A broad-spectrum antibiotic that was withdrawn from the market due to risk of liver failure. | 3.23 | 1 | 0 | ||
| cefprozil [no description available] | 3.23 | 1 | 0 | cephalosporin; semisynthetic derivative | antibacterial drug |
| efavirenz efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection. | 3.23 | 1 | 0 | acetylenic compound; benzoxazine; cyclopropanes; organochlorine compound; organofluorine compound | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| nelfinavir Nelfinavir: A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.. nelfinavir : An aryl sulfide that is used (as its mesylate salt) for treatment of HIV and also exhibits some anticancer properties. | 3.23 | 1 | 0 | aryl sulfide; benzamides; organic heterobicyclic compound; phenols; secondary alcohol; tertiary amino compound | antineoplastic agent; HIV protease inhibitor |
| fenofibric acid fenofibric acid: RN given refers to parent cpd without isomeric designation; structure. fenofibric acid : A monocarboxylic acid that is 2-methylpropanoic acid substituted by a 4-(4-chlorobenzoyl)phenoxy group at position 2. It is a metabolite of the drug fenofibrate. | 3.23 | 1 | 0 | aromatic ketone; chlorobenzophenone; monocarboxylic acid | drug metabolite; marine xenobiotic metabolite |
| plerixafor plerixafor: a bicyclam derivate, highly potent & selective inhibitor of HIV-1 & HIV-2. plerixafor : An azamacrocycle consisting of two cyclam rings connected by a 1,4-phenylenebis(methylene) linker. It is a CXCR4 chemokine receptor antagonist and a hematopoietic stem cell mobilizer. It is used in combination with grulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells to the perpheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma and multiple myeloma. | 3.23 | 1 | 0 | azacycloalkane; azamacrocycle; benzenes; crown amine; secondary amino compound; tertiary amino compound | anti-HIV agent; antineoplastic agent; C-X-C chemokine receptor type 4 antagonist; immunological adjuvant |
| amprenavir [no description available] | 3.23 | 1 | 0 | carbamate ester; sulfonamide; tetrahydrofuryl ester | antiviral drug; HIV protease inhibitor |
| oseltamivir Oseltamivir: An acetamido cyclohexene that is a structural homolog of SIALIC ACID and inhibits NEURAMINIDASE.. oseltamivir : A cyclohexenecarboxylate ester that is the ethyl ester of oseltamivir acid. An antiviral prodrug (it is hydrolysed to the active free carboxylic acid in the liver), it is used to slow the spread of influenza. | 3.23 | 1 | 0 | acetamides; amino acid ester; cyclohexenecarboxylate ester; primary amino compound | antiviral drug; EC 3.2.1.18 (exo-alpha-sialidase) inhibitor; environmental contaminant; prodrug; xenobiotic |
| epigallocatechin gallate epigallocatechin gallate: a steroid 5alpha-reductase inhibitor and antimutagen in green tea (Camellia sinensis). (-)-epigallocatechin 3-gallate : A gallate ester obtained by the formal condensation of gallic acid with the (3R)-hydroxy group of (-)-epigallocatechin. | 3.15 | 1 | 0 | flavans; gallate ester; polyphenol | antineoplastic agent; antioxidant; apoptosis inducer; geroprotector; Hsp90 inhibitor; neuroprotective agent; plant metabolite |
| histamine phosphate histamine phosphate : A phosphate salt that is the diphosphate salt of histamine. | 3.23 | 1 | 0 | phosphate salt | histamine agonist |
| tilbroquinol [no description available] | 3.23 | 1 | 0 | organohalogen compound; quinolines | |
| bendamustine [no description available] | 3.23 | 1 | 0 | benzimidazoles | |
| droxicam droxicam: structure given in first source. droxicam : An organic heterotricyclic compound that is 2H,5H-[1,3]oxazino[5,6-c][1,2]benzothiazine-2,4(3H)-dione 6,6-dioxide substituted at positions 3 and 5 by pyridin-2-yl and methyl groups respectively. A prodrug of piroxicam, it is used for the relief of pain and inflammation in musculoskeletal disorders such as rheumatoid arthritis and osteoarthritis. | 3.23 | 1 | 0 | organic heterotricyclic compound; pyridines | cyclooxygenase 1 inhibitor; hepatotoxic agent; non-narcotic analgesic; non-steroidal anti-inflammatory drug; platelet aggregation inhibitor; prodrug |
| ebrotidine ebrotidine: an H2-receptor antagonist and gastric mucosa protector | 3.23 | 1 | 0 | sulfonamide | |
| repaglinide [no description available] | 3.23 | 1 | 0 | piperidines | |
| telmisartan Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.. telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension. | 3.23 | 1 | 0 | benzimidazoles; biphenyls; carboxybiphenyl | angiotensin receptor antagonist; antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; environmental contaminant; xenobiotic |
| sertraline Sertraline: A selective serotonin uptake inhibitor that is used in the treatment of depression.. sertraline : A member of the class of tetralins that is tetralin which is substituted at positions 1 and 4 by a methylamino and a 3,4-dichlorophenyl group, respectively (the S,S diastereoisomer). A selective serotonin-reuptake inhibitor (SSRI), it is administered orally as the hydrochloride salt as an antidepressant for the treatment of depression, obsessive-compulsive disorder, panic disorder and post-traumatic stress disorder. | 3.23 | 1 | 0 | dichlorobenzene; secondary amino compound; tetralins | antidepressant; serotonin uptake inhibitor |
| zoledronic acid Zoledronic Acid: An imidobisphosphonate inhibitor of BONE RESORPTION that is used for the treatment of malignancy-related HYPERCALCEMIA; OSTEITIS DEFORMANS; and OSTEOPOROSIS.. zoledronic acid : An imidazole compound having a 2,2-bis(phosphono)-2-hydroxyethane-1-yl substituent at the 1-position. | 3.23 | 1 | 0 | 1,1-bis(phosphonic acid); imidazoles | bone density conservation agent |
| acamprosate Acamprosate: Structural analog of taurine that is used for the prevention of relapse in individuals with ALCOHOLISM.. acamprosate : An organosulfonic acid that is propane-1-sulfonic acid substituted by an acetylamino group at position 3. | 3.23 | 1 | 0 | acetamides; organosulfonic acid | environmental contaminant; neurotransmitter agent; xenobiotic |
| isaxonine isaxonine: promotes nerve growth | 3.23 | 1 | 0 | aminopyrimidine | |
| nebivolol 2,2'-iminobis[1-(6-fluoro-3,4-dihydro-2H-chromen-2-yl)ethanol] : A member of the class of chromanes that is 2,2'-iminodiethanol in which one hydrogen attached to each hydroxy-bearing carbon is replaced by a 6-fluorochroman-2-yl group. | 3.23 | 1 | 0 | chromanes; diol; organofluorine compound; secondary alcohol; secondary amino compound | |
| uk 68798 [no description available] | 3.23 | 1 | 0 | aromatic ether; sulfonamide; tertiary amino compound | anti-arrhythmia drug; potassium channel blocker |
| hp 873 iloperidone: an atypical, negative symptom antipsychotic agent. iloperidone : A member of the class of piperidines that is the 4-acetyl-2-methoxyphenyl ether of 3-(piperidin-1-yl)propan-1-ol which is substituted at position 4 of the piperidine ring by a 6-fluoro-1,2-benzoxazol-3-yl group. A member of the group of second generation antipsychotics (also known as an atypical antipsychotics), it is used for the treatment of schizophrenia. | 3.23 | 1 | 0 | 1,2-benzoxazoles; aromatic ether; aromatic ketone; methyl ketone; monoamine; organofluorine compound; piperidines; tertiary amino compound | dopaminergic antagonist; second generation antipsychotic; serotonergic antagonist |
| dexrazoxane Dexrazoxane: The (+)-enantiomorph of razoxane. | 3.23 | 1 | 0 | razoxane | antineoplastic agent; cardiovascular drug; chelator; immunosuppressive agent |
| fenoxypropazine [no description available] | 3.23 | 1 | 0 | aromatic ether | |
| voriconazole Voriconazole: A triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 CYP3A.. voriconazole : A triazole-based antifungal agent used for the treatment of esophageal candidiasis, invasive pulmonary aspergillosis, and serious fungal infections caused by Scedosporium apiospermum and Fusarium spp. It is an inhibitor of cytochrome P450 2C9 (CYP2C9) and CYP3A4. | 3.23 | 1 | 0 | conazole antifungal drug; difluorobenzene; pyrimidines; tertiary alcohol; triazole antifungal drug | P450 inhibitor |
| aceclofenac [no description available] | 3.23 | 1 | 0 | amino acid; carboxylic ester; dichlorobenzene; monocarboxylic acid; secondary amino compound | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| nitrefazole [no description available] | 3.23 | 1 | 0 | imidazoles | |
| doripenem Doripenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of infections such as HOSPITAL-ACQUIRED PNEUMONIA, and complicated intra-abdominal or urinary-tract infections, including PYELONEPHRITIS. | 3.23 | 1 | 0 | carbapenems | |
| atovaquone Atovaquone: A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.. atovaquone : A naphthoquinone compound having a 4-(4-chlorophenyl)cyclohexyl group at the 2-position and a hydroxy substituent at the 3-position. | 3.23 | 1 | 0 | hydroxy-1,2-naphthoquinone | |
| rivastigmine [no description available] | 3.23 | 1 | 0 | carbamate ester; tertiary amino compound | cholinergic drug; EC 3.1.1.8 (cholinesterase) inhibitor; neuroprotective agent |
| frovatriptan [no description available] | 3.23 | 1 | 0 | carbazoles | |
| eletriptan eletriptan: 5-HT(1B/1D) receptor agonist; structure in first source. eletriptan : An N-alkylpyrrolidine, that is N-methylpyrrolidine in which the pro-R hydrogen at position 2 is replaced by a {5-[2-(phenylsulfonyl)ethyl]-1H-indol-3-yl}methyl group. | 3.23 | 1 | 0 | indoles; N-alkylpyrrolidine; sulfone | non-steroidal anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| rosiglitazone [no description available] | 3.23 | 1 | 0 | aminopyridine; thiazolidinediones | EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; insulin-sensitizing drug |
| bexarotene [no description available] | 3.23 | 1 | 0 | benzoic acids; naphthalenes; retinoid | antineoplastic agent |
| clarithromycin Clarithromycin: A semisynthetic macrolide antibiotic derived from ERYTHROMYCIN that is active against a variety of microorganisms. It can inhibit PROTEIN SYNTHESIS in BACTERIA by reversibly binding to the 50S ribosomal subunits. This inhibits the translocation of aminoacyl transfer-RNA and prevents peptide chain elongation.. clarithromycin : The 6-O-methyl ether of erythromycin A, clarithromycin is a macrolide antibiotic used in the treatment of respiratory-tract, skin and soft-tissue infections. It is also used to eradicate Helicobacter pylori in the treatment of peptic ulcer disease. It prevents bacteria from growing by interfering with their protein synthesis. | 3.23 | 1 | 0 | macrolide antibiotic | antibacterial drug; environmental contaminant; protein synthesis inhibitor; xenobiotic |
| moexipril [no description available] | 3.23 | 1 | 0 | peptide | |
| mci 9038 [no description available] | 3.23 | 1 | 0 | peptide | |
| fulvestrant Fulvestrant: An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer.. fulvestrant : A 3-hydroxy steroid that is 17beta-estradiol in which the 7alpha hydrogen has been replaced by a nonyl group in which one of the hydrogens of the terminal methyl has been replaced by a (4,4,5,5,5-pentafluoropentyl)sulfinyl group. An estrogen receptor antagonist, it is used in the treatment of breast cancer. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-hydroxy steroid; organofluorine compound; sulfoxide | antineoplastic agent; estrogen antagonist; estrogen receptor antagonist |
| bosentan anhydrous Bosentan: A sulfonamide and pyrimidine derivative that acts as a dual endothelin receptor antagonist used to manage PULMONARY HYPERTENSION and SYSTEMIC SCLEROSIS. | 3.23 | 1 | 0 | primary alcohol; pyrimidines; sulfonamide | antihypertensive agent; endothelin receptor antagonist |
| cp-55,940 [no description available] | 3.15 | 1 | 0 | ||
| perindopril Perindopril: An angiotensin-converting enzyme inhibitor. It is used in patients with hypertension and heart failure.. perindopril : An alpha-amino acid ester that is the ethyl ester of N-{(2S)-1-[(2S,3aS,7aS)-2-carboxyoctahydro-1H-indol-1-yl]-1-oxopropan-2-yl}-L-norvaline | 3.23 | 1 | 0 | alpha-amino acid ester; dicarboxylic acid monoester; ethyl ester; organic heterobicyclic compound | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| tadalafil [no description available] | 3.23 | 1 | 0 | benzodioxoles; pyrazinopyridoindole | EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent |
| paliperidone 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one : A member of the class of pyridopyrimidines that is 9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.. paliperidone : A racemate comprising equimolar amounts of (R)- and (S)-paliperidone. Paliperidone is the primary active metabolite of the older antipsychotic risperidone and is used for treatment of schizophrenia. | 3.23 | 1 | 0 | 1,2-benzoxazoles; heteroarylpiperidine; organofluorine compound; pyridopyrimidine; secondary alcohol | |
| nitisinone [no description available] | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; C-nitro compound; cyclohexanones; mesotrione | EC 1.13.11.27 (4-hydroxyphenylpyruvate dioxygenase) inhibitor |
| clofarabine [no description available] | 3.23 | 1 | 0 | adenosines; organofluorine compound | antimetabolite; antineoplastic agent |
| pramipexole Pramipexole: A benzothiazole derivative and dopamine agonist with antioxidant properties that is used in the treatment of PARKINSON DISEASE and RESTLESS LEGS SYNDROME.. pramipexole : A member of the class of benzothiazoles that is 4,5,6,7-tetrahydro-1,3-benzothiazole in which the hydrogens at the 2 and 6-pro-S-positions are substituted by amino and propylamino groups, respectively. | 3.23 | 1 | 0 | benzothiazoles; diamine | antidyskinesia agent; antiparkinson drug; dopamine agonist; radical scavenger |
| valdecoxib [no description available] | 3.23 | 1 | 0 | isoxazoles; sulfonamide | antipyretic; antirheumatic drug; cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| almotriptan almotriptan : An indole compound having a 2-(dimethylamino)ethyl group at the 3-position and a (pyrrolidin-1-ylsulfonyl)methyl group at the 5-position. | 3.23 | 1 | 0 | indoles; sulfonamide; tertiary amine | non-steroidal anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| gefitinib [no description available] | 3.23 | 1 | 0 | aromatic ether; monochlorobenzenes; monofluorobenzenes; morpholines; quinazolines; secondary amino compound; tertiary amino compound | antineoplastic agent; epidermal growth factor receptor antagonist |
| desloratadine desloratadine: major metabolite of loratadine. desloratadine : Loratadine in which the ethoxycarbonyl group attached to the piperidine ring is replaced by hydrogen. The major metabolite of loratidine, desloratadine is an antihistamine which is used for the symptomatic relief of allergic conditions including rhinitis and chronic urticaria. It does not readily enter the central nervous system, so does not cause drowsiness. | 3.23 | 1 | 0 | benzocycloheptapyridine | anti-allergic agent; cholinergic antagonist; drug metabolite; H1-receptor antagonist |
| desvenlafaxine O-desmethylvenlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-hydroxyphenyl group. It is a metabolite of the drug venlafaxine. | 3.23 | 1 | 0 | cyclohexanols; phenols; tertiary amino compound | antidepressant; drug metabolite; marine xenobiotic metabolite |
| methotrexate [no description available] | 3.23 | 1 | 0 | dicarboxylic acid; monocarboxylic acid amide; pteridines | abortifacient; antimetabolite; antineoplastic agent; antirheumatic drug; dermatologic drug; DNA synthesis inhibitor; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; immunosuppressive agent |
| tamsulosin [no description available] | 3.23 | 1 | 0 | 5-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzenesulfonamide | alpha-adrenergic antagonist; antineoplastic agent |
| rufinamide rufinamide: for treatment of Lennox-Gastaut syndrome; structure in first source | 3.23 | 1 | 0 | aromatic amide; heteroarene | |
| olmesartan medoxomil Olmesartan Medoxomil: An ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to manage HYPERTENSION. | 3.23 | 1 | 0 | biphenyls | |
| dexpanthenol dexpanthenol: The alcohol of pantothenic acid | 3.23 | 1 | 0 | amino alcohol; monocarboxylic acid amide | cholinergic drug; provitamin |
| fosamprenavir fosamprenavir: a prodrug of the protease inhibitor amprenavir. fosamprenavir : A sulfonamide with a structure based on that of sulfanilamide substituted on the sulfonamide nitrogen by a (2R,3S)-4-phenyl-2-(phosphonooxy)-3-({[(3S)-tetrahydrofuran-3-yloxy]carbonyl}amino)butyl group. It is a pro-drug of the HIV protease inhibitor and antiretroviral drug amprenavir. | 3.23 | 1 | 0 | sulfonamide | prodrug |
| febuxostat Febuxostat: A thiazole derivative and inhibitor of XANTHINE OXIDASE that is used for the treatment of HYPERURICEMIA in patients with chronic GOUT.. febuxostat : A 1,3-thiazolemonocarboxylic acid that is 4-methyl-1,3-thiazole-5-carboxylic acid which is substituted by a 3-cyano-4-(2-methylpropoxy)phenyl group at position 2. It is an orally-active, potent, and selective xanthine oxidase inhibitor used for the treatment of chronic hyperuricaemia in patients with gout. | 3.23 | 1 | 0 | 1,3-thiazolemonocarboxylic acid; aromatic ether; nitrile | EC 1.17.3.2 (xanthine oxidase) inhibitor |
| escitalopram Escitalopram: S-enantiomer of CITALOPRAM. Belongs to a class of drugs known as SELECTIVE SEROTONIN REUPTAKE INHIBITORS, used to treat depression and generalized anxiety disorder.. escitalopram : A 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile that has S-configuration at the chiral centre. It is the active enantiomer of citalopram. | 3.23 | 1 | 0 | 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile | antidepressant; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor |
| 10-propargyl-10-deazaaminopterin 10-propargyl-10-deazaaminopterin: structure in first source. pralatrexate : A pteridine that is the N-4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl derivative of L-glutamic acid. Used for treatment of Peripheral T-Cell Lymphoma, an aggressive form of non-Hodgkins lymphoma. | 3.23 | 1 | 0 | N-acyl-L-glutamic acid; pteridines; terminal acetylenic compound | antimetabolite; antineoplastic agent; EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
| docetaxel anhydrous Docetaxel: A semisynthetic analog of PACLITAXEL used in the treatment of locally advanced or metastatic BREAST NEOPLASMS and NON-SMALL CELL LUNG CANCER.. docetaxel anhydrous : A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group. | 3.23 | 1 | 0 | secondary alpha-hydroxy ketone; tetracyclic diterpenoid | antimalarial; antineoplastic agent; photosensitizing agent |
| atazanavir atazanavir : A heavily substituted carbohydrazide that is an antiretroviral drug of the protease inhibitor (PI) class used to treat infection of human immunodeficiency virus (HIV). | 3.23 | 1 | 0 | carbohydrazide | antiviral drug; HIV protease inhibitor |
| levofloxacin Levofloxacin: The L-isomer of Ofloxacin.. levofloxacin : An optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase. | 3.23 | 1 | 0 | 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid; fluoroquinolone antibiotic; quinolone antibiotic | antibacterial drug; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; topoisomerase IV inhibitor |
| ezetimibe Ezetimibe: An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS.. ezetimibe : A beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer). | 3.23 | 1 | 0 | azetidines; beta-lactam; organofluorine compound | anticholesteremic drug; antilipemic drug; antimetabolite |
| ertapenem Ertapenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of Gram-positive and Gram-negative bacterial infections including intra-abdominal infections, acute gynecological infections, complicated urinary tract infections, skin infections, and respiratory tract infections. It is also used to prevent infection in colorectal surgery.. ertapenem : Meropenem in which the one of the two methyl groups attached to the amide nitrogen is replaced by hydrogen while the other is replaced by a 3-carboxyphenyl group. The sodium salt is used for the treatment of moderate to severe susceptible infections including intra-abdominal and acute gynaecological infections, pneumonia, and infections of the skin and of the urinary tract. | 3.23 | 1 | 0 | carbapenemcarboxylic acid; pyrrolidinecarboxamide | antibacterial drug |
| cox 189 lumiracoxib: a COX-2 inhibitor. lumiracoxib : An amino acid that is phenylacetic acid which is substituted at position 2 by the nitrogen of 2-chloro-6-fluoroaniline and at position 5 by a methyl group. A highly selective cyclooxygenase 2 inhibitor, it was briefly used for the treatment of osteoarthritis, but was withdrawn due to concersns of hepatotoxicity. | 3.23 | 1 | 0 | amino acid; monocarboxylic acid; organochlorine compound; organofluorine compound; secondary amino compound | cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| conivaptan conivaptan : The amide resulting from the formal condensation of 4-[(biphenyl-2-ylcarbonyl)amino]benzoic acid with the benzazepine nitrogen of 2-methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine. It is an antagonist for two of the three types of arginine vasopressin (AVP) receptors, V1a and V2. It is used as its hydrochloride salt for the treatment of hyponatraemia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH). | 3.23 | 1 | 0 | benzazepine | aquaretic; vasopressin receptor antagonist |
| moxifloxacin Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents. | 3.23 | 1 | 0 | aromatic ether; cyclopropanes; fluoroquinolone antibiotic; pyrrolidinopiperidine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antibacterial drug |
| pralnacasan pralnacasan: NSAID, ICE inhibitor & metastasis inhibitor; RN & structure in first source | 3.23 | 1 | 0 | ||
| clevidipine clevidipine: a calcium channel blocker and antihypertensive agent; structure in first source | 3.23 | 1 | 0 | dihydropyridine | |
| solifenacin [no description available] | 3.23 | 1 | 0 | isoquinolines | |
| dexmethylphenidate dexmethylphenidate : A methyl phenyl(piperidin-2-yl)acetate in which both stereocentres have R configuration. It is the active enantiomer in the racemic drug methylphenidate. | 3.23 | 1 | 0 | methyl phenyl(piperidin-2-yl)acetate | adrenergic agent |
| naproxen Naproxen: An anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout.. naproxen : A methoxynaphthalene that is 2-methoxynaphthalene substituted by a carboxy ethyl group at position 6. Naproxen is a non-steroidal anti-inflammatory drug commonly used for the reduction of pain, fever, inflammation and stiffness caused by conditions such as osteoarthritis, kidney stones, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, bursitis, and for the treatment of primary dysmenorrhea. It works by inhibiting both the COX-1 and COX-2 enzymes. | 3.23 | 1 | 0 | methoxynaphthalene; monocarboxylic acid | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; environmental contaminant; gout suppressant; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| cinacalcet cinacalcet : A secondary amino compound that is (1R)-1-(naphthalen-1-yl)ethanamine in which one of the hydrogens attached to the nitrogen is substituted by a 3-[3-(trifluoromethyl)phenyl]propyl group. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; naphthalenes; secondary amino compound | calcimimetic; P450 inhibitor |
| lubiprostone [no description available] | 3.23 | 1 | 0 | ||
| telbivudine [no description available] | 3.23 | 1 | 0 | pyrimidine 2'-deoxyribonucleoside | antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| paromomycin Paromomycin: An aminoglycoside antibacterial and antiprotozoal agent produced by species of STREPTOMYCES.. paromomycin : An amino cyclitol glycoside that is the 1-O-(2-amino-2-deoxy-alpha-D-glucopyranoside) and the 3-O-(2,6-diamino-2,6-dideoxy-beta-L-idopyranosyl)-beta-D-ribofuranoside of 4,6-diamino-2,3-dihydroxycyclohexane (the 1R,2R,3S,4R,6S diastereoisomer). It is obtained from various Streptomyces species. A broad-spectrum antibiotic, it is used (generally as the sulfate salt) for the treatment of acute and chronic intestinal protozoal infections, but is not effective for extraintestinal protozoal infections. It is also used as a therapeutic against visceral leishmaniasis. | 3.23 | 1 | 0 | amino cyclitol glycoside; aminoglycoside antibiotic | anthelminthic drug; antibacterial drug; antiparasitic agent; antiprotozoal drug |
| anidulafungin Anidulafungin: Echinocandin antifungal agent that is used in the treatment of CANDIDEMIA and CANDIDIASIS.. anidulafungin : A semisynthetic echinocandin anti-fungal drug. It is active against Aspergillus and Candida species and is used for the treatment of invasive candidiasis. | 3.23 | 1 | 0 | antibiotic antifungal drug; azamacrocycle; echinocandin; heterodetic cyclic peptide; semisynthetic derivative | |
| 17 alpha-hydroxyprogesterone caproate 17 alpha-Hydroxyprogesterone Caproate: Hydroxyprogesterone derivative that acts as a PROGESTIN and is used to reduce the risk of recurrent MISCARRIAGE and of PREMATURE BIRTH. It is also used in combination with ESTROGEN in the management of MENSTRUATION DISORDERS. | 3.23 | 1 | 0 | corticosteroid hormone | |
| varenicline Varenicline: A benzazepine derivative that functions as an ALPHA4-BETA2 NICOTINIC RECEPTOR partial agonist. It is used for SMOKING CESSATION.. varenicline : An organic heterotetracyclic compound that acts as a partial agonist for nicotinic cholinergic receptors and is used (in the form of its tartate salt) as an aid to giving up smoking. | 3.23 | 1 | 0 | ||
| fiduxosin fiduxosin: fiduxosin (ABT-980) is the (3aR,9bR)-isomer; structure in first source | 3.23 | 1 | 0 | ||
| atropine tropan-3alpha-yl 3-hydroxy-2-phenylpropanoate : A tropane alkaloid that is (1R,5)-8-methyl-8-azabicyclo[3.2.1]octane substituted by a (3-hydroxy-2-phenylpropanoyl)oxy group at position 3. | 3.23 | 1 | 0 | ||
| erlotinib [no description available] | 3.23 | 1 | 0 | aromatic ether; quinazolines; secondary amino compound; terminal acetylenic compound | antineoplastic agent; epidermal growth factor receptor antagonist; protein kinase inhibitor |
| cilengitide Cilengitide: an alphaVbeta3 integrin antagonist that paralyzes cancer cells | 3.15 | 1 | 0 | oligopeptide | |
| etravirine [no description available] | 3.23 | 1 | 0 | aminopyrimidine; aromatic ether; dinitrile; organobromine compound | antiviral agent; HIV-1 reverse transcriptase inhibitor |
| dronedarone Dronedarone: A non-iodinated derivative of amiodarone that is used for the treatment of ARRHYTHMIA.. dronedarone : A member of the class of 1-benzofurans used for the treatment of cardiac arrhythmias. | 3.23 | 1 | 0 | 1-benzofurans; aromatic ether; aromatic ketone; sulfonamide; tertiary amino compound | anti-arrhythmia drug; environmental contaminant; xenobiotic |
| ramelteon ramelteon: melatonin MT1/MT2 receptor agonist | 3.23 | 1 | 0 | indanes | |
| lapatinib [no description available] | 3.23 | 1 | 0 | furans; organochlorine compound; organofluorine compound; quinazolines | antineoplastic agent; tyrosine kinase inhibitor |
| darunavir Darunavir: An HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.. darunavir : An N,N-disubstituted benzenesulfonamide bearing an unsubstituted amino group at the 4-position, used for the treatment of HIV infection. A second-generation HIV protease inhibitor, darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including those from treatment-experienced patients with multiple resistance mutations to other protease inhibitors. | 3.23 | 1 | 0 | carbamate ester; furofuran; sulfonamide | antiviral drug; HIV protease inhibitor |
| deferasirox Deferasirox: A triazole and benzoate derivative that acts as a selective iron chelator. It is used in the management of chronic IRON OVERLOAD due to blood transfusion or non-transfusion dependent THALASSEMIA.. deferasirox : A member of the class of triazoles, deferasirox is 1,2,4-triazole substituted by a 4-carboxyphenyl group at position 1 and by 2-hydroxyphenyl groups at positions 3 and 5. An orally active iron chelator, it is used to manage chronic iron overload in patients receiving long-term blood transfusions. | 3.23 | 1 | 0 | benzoic acids; monocarboxylic acid; phenols; triazoles | iron chelator |
| tbc-11251 sitaxsentan: endothelin A receptor antagonist; structure in first source | 3.23 | 1 | 0 | benzodioxoles | |
| tolvaptan [no description available] | 3.23 | 1 | 0 | benzazepine; benzenedicarboxamide | aquaretic; vasopressin receptor antagonist |
| sorafenib [no description available] | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; phenylureas; pyridinecarboxamide | angiogenesis inhibitor; anticoronaviral agent; antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; ferroptosis inducer; tyrosine kinase inhibitor |
| lenalidomide [no description available] | 3.23 | 1 | 0 | aromatic amine; dicarboximide; isoindoles; piperidones | angiogenesis inhibitor; antineoplastic agent; immunomodulator |
| regadenoson [no description available] | 3.23 | 1 | 0 | purine nucleoside | |
| lacosamide Lacosamide: An acetamide derivative that acts as a blocker of VOLTAGE-GATED SODIUM CHANNELS. It is used as an anticonvulsant, for adjunctive or monotherapy, in the treatment of PARTIAL SEIZURES. | 3.23 | 1 | 0 | N-acyl-amino acid | |
| vincaleukoblastine [no description available] | 3.23 | 1 | 0 | acetate ester; indole alkaloid fundamental parent; methyl ester; organic heteropentacyclic compound; organic heterotetracyclic compound; tertiary alcohol; tertiary amino compound; vinca alkaloid | antineoplastic agent; immunosuppressive agent; microtubule-destabilising agent; plant metabolite |
| benzarone benzarone: antihemorrhagic agent; structure | 3.23 | 1 | 0 | 1-benzofurans | |
| estramustine Estramustine: A nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties.. estramustine : A carbamate ester obtained by the formal condensation of the hydroxy group of 17beta-estradiol with the carboxy group of bis(2-chloroethyl)carbamic acid. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; carbamate ester; organochlorine compound | alkylating agent; antineoplastic agent; radiation protective agent |
| bortezomib [no description available] | 3.23 | 1 | 0 | amino acid amide; L-phenylalanine derivative; pyrazines | antineoplastic agent; antiprotozoal drug; protease inhibitor; proteasome inhibitor |
| ritonavir Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver. | 3.23 | 1 | 0 | 1,3-thiazoles; carbamate ester; carboxamide; L-valine derivative; ureas | antiviral drug; environmental contaminant; HIV protease inhibitor; xenobiotic |
| oxytocin Oxytocin: A nonapeptide hormone released from the neurohypophysis (PITUITARY GLAND, POSTERIOR). It differs from VASOPRESSIN by two amino acids at residues 3 and 8. Oxytocin acts on SMOOTH MUSCLE CELLS, such as causing UTERINE CONTRACTIONS and MILK EJECTION.. oxytocin : A cyclic nonapeptide hormone with amino acid sequence CYIQNCPLG that also acts as a neurotransmitter in the brain; the principal uterine-contracting and milk-ejecting hormone of the posterior pituitary. Together with the neuropeptide vasopressin, it is believed to influence social cognition and behaviour. | 3.23 | 1 | 0 | heterodetic cyclic peptide; peptide hormone | oxytocic; vasodilator agent |
| pentostatin Pentostatin: A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.. pentostatin : A member of the class of coformycins that is coformycin in which the hydroxy group at position 2' is replaced with a hydrogen. It is a drug used for the treatment of hairy cell leukaemia. | 3.23 | 1 | 0 | coformycins | antimetabolite; antineoplastic agent; Aspergillus metabolite; bacterial metabolite; EC 3.5.4.4 (adenosine deaminase) inhibitor |
| quinidine Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.. quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy. | 3.23 | 1 | 0 | cinchona alkaloid | alpha-adrenergic antagonist; anti-arrhythmia drug; antimalarial; drug allergen; EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor; EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor; muscarinic antagonist; P450 inhibitor; potassium channel blocker; sodium channel blocker |
| meropenem Meropenem: A thienamycin derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of bacterial infections, including infections in immunocompromised patients.. meropenem : A carbapenemcarboxylic acid in which the azetidine and pyrroline rings carry 1-hydroxymethyl and in which the azetidine and pyrroline rings carry 1-hydroxymethyl and 5-(dimethylcarbamoyl)pyrrolidin-3-ylthio substituents respectively. | 3.23 | 1 | 0 | alpha,beta-unsaturated monocarboxylic acid; carbapenemcarboxylic acid; organic sulfide; pyrrolidinecarboxamide | antibacterial agent; antibacterial drug; drug allergen |
| griseofulvin Griseofulvin: An antifungal agent used in the treatment of TINEA infections.. griseofulvin : An oxaspiro compound produced by Penicillium griseofulvum. It is used by mouth as an antifungal drug for infections involving the scalp, hair, nails and skin that do not respond to topical treatment. | 3.23 | 1 | 0 | 1-benzofurans; antibiotic antifungal drug; benzofuran antifungal drug; organochlorine compound; oxaspiro compound | antibacterial agent; Penicillium metabolite |
| cefoxitin Cefoxitin: A semisynthetic cephamycin antibiotic resistant to beta-lactamase.. cefoxitin : A semisynthetic cephamycin antibiotic which, in addition to the methoxy group at the 7alpha position, has 2-thienylacetamido and carbamoyloxymethyl side-groups. It is resistant to beta-lactamase. | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin; cephamycin; semisynthetic derivative | antibacterial drug |
| saquinavir Saquinavir: An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.. saquinavir : An aspartic acid derivative obtained by formal condensation of the primary amino group of (2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl]-3-hydroxy-1-phenylbutan-2-ylamine with the carboxy group of N(2)(-quinolin-2-ylcarbonyl)-L-asparagine. An inhibitor of HIV-1 protease. | 3.23 | 1 | 0 | L-asparagine derivative; quinolines | antiviral drug; HIV protease inhibitor |
| pancuronium Pancuronium: A bis-quaternary steroid that is a competitive nicotinic antagonist. As a neuromuscular blocking agent it is more potent than CURARE but has less effect on the circulatory system and on histamine release.. pancuronium : A steroid ester in which a 5alpha-androstane skeleton is C-3alpha- and C-17beta-disubstituted with acetoxy groups and 2beta- and 16beta-disubstituted with 1-methylpiperidinium-1-yl groups. It is a non-depolarizing curare-mimetic muscle relaxant. | 3.23 | 1 | 0 | acetate ester; steroid ester | cholinergic antagonist; muscle relaxant; nicotinic antagonist |
| abacavir abacavir: a carbocyclic nucleoside with potent selective anti-HIV activity. abacavir : A 2,6-diaminopurine that is (1S)-cyclopent-2-en-1-ylmethanol in which the pro-R hydrogen at the 4-position is substituted by a 2-amino-6-(cyclopropylamino)-9H-purin-9-yl group. A nucleoside analogue reverse transcriptase inhibitor (NRTI) with antiretroviral activity against HIV, it is used (particularly as the sulfate) with other antiretrovirals in combination therapy of HIV infection. | 3.23 | 1 | 0 | 2,6-diaminopurines | antiviral drug; drug allergen; HIV-1 reverse transcriptase inhibitor |
| miglitol [no description available] | 3.23 | 1 | 0 | piperidines | |
| metyrosine alpha-methyl-L-tyrosine : An L-tyrosine derivative that consists of L-tyrosine bearing an additional methyl substituent at position 2. An inhibitor of the enzyme tyrosine 3-monooxygenase, and consequently of the synthesis of catecholamines. It is used to control the symptoms of excessive sympathetic stimulation in patients with pheochromocytoma. | 3.23 | 1 | 0 | L-tyrosine derivative; non-proteinogenic L-alpha-amino acid | antihypertensive agent; EC 1.14.16.2 (tyrosine 3-monooxygenase) inhibitor |
| linezolid [no description available] | 3.23 | 1 | 0 | acetamides; morpholines; organofluorine compound; oxazolidinone | antibacterial drug; protein synthesis inhibitor |
| naringin [no description available] | 3.15 | 1 | 0 | (2S)-flavan-4-one; 4'-hydroxyflavanones; dihydroxyflavanone; disaccharide derivative; neohesperidoside | anti-inflammatory agent; antineoplastic agent; metabolite |
| clindamycin phosphate [no description available] | 3.23 | 1 | 0 | ||
| eplerenone Eplerenone: A spironolactone derivative and selective ALDOSTERONE RECEPTOR antagonist that is used in the management of HYPERTENSION and CONGESTIVE HEART FAILURE, post-MYOCARDIAL INFARCTION. | 3.23 | 1 | 0 | 3-oxo-Delta(4) steroid; epoxy steroid; gamma-lactone; methyl ester; organic heteropentacyclic compound; oxaspiro compound; steroid acid ester | aldosterone antagonist; antihypertensive agent |
| tolterodine [no description available] | 3.23 | 1 | 0 | tertiary amine | antispasmodic drug; muscarinic antagonist; muscle relaxant |
| darifenacin darifenacin : 2-[(3S)-1-Ethylpyrrolidin-3-yl]-2,2-diphenylacetamide in which one of the hydrogens at the 2-position of the ethyl group is substituted by a 2,3-dihydro-1-benzofuran-5-yl group. It is a selective antagonist for the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions, and is used as the hydrobromide salt in the management of urinary incontinence. | 3.23 | 1 | 0 | 1-benzofurans; monocarboxylic acid amide; pyrrolidines | antispasmodic drug; muscarinic antagonist |
| tretinoin Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).. retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).. all-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry. | 3.23 | 1 | 0 | retinoic acid; vitamin A | anti-inflammatory agent; antineoplastic agent; antioxidant; AP-1 antagonist; human metabolite; keratolytic drug; retinoic acid receptor agonist; retinoid X receptor agonist; signalling molecule |
| retinol Vitamin A: Retinol and derivatives of retinol that play an essential role in metabolic functioning of the retina, the growth of and differentiation of epithelial tissue, the growth of bone, reproduction, and the immune response. Dietary vitamin A is derived from a variety of CAROTENOIDS found in plants. It is enriched in the liver, egg yolks, and the fat component of dairy products.. vitamin A : Any member of a group of fat-soluble retinoids produced via metabolism of provitamin A carotenoids that exhibit biological activity against vitamin A deficiency. Vitamin A is involved in immune function, vision, reproduction, and cellular communication.. all-trans-retinol : A retinol in which all four exocyclic double bonds have E- (trans-) geometry.. retinol : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraen-1-ol substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified). | 3.23 | 1 | 0 | retinol; vitamin A | human metabolite; mouse metabolite; plant metabolite |
| tacrolimus Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.. tacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis. | 3.23 | 1 | 0 | macrolide lactam | bacterial metabolite; immunosuppressive agent |
| rosuvastatin rosuvastatin : A dihydroxy monocarboxylic acid that is (6E)-7-{4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-(propan-2-yl)pyrimidin-5-yl} hept-6-enoic acid carrying two hydroxy substituents at positions 3 and 5 (the 3R,5S-diastereomer). | 3.23 | 1 | 0 | dihydroxy monocarboxylic acid; monofluorobenzenes; pyrimidines; statin (synthetic); sulfonamide | anti-inflammatory agent; antilipemic drug; cardioprotective agent; CETP inhibitor; environmental contaminant; xenobiotic |
| mycophenolic acid Mycophenolic Acid: Compound derived from Penicillium stoloniferum and related species. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase (IMP DEHYDROGENASE). Mycophenolic acid exerts selective effects on the immune system in which it prevents the proliferation of T-CELLS, LYMPHOCYTES, and the formation of antibodies from B-CELLS. It may also inhibit recruitment of LEUKOCYTES to sites of INFLAMMATION.. mycophenolate : A monocarboxylic acid anion resulting from the removal of a proton from the carboxy group of mycophenolic acid.. mycophenolic acid : A member of the class of 2-benzofurans that is 2-benzofuran-1(3H)-one which is substituted at positions 4, 5, 6, and 7 by methyl, methoxy, (2E)-5-carboxy-3-methylpent-2-en-1-yl, and hydroxy groups, respectively. It is an antibiotic produced by Penicillium brevi-compactum, P. stoloniferum, P. echinulatum and related species. An immunosuppressant, it is widely used (partiularly as its sodium salt and as the 2-(morpholin-4-yl)ethyl ester prodrug, mycophenolate mofetil) to prevent tissue rejection following organ transplants and for the treatment of certain autoimmune diseases. | 3.23 | 1 | 0 | 2-benzofurans; gamma-lactone; monocarboxylic acid; phenols | anticoronaviral agent; antimicrobial agent; antineoplastic agent; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; environmental contaminant; immunosuppressive agent; mycotoxin; Penicillium metabolite; xenobiotic |
| clindamycin Clindamycin: An antibacterial agent that is a semisynthetic analog of LINCOMYCIN.. clindamycin : A carbohydrate-containing antibiotic that is the semisynthetic derivative of lincomycin, a natural antibiotic. | 3.23 | 1 | 0 | ||
| fosfomycin Fosfomycin: An antibiotic produced by Streptomyces fradiae.. fosfomycin : A phosphonic acid having an (R,S)-1,2-epoxypropyl group attached to phosphorus. | 3.23 | 1 | 0 | epoxide; phosphonic acids | antimicrobial agent; EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor |
| zithromax Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections. | 3.23 | 1 | 0 | macrolide antibiotic | antibacterial drug; environmental contaminant; xenobiotic |
| octreotide [no description available] | 3.23 | 1 | 0 | ||
| eptifibatide [no description available] | 3.23 | 1 | 0 | homodetic cyclic peptide; macrocycle; organic disulfide | anticoagulant; platelet aggregation inhibitor |
| decitabine [no description available] | 3.23 | 1 | 0 | 2'-deoxyribonucleoside | |
| teniposide [no description available] | 3.23 | 1 | 0 | aromatic ether; beta-D-glucoside; cyclic acetal; furonaphthodioxole; gamma-lactone; monosaccharide derivative; phenols; thiophenes | antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor |
| dactinomycin Dactinomycin: A compound composed of a two CYCLIC PEPTIDES attached to a phenoxazine that is derived from STREPTOMYCES parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, protein synthesis also declines after dactinomycin therapy. (From AMA Drug Evaluations Annual, 1993, p2015) | 3.23 | 1 | 0 | actinomycin | mutagen |
| melphalan Melphalan: An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - MELPHALAN, the racemic mixture - MERPHALAN, and the dextro isomer - MEDPHALAN; toxic to bone marrow, but little vesicant action; potential carcinogen.. melphalan : A phenylalanine derivative comprising L-phenylalanine having [bis(2-chloroethyl)amino group at the 4-position on the phenyl ring. | 3.23 | 1 | 0 | L-phenylalanine derivative; nitrogen mustard; non-proteinogenic L-alpha-amino acid; organochlorine compound | alkylating agent; antineoplastic agent; carcinogenic agent; drug allergen; immunosuppressive agent |
| tenofovir tenofovir (anhydrous) : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens is replaced by a [(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(isopropyloxycarbonyloxymethyl) ester (disoproxil ester) prodrug is used as the fumaric acid salt in combination therapy for the treatment of HIV infection. | 3.23 | 1 | 0 | nucleoside analogue; phosphonic acids | antiviral drug; drug metabolite; HIV-1 reverse transcriptase inhibitor |
| posaconazole [no description available] | 3.23 | 1 | 0 | aromatic ether; conazole antifungal drug; N-arylpiperazine; organofluorine compound; oxolanes; triazole antifungal drug; triazoles | trypanocidal drug |
| micafungin Micafungin: A cyclic lipo-hexapeptide echinocandin antifungal agent that is used for the treatment and prevention of CANDIDIASIS.. micafungin : A cyclic hexapeptide echinocandin antibiotic which exerts its effect by inhibiting the synthesis of 1,3-beta-D-glucan, an integral component of the fungal cell wall. It is used as the sodium salt for the treatment of invasive candidiasis, and of aspergillosis in patients who are intolerant of other therapy. | 3.23 | 1 | 0 | antibiotic antifungal drug; echinocandin | antiinfective agent |
| riboflavin vitamin B2 : Any member of a group of vitamers that belong to the chemical structural class called flavins that exhibit biological activity against vitamin B2 deficiency. Symptoms associated with vitamin B2 deficiency include glossitis, seborrhea, angular stomaitis, cheilosis and photophobia. The vitamers include riboflavin and its phosphate derivatives (and includes their salt, ionised and hydrate forms). | 3.23 | 1 | 0 | flavin; vitamin B2 | anti-inflammatory agent; antioxidant; cofactor; Escherichia coli metabolite; food colouring; fundamental metabolite; human urinary metabolite; mouse metabolite; photosensitizing agent; plant metabolite |
| sodium bicarbonate Sodium Bicarbonate: A white, crystalline powder that is commonly used as a pH buffering agent, an electrolyte replenisher, systemic alkalizer and in topical cleansing solutions. | 3.23 | 1 | 0 | one-carbon compound; organic sodium salt | antacid; food anticaking agent |
| arsenic trioxide Tetraarsenic Oxide: A form of As2O3 that exists as As4O6 in the solid state. It dissociates to As2O3 upon heating to the vapor phase above 800 degrees Celsius. | 3.23 | 1 | 0 | arsenic oxide | antineoplastic agent; insecticide |
| sr 90107 fondaparinux sodium : An organic sodium salt, being the decasodium salt of fondaparinux. | 3.23 | 1 | 0 | ||
| meglumine iodipamide [no description available] | 3.23 | 1 | 0 | organoammonium salt | radioopaque medium |
| thyrotropin-releasing hormone PR 546: no other info available 9/89. protirelin : A tripeptide composed of L-pyroglutamyl, L-histidyl and L-prolinamide residues joined in sequence. | 3.23 | 1 | 0 | peptide hormone; tripeptide | human metabolite |
| cannabidiol Cannabidiol: Compound isolated from Cannabis sativa extract.. cannabidiol : An cannabinoid that is cyclohexene which is substituted by a methyl group at position 1, a 2,6-dihydroxy-4-pentylphenyl group at position 3, and a prop-1-en-2-yl group at position 4. | 3.15 | 1 | 0 | olefinic compound; phytocannabinoid; resorcinols | antimicrobial agent; plant metabolite |
| arginine vasopressin Arginine Vasopressin: The predominant form of mammalian antidiuretic hormone. It is a nonapeptide containing an ARGININE at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. Arg-vasopressin is used to treat DIABETES INSIPIDUS or to improve vasomotor tone and BLOOD PRESSURE.. argipressin : The predominant form of mammalian vasopressin (antidiuretic hormone). It is a nonapeptide containing an arginine at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. | 3.23 | 1 | 0 | vasopressin | cardiovascular drug; hematologic agent; mitogen |
| s 1033 [no description available] | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; imidazoles; pyridines; pyrimidines; secondary amino compound; secondary carboxamide | anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor |
| propylthiouracil Propylthiouracil: A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534). 6-propyl-2-thiouracil : A pyrimidinethione consisting of uracil in which the 2-oxo group is substituted by a thio group and the hydrogen at position 6 is substituted by a propyl group. | 3.23 | 1 | 0 | pyrimidinethione | antidote to paracetamol poisoning; antimetabolite; antioxidant; antithyroid drug; carcinogenic agent; EC 1.14.13.39 (nitric oxide synthase) inhibitor; hormone antagonist |
| etomidate Etomidate: Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic.. etomidate : The ethyl ester of 1-[(1R)-1-phenylethyl]-1H-imidazole-5-carboxylic acid. It is an intravenous general anaesthetic with no analgesic activity. | 3.23 | 1 | 0 | ethyl ester; imidazoles | intravenous anaesthetic; sedative |
| mercaptopurine Mercaptopurine: An antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.. purine-6-thiol : A thiol that is the tautomer of mercaptopurine.. mercaptopurine : A member of the class of purines that is 6,7-dihydro-1H-purine carrying a thione group at position 6. An adenine analogue, it is used in the treatment of acute lymphocytic leukemia (ALL), chronic myeloid leukemia (CML), Crohn's disease, and ulcerative colitis. | 3.23 | 1 | 0 | aryl thiol; purines; thiocarbonyl compound | anticoronaviral agent; antimetabolite; antineoplastic agent |
| pyrantel Pyrantel: A depolarizing neuromuscular-blocking agent, that causes persistent nicotinic activation resulting in spastic paralysis of susceptible nematodes. It is a drug of second-choice after benzimidazoles for treatment of ascariasis, hookworm, and pinworm infections, being effective after a single dose. (From Smith and Reynard, Textbook of Pharmacology, 1992, p920). pyrantel : A carboxamidine that is 1,4,5,6-tetrahydropyrimidine that is substituted at position 1 by a methyl group and at position 2 by an (E)-2-(2-thienyl)vinyl group. It is used, particularly as the embonate [4,4'-methylenebis(3-hydroxy-2-naphthoate)] salt, as an anthelmintic that is effective against intestinal nematodes including threadworms, roundworms and hookworms, and is included in the WHO 'Model List of Essential Medicines'. | 3.23 | 1 | 0 | 1,4,5,6-tetrahydropyrimidines; carboxamidine; thiophenes | antinematodal drug |
| thiothixene [no description available] | 3.23 | 1 | 0 | N-methylpiperazine | anticoronaviral agent |
| eszopiclone Eszopiclone: A pyridine, pyrazine, and piperazine derivative that is used as a HYPNOTIC AND SEDATIVE in the treatment of INSOMNIA.. eszopiclone : The (5S)- (active) enantiomer of zopiclone. Unlike almost all other hypnotic sedatives, which are approved only for the relief of short-term (6-8 weeks) insomnia, eszopiclone is approved by the U.S. Food and Drug Administration for long-term use. | 3.23 | 1 | 0 | zopiclone | central nervous system depressant; sedative |
| benztropine Benztropine: A centrally active muscarinic antagonist that has been used in the symptomatic treatment of PARKINSON DISEASE. Benztropine also inhibits the uptake of dopamine.. benzatropine : Tropane in which a hydrogen at position 3 is substituted by a diphenylmethoxy group (endo-isomer). An acetylcholine receptor antagonist, it is used (particularly as its methanesulphonate salt) in the treatment of Parkinson's disease, and to reduce parkinsonism and akathisia side effects of antipsychotic treatments. | 3.23 | 1 | 0 | diarylmethane | |
| methimazole Methimazole: A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme.. methimazole : A member of the class of imidazoles that it imidazole-2-thione in which a methyl group replaces the hydrogen which is attached to a nitrogen. | 3.23 | 1 | 0 | 1,3-dihydroimidazole-2-thiones | antithyroid drug |
| sulindac Sulindac: A sulfinylindene derivative prodrug whose sulfinyl moiety is converted in vivo to an active NSAID analgesic. Specifically, the prodrug is converted by liver enzymes to a sulfide which is excreted in the bile and then reabsorbed from the intestine. This helps to maintain constant blood levels with reduced gastrointestinal side effects.. sulindac : A monocarboxylic acid that is 1-benzylidene-1H-indene which is substituted at positions 2, 3, and 5 by methyl, carboxymethyl, and fluorine respectively, and in which the phenyl group of the benzylidene moiety is substituted at the para position by a methylsulfinyl group. It is a prodrug for the corresponding sulfide, a non-steroidal anti-inflammatory drug, used particularly in the treatment of acute and chronic inflammatory conditions. | 3.23 | 1 | 0 | monocarboxylic acid; organofluorine compound; sulfoxide | analgesic; antineoplastic agent; antipyretic; apoptosis inducer; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug; tocolytic agent |
| terbinafine [no description available] | 3.23 | 1 | 0 | acetylenic compound; allylamine antifungal drug; enyne; naphthalenes; tertiary amine | EC 1.14.13.132 (squalene monooxygenase) inhibitor; P450 inhibitor; sterol biosynthesis inhibitor |
| thioguanine anhydrous Thioguanine: An antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.. tioguanine : A 2-aminopurine that is the 6-thiono derivative of 2-amino-1,9-dihydro-6H-purine. Incorporates into DNA and inhibits synthesis. Used in the treatment of leukaemia. | 3.23 | 1 | 0 | 2-aminopurines | anticoronaviral agent; antimetabolite; antineoplastic agent |
| succimer Succimer: A mercaptodicarboxylic acid used as an antidote to heavy metal poisoning because it forms strong chelates with them.. succimer : A sulfur-containing carboxylic acid that is succinic acid bearing two mercapto substituents at positions 2 and 3. A lead chelator used as an antedote to lead poisoning. | 3.23 | 1 | 0 | dicarboxylic acid; dithiol; sulfur-containing carboxylic acid | chelator |
| digoxin Digoxin: A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666). digoxin : A cardenolide glycoside that is digitoxin beta-hydroxylated at C-12. A cardiac glycoside extracted from the foxglove plant, Digitalis lanata, it is used to control ventricular rate in atrial fibrillation and in the management of congestive heart failure with atrial fibrillation, but the margin between toxic and therapeutic doses is small. | 3.23 | 1 | 0 | cardenolide glycoside; steroid saponin | anti-arrhythmia drug; cardiotonic drug; EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor; epitope |
| streptozocin [no description available] | 3.23 | 1 | 0 | ||
| tamoxifen [no description available] | 3.23 | 1 | 0 | stilbenoid; tertiary amino compound | angiogenesis inhibitor; antineoplastic agent; bone density conservation agent; EC 1.2.3.1 (aldehyde oxidase) inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; estrogen antagonist; estrogen receptor antagonist; estrogen receptor modulator |
| ethionamide Ethionamide: A second-line antitubercular agent that inhibits mycolic acid synthesis.. ethionamide : A thiocarboxamide that is pyridine-4-carbothioamide substituted by an ethyl group at position 2. A prodrug that undergoes metabolic activation by conversion to the corresponding S-oxide. | 3.23 | 1 | 0 | pyridines; thiocarboxamide | antilipemic drug; antitubercular agent; fatty acid synthesis inhibitor; leprostatic drug; prodrug |
| cancidas [no description available] | 3.23 | 1 | 0 | ||
| lincomycin Lincomycin: An antibiotic produced by Streptomyces lincolnensis var. lincolnensis. It has been used in the treatment of staphylococcal, streptococcal, and Bacteroides fragilis infections.. lincomycin : A carbohydrate-containing antibiotic produced by the actinomyces Streptomyces lincolnensis. | 3.23 | 1 | 0 | carbohydrate-containing antibiotic; L-proline derivative; monocarboxylic acid amide; pyrrolidinecarboxamide; S-glycosyl compound | antimicrobial agent; bacterial metabolite |
| ranitidine Ranitidine: A non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.. ranitidine : A member of the class of furans used to treat peptic ulcer disease (PUD) and gastroesophageal reflux disease. | 3.23 | 1 | 0 | C-nitro compound; furans; organic sulfide; tertiary amino compound | anti-ulcer drug; drug allergen; environmental contaminant; H2-receptor antagonist; xenobiotic |
| aplaviroc aplaviroc: a spiro-diketo-piperazine; a potent noncompetitive allosteric antagonist of the CCR5 receptor with concomitantly potent antiviral effects for HIV-1; structure in first source | 3.23 | 1 | 0 | ||
| hmr 3647 [no description available] | 3.23 | 1 | 0 | ||
| maraviroc [no description available] | 3.23 | 1 | 0 | tropane alkaloid | |
| toremifene Toremifene: A first generation selective estrogen receptor modulator (SERM). Like TAMOXIFEN, it is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on mammary and uterine tissue. | 3.23 | 1 | 0 | aromatic ether; organochlorine compound; tertiary amine | antineoplastic agent; bone density conservation agent; estrogen antagonist; estrogen receptor modulator |
| nelarabine nelarabine: prodrug of ara-G. nelarabine : A purine nucleoside in which O-methylguanine is attached to arabinofuranose via a beta-N(9)-glycosidic bond. Inhibits DNA synthesis and causes cell death; a prodrug of 9-beta-D-arabinofuranosylguanine (ara-G). | 3.23 | 1 | 0 | beta-D-arabinoside; monosaccharide derivative; purine nucleoside | antineoplastic agent; DNA synthesis inhibitor; prodrug |
| dermatan sulfate Dermatan Sulfate: A naturally occurring glycosaminoglycan found mostly in the skin and in connective tissue. It differs from CHONDROITIN SULFATE A (see CHONDROITIN SULFATES) by containing IDURONIC ACID in place of glucuronic acid, its epimer, at carbon atom 5. (from Merck, 12th ed). alpha-L-IdopA-(1->3)-beta-D-GalpNAc4S : An oligosaccharide sulfate that is 2-acetamido-2-deoxy-4-O-sulfo-beta-D-galactopyranose in which the hydroxy group at position 3 has been converted to the corresponding alpha-L-idopyranuronoside.. dermatan sulfate : Any of a group of glycosaminoglycans with repeating units consisting of variously sulfated beta1->4-linked L-iduronyl-(alpha1->3)-N-acetyl-D-galactosamine units. | 3.23 | 1 | 0 | amino disaccharide; glycosylgalactose derivative; iduronic acids; oligosaccharide sulfate | |
| dolasetron [no description available] | 3.23 | 1 | 0 | indolyl carboxylic acid | |
| orlistat Orlistat: A lactone derivative of LEUCINE that acts as a pancreatic lipase inhibitor to limit the absorption of dietary fat; it is used in the management of obesity.. orlistat : A carboxylic ester resulting from the formal condensation of the carboxy group of N-formyl-L-leucine with the hydroxy group of (3S,4S)-3-hexyl-4-[(2S)-2-hydroxytridecyl]oxetan-2-one. A pancreatic lipase inhibitor, it is used as an anti-obesity drug. | 3.23 | 1 | 0 | beta-lactone; carboxylic ester; formamides; L-leucine derivative | anti-obesity agent; bacterial metabolite; EC 2.3.1.85 (fatty acid synthase) inhibitor; EC 3.1.1.3 (triacylglycerol lipase) inhibitor |
| quinine [no description available] | 3.23 | 1 | 0 | cinchona alkaloid | antimalarial; muscle relaxant; non-narcotic analgesic |
| fospropofol [no description available] | 3.23 | 1 | 0 | alkylbenzene | |
| rasagiline [no description available] | 3.23 | 1 | 0 | indanes; secondary amine; terminal acetylenic compound | EC 1.4.3.4 (monoamine oxidase) inhibitor; neuroprotective agent |
| dasatinib N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN). | 3.23 | 1 | 0 | 1,3-thiazoles; aminopyrimidine; monocarboxylic acid amide; N-(2-hydroxyethyl)piperazine; N-arylpiperazine; organochlorine compound; secondary amino compound; tertiary amino compound | anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor |
| am 630 iodopravadoline: an aminoalkylindole; a competitive cannabinoid receptor antagonist; structure given in first source | 3.15 | 1 | 0 | N-acylindole | |
| sitagliptin sitagliptin : A triazolopyrazine that exhibits hypoglycemic activity. | 3.23 | 1 | 0 | triazolopyrazine; trifluorobenzene | EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; environmental contaminant; hypoglycemic agent; serine proteinase inhibitor; xenobiotic |
| tolcapone Tolcapone: A benzophenone and nitrophenol compound that acts as an inhibitor of CATECHOL O-METHYLTRANSFERASE, an enzyme involved in the metabolism of DOPAMINE and LEVODOPA. It is used in the treatment of PARKINSON DISEASE in patients for whom levodopa is ineffective or contraindicated.. tolcapone : Benzophenone substituted on one of the phenyl rings at C-3 and C-4 by hydroxy groups and at C-5 by a nitro group, and on the other phenyl ring by a methyl group at C-4. It is an inhibitor of catechol O-methyltransferase. | 3.23 | 1 | 0 | 2-nitrophenols; benzophenones; catechols | antiparkinson drug; EC 2.1.1.6 (catechol O-methyltransferase) inhibitor |
| dinoprostone prostaglandin E2 : Prostaglandin F2alpha in which the hydroxy group at position 9 has been oxidised to the corresponding ketone. Prostaglandin E2 is the most common and most biologically potent of mammalian prostaglandins. | 3.15 | 1 | 0 | prostaglandins E | human metabolite; mouse metabolite; oxytocic |
| calcitriol dihydroxy-vitamin D3: as a major in vitro metabolite of 1alpha,25-dihydroxyvitamin D3, produced in primary cultures of neonatal human keratinocytes | 3.23 | 1 | 0 | D3 vitamins; hydroxycalciol; triol | antineoplastic agent; antipsoriatic; bone density conservation agent; calcium channel agonist; calcium channel modulator; hormone; human metabolite; immunomodulator; metabolite; mouse metabolite; nutraceutical |
| vitamin d 2 Ergocalciferols: Derivatives of ERGOSTEROL formed by ULTRAVIOLET RAYS breaking of the C9-C10 bond. They differ from CHOLECALCIFEROL in having a double bond between C22 and C23 and a methyl group at C24.. vitamin D2 : A vitamin D supplement and has been isolated from alfalfa. | 3.23 | 1 | 0 | hydroxy seco-steroid; seco-ergostane; vitamin D | bone density conservation agent; nutraceutical; plant metabolite; rodenticide |
| amphotericin b Amphotericin B: Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela.. amphotericin B : A macrolide antibiotic used to treat potentially life-threatening fungal infections. | 3.23 | 1 | 0 | antibiotic antifungal drug; macrolide antibiotic; polyene antibiotic | antiamoebic agent; antiprotozoal drug; bacterial metabolite |
| pulmicort Budesonide: A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS.. budesonide : A glucocorticoid steroid having a highly oxygenated pregna-1,4-diene structure. It is used mainly in the treatment of asthma and non-infectious rhinitis and for treatment and prevention of nasal polyposis. | 3.23 | 1 | 0 | 11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; cyclic acetal; glucocorticoid; primary alpha-hydroxy ketone | anti-inflammatory drug; bronchodilator agent; drug allergen |
| oxymetholone Oxymetholone: A synthetic hormone with anabolic and androgenic properties. It is used mainly in the treatment of anemias. According to the Fourth Annual Report on Carcinogens (NTP 85-002), this compound may reasonably be anticipated to be a carcinogen. (From Merck Index, 11th ed). oxymetholone : A 3-oxo-5alpha- steroid that is 4,5alpha-dihydrotestosterone which is substituted by a hydroxymethylidene group at position 2 and by a methyl group at the 17alpha position. A synthetic androgen, it was mainly used for the treatment of anaemias until being replaced by treatments with fewer side effects. | 3.23 | 1 | 0 | ||
| eprosartan eprosartan: angiotensin II receptor antagonist. eprosartan : A member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure. | 3.23 | 1 | 0 | dicarboxylic acid; imidazoles; thiophenes | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| montelukast montelukast: a leukotriene D4 receptor antagonist | 3.23 | 1 | 0 | aliphatic sulfide; monocarboxylic acid; quinolines | anti-arrhythmia drug; anti-asthmatic drug; leukotriene antagonist |
| mivacurium Mivacurium: An isoquinoline derivative that is used as a short-acting non-depolarizing agent. | 3.23 | 1 | 0 | isoquinolines | |
| hemabate carboprost tromethamine : The tromethamine salt of carboprost. It is used as an abortifacient agent that is effective in both the first and second trimesters of pregnancy. | 3.23 | 1 | 0 | ||
| mycophenolate mofetil mycophenolate mofetil : A carboxylic ester resulting from the formal condensation between the carboxylic acid group of mycophenolic acid and the hydroxy group of 2-(morpholin-4-yl)ethanol. In the liver, it is metabolised to mycophenolic acid, an immunosuppressant for which it is a prodrug. It is widely used to prevent tissue rejection following organ transplants as well as for the treatment of certain autoimmune diseases. | 3.23 | 1 | 0 | carboxylic ester; ether; gamma-lactone; phenols; tertiary amino compound | anticoronaviral agent; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; immunosuppressive agent; prodrug |
| entacapone entacapone: structure given in first source. entacapone : A monocarboxylic acid amide that is N,N-diethylprop-2-enamide in which the hydrogen at position 2 is substituted by a cyano group and the hydrogen at the 3E position is substituted by a 3,4-dihydroxy-5-nitrophenyl group. | 3.23 | 1 | 0 | 2-nitrophenols; catechols; monocarboxylic acid amide; nitrile | antidyskinesia agent; antiparkinson drug; central nervous system drug; EC 2.1.1.6 (catechol O-methyltransferase) inhibitor |
| paricalcitol [no description available] | 3.23 | 1 | 0 | hydroxy seco-steroid; seco-cholestane | antiparathyroid drug |
| sciadopitysin sciadopitysin: biflavonoid from Taxus celebica & Ginkgo biloba. sciadopitysin : A biflavonoid that is a 7, 4', 4'''-trimethyl ether derivative of amentoflavone. | 3.15 | 1 | 0 | biflavonoid; hydroxyflavone; methoxyflavone; ring assembly | bone density conservation agent; platelet aggregation inhibitor |
| 7432 s Ceftibuten: A cephalosporin antibacterial agent that is used in the treatment of infections, including urinary-tract and respiratory-tract infections.. ceftibuten : A third-generation cephalosporin antibiotic with a [(2Z)-2-(2-amino-1,3-thiazol-4-yl)-4-carboxybut-2-enoyl]amino substituent at the 7 position of the cephem skeleton. An orally-administered agent, ceftibuten is used as the dihydrate to treat urinary-tract and respiratory-tract infections. | 3.23 | 1 | 0 | cephalosporin; dicarboxylic acid | antibacterial drug |
| isotretinoin Isotretinoin: A topical dermatologic agent that is used in the treatment of ACNE VULGARIS and several other skin diseases. The drug has teratogenic and other adverse effects.. isotretinoin : A retinoic acid that is all-trans-retinoic acid in which the double bond which is alpha,beta- to the carboxy group is isomerised to Z configuration. A synthetic retinoid, it is used for the treatment of severe cases of acne and other skin diseases. | 3.23 | 1 | 0 | retinoic acid | antineoplastic agent; keratolytic drug; teratogenic agent |
| epoprostenol [no description available] | 3.23 | 1 | 0 | prostaglandins I | mouse metabolite |
| indocyanine green [no description available] | 3.23 | 1 | 0 | 1,1-diunsubstituted alkanesulfonate; benzoindole; cyanine dye | |
| triprolidine Triprolidine: Histamine H1 antagonist used in allergic rhinitis; ASTHMA; and URTICARIA. It is a component of COUGH and COLD medicines. It may cause drowsiness.. triprolidine : An N-alkylpyrrolidine that is acrivastine in which the pyridine ring is lacking the propenoic acid substituent. It is a sedating antihistamine that is used (generally as the monohydrochloride monohydrate) for the relief of the symptoms of uticaria, rhinitis, and various pruritic skin disorders. | 3.23 | 1 | 0 | N-alkylpyrrolidine; olefinic compound; pyridines | H1-receptor antagonist |
| pitavastatin pitavastatin : A dihydroxy monocarboxylic acid that is (6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]hept-6-enoic acid in which the two hydroxy groups are located at positions 3 and 5 (the 3R,5S-stereoisomer). Used as its calcium salt for treatment of hypercholesterolemia (elevated levels of cholesterol in the blood) on patients unable to sufficiently lower their cholesterol levels by diet and exercise. | 3.23 | 1 | 0 | cyclopropanes; dihydroxy monocarboxylic acid; monofluorobenzenes; quinolines; statin (synthetic) | antioxidant |
| ethamolin monoethanolamine oleate: used for treatment of pyogenic granuloma | 3.23 | 1 | 0 | long-chain fatty acid | |
| alatrofloxacin mesylate [no description available] | 3.23 | 1 | 0 | ||
| codeine [no description available] | 3.23 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound | antitussive; drug allergen; environmental contaminant; opioid analgesic; opioid receptor agonist; prodrug; xenobiotic |
| cyclosporine ramihyphin A: one of the metabolites produced by Fusarium sp. S-435; RN given refers to cpd with unknown MF | 3.23 | 1 | 0 | homodetic cyclic peptide | anti-asthmatic drug; anticoronaviral agent; antifungal agent; antirheumatic drug; carcinogenic agent; dermatologic drug; EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor; geroprotector; immunosuppressive agent; metabolite |
| acitretin Acitretin: An oral retinoid effective in the treatment of psoriasis. It is the major metabolite of ETRETINATE with the advantage of a much shorter half-life when compared with etretinate.. acitretin : A retinoid that consists of 3,7-dimethylnona-2,4,6,8-tetraenoic acid having a 4-methoxy-2,3,6-trimethylphenyl group attached at position 9. | 3.23 | 1 | 0 | acitretin; alpha,beta-unsaturated monocarboxylic acid; retinoid | keratolytic drug |
| estropipate estropipate: used therapeutically in menopausal patients | 3.23 | 1 | 0 | piperazinium salt; steroid sulfate | |
| hydromorphone Hydromorphone: An opioid analgesic made from MORPHINE and used mainly as an analgesic. It has a shorter duration of action than morphine.. hydromorphone : A morphinane alkaloid that is a hydrogenated ketone derivative of morphine. A semi-synthetic drug, it is a centrally acting pain medication of the opioid class. | 3.23 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound | mu-opioid receptor agonist; opioid analgesic |
| levetiracetam Levetiracetam: A pyrrolidinone and acetamide derivative that is used primarily for the treatment of SEIZURES and some movement disorders, and as a nootropic agent.. levetiracetam : A pyrrolidinone and carboxamide that is N-methylpyrrolidin-2-one in which one of the methyl hydrogens is replaced by an aminocarbonyl group, while another is replaced by an ethyl group (the S enantiomer). An anticonvulsant, it is used for the treatment of epilepsy in both human and veterinary medicine. | 3.23 | 1 | 0 | pyrrolidin-2-ones | anticonvulsant; environmental contaminant; xenobiotic |
| ly 163892 loracarbef: 1-carbacephem antibiotic; has a broad spectrum of antimicrobial activity; structure given in first source; carbacephems differ from cephalosporins in the substitution of a sulfur atom in the dihydrothiazine ring with a methylene group to form a tetrahydropyridine ring. loracarbef : A synthetic "carba" analogue of cefaclor, with carbon replacing sulfur at position 1. Used to treat a wide range of infections caused by both gram-positive and gram-negative bacteria. | 3.23 | 1 | 0 | carbacephem; zwitterion | antibacterial drug; antimicrobial agent |
| nabilone nabilone: cannabinol deriv; RN given refers to cpd without isomeric designation; structure | 3.23 | 1 | 0 | ||
| naloxone Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose. | 3.23 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound; tertiary alcohol | antidote to opioid poisoning; central nervous system depressant; mu-opioid receptor antagonist |
| oxycodone Oxycodone: A semisynthetic derivative of CODEINE.. oxycodone : A semisynthetic opioid of formula C18H21NO4 that is derived from thebaine. It is a moderately potent opioid analgesic, generally used for relief of moderate to severe pain. | 3.23 | 1 | 0 | organic heteropentacyclic compound; semisynthetic derivative | antitussive; mu-opioid receptor agonist; opioid analgesic |
| oxymorphone Oxymorphone: An opioid analgesic with actions and uses similar to those of MORPHINE, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092) | 3.23 | 1 | 0 | morphinane alkaloid | |
| vitamin k 1 Vitamin K 1: A family of phylloquinones that contains a ring of 2-methyl-1,4-naphthoquinone and an isoprenoid side chain. Members of this group of vitamin K 1 have only one double bond on the proximal isoprene unit. Rich sources of vitamin K 1 include green plants, algae, and photosynthetic bacteria. Vitamin K1 has antihemorrhagic and prothrombogenic activity.. phylloquinone : A member of the class of phylloquinones that consists of 1,4-naphthoquinone having methyl and phytyl groups at positions 2 and 3 respectively. The parent of the class of phylloquinones. | 3.23 | 1 | 0 | phylloquinones; vitamin K | cofactor; human metabolite; plant metabolite |
| sirolimus Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.. sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent. | 3.23 | 1 | 0 | antibiotic antifungal drug; cyclic acetal; cyclic ketone; ether; macrolide lactam; organic heterotricyclic compound; secondary alcohol | antibacterial drug; anticoronaviral agent; antineoplastic agent; bacterial metabolite; geroprotector; immunosuppressive agent; mTOR inhibitor |
| topiramate Topiramate: A sulfamate-substituted fructose analog that was originally identified as a hypoglycemic agent. It is used for the treatment of EPILEPSY and MIGRAINE DISORDERS, and may also promote weight loss.. topiramate : A hexose derivative that is 2,3:4,5-di-O-isopropylidene-beta-D-fructopyranose in which the hydroxy group has been converted to the corresponding sulfamate ester. It blocks voltage-dependent sodium channels and is used as an antiepileptic and for the prevention of migraine. | 3.23 | 1 | 0 | cyclic ketal; ketohexose derivative; sulfamate ester | anticonvulsant; sodium channel blocker |
| trospium chloride trospium chloride : An organic chloride salt of trospium. It is an antispasmodic drug used for the treatment of overactive bladder. | 3.23 | 1 | 0 | ||
| morphine Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn. | 3.23 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound; tertiary amino compound | anaesthetic; drug allergen; environmental contaminant; geroprotector; mu-opioid receptor agonist; opioid analgesic; plant metabolite; vasodilator agent; xenobiotic |
| benzphetamine Benzphetamine: A sympathomimetic agent with properties similar to DEXTROAMPHETAMINE. It is used in the treatment of obesity. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1222). benzphetamine : Dextroamphetamine in which the the hydrogens attached to the amino group are substituted by a methyl and a benzyl group. A sympathomimetic agent with properties similar to dextroamphetamine, it is used as its hydrochloride salt in the treatment of obesity. | 3.23 | 1 | 0 | amphetamines; tertiary amine | adrenergic uptake inhibitor; appetite depressant; dopamine uptake inhibitor; sympathomimetic agent |
| deamino arginine vasopressin Deamino Arginine Vasopressin: A synthetic analog of the pituitary hormone, ARGININE VASOPRESSIN. Its action is mediated by the VASOPRESSIN receptor V2. It has prolonged antidiuretic activity, but little pressor effects. It also modulates levels of circulating FACTOR VIII and VON WILLEBRAND FACTOR. | 3.23 | 1 | 0 | heterodetic cyclic peptide | diagnostic agent; renal agent; vasopressin receptor agonist |
| dexmedetomidine [no description available] | 3.23 | 1 | 0 | medetomidine | alpha-adrenergic agonist; analgesic; non-narcotic analgesic; sedative |
| goserelin Goserelin: A synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE. Goserelin is used in treatments of malignant NEOPLASMS of the prostate, uterine fibromas, and metastatic breast cancer. | 3.23 | 1 | 0 | organic molecular entity | |
| nalbuphine Nalbuphine: A narcotic used as a pain medication. It appears to be an agonist at KAPPA RECEPTORS and an antagonist or partial agonist at MU RECEPTORS. | 3.23 | 1 | 0 | organic heteropentacyclic compound | mu-opioid receptor antagonist; opioid analgesic |
| nateglinide Nateglinide: A phenylalanine and cyclohexane derivative that acts as a hypoglycemic agent by stimulating the release of insulin from the pancreas. It is used in the treatment of TYPE 2 DIABETES.. nateglinide : An N-acyl-D-phenylalanine resulting from the formal condensation of the amino group of D-phenylalanine with the carboxy group of trans-4-isopropylcyclohexanecarboxylic acid. An orally-administered, rapidly-absorbed, short-acting insulinotropic agent, it is used for the treatment of type 2 diabetes mellitus. | 3.23 | 1 | 0 | phenylalanine derivative | |
| vinorelbine [no description available] | 3.23 | 1 | 0 | acetate ester; methyl ester; organic heteropentacyclic compound; organic heterotetracyclic compound; ring assembly; vinca alkaloid | antineoplastic agent; photosensitizing agent |
| silodosin silodosin: an alpha(1a)-adrenoceptor-selective antagonist; structure given in first source | 3.23 | 1 | 0 | indolecarboxamide | |
| fluvoxamine Fluvoxamine: A selective serotonin reuptake inhibitor that is used in the treatment of DEPRESSION and a variety of ANXIETY DISORDERS.. fluvoxamine : An oxime O-ether that is benzene substituted by a (1E)-N-(2-aminoethoxy)-5-methoxypentanimidoyl group at position 1 and a trifluoromethyl group at position 4. It is a selective serotonin reuptake inhibitor that is used for the treatment of obsessive-compulsive disorder. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; 5-methoxyvalerophenone O-(2-aminoethyl)oxime | antidepressant; anxiolytic drug; serotonin uptake inhibitor |
| su 11248 [no description available] | 3.23 | 1 | 0 | monocarboxylic acid amide; pyrroles | angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; immunomodulator; neuroprotective agent; vascular endothelial growth factor receptor antagonist |
| (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid : A dihydroxy monocarboxylic acid that is N-isopropylindole which is substituted at position 3 by a p-fluorophenyl group and at position 2 by a 6-carboxy-3,5-dihydroxyhex-1-en-1-yl group. It has four possible diastereoisomers. | 3.23 | 1 | 0 | dihydroxy monocarboxylic acid; indoles; organofluorine compound | |
| levorphanol Levorphanol: A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection. | 3.23 | 1 | 0 | morphinane alkaloid | |
| naltrexone Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.. naltrexone : An organic heteropentacyclic compound that is naloxone substituted in which the allyl group attached to the nitrogen is replaced by a cyclopropylmethyl group. A mu-opioid receptor antagonist, it is used to treat alcohol dependence. | 3.23 | 1 | 0 | cyclopropanes; morphinane-like compound; organic heteropentacyclic compound | antidote to opioid poisoning; central nervous system depressant; environmental contaminant; mu-opioid receptor antagonist; xenobiotic |
| dextromethorphan Dextromethorphan: Methyl analog of DEXTRORPHAN that shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (RECEPTORS, N-METHYL-D-ASPARTATE) and acts as a non-competitive channel blocker. It is one of the widely used ANTITUSSIVES, and is also used to study the involvement of glutamate receptors in neurotoxicity.. dextromethorphan : A 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene in which the sterocenters at positions 4a, 10 and 10a have S-configuration. It is a prodrug of dextrorphan and used as an antitussive drug for suppressing cough. | 3.23 | 1 | 0 | 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene | antitussive; environmental contaminant; neurotoxin; NMDA receptor antagonist; oneirogen; prodrug; xenobiotic |
| butorphanol Butorphanol: A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain.. butorphanol : Levorphanol in which a hydrogen at position 14 of the morphinan skeleton is substituted by hydroxy and one of the hydrogens of the N-methyl group is substituted by cyclopropyl. A semi-synthetic opioid agonist-antagonist analgesic, it is used as its (S,S)-tartaric acid salt for relief or moderate to severe pain. | 3.23 | 1 | 0 | morphinane alkaloid | antitussive; kappa-opioid receptor agonist; mu-opioid receptor agonist; opioid analgesic |
| cefixime [no description available] | 3.23 | 1 | 0 | cephalosporin | antibacterial drug; drug allergen |
| lisinopril Lisinopril: One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure. | 3.23 | 1 | 0 | dipeptide | EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| benazepril benazepril: structure given in first source. benazepril : A benzazepine that is benazeprilat in which the carboxy group of the 2-amino-4-phenylbutanoic acid moiety has been converted to the corresponding ethyl ester. It is used (generally as its hydrochloride salt) as a prodrug for the angiotensin-converting enzyme inhibitor benazeprilat in the treatment of hypertension and heart failure. | 3.23 | 1 | 0 | benzazepine; dicarboxylic acid monoester; ethyl ester; lactam | EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug |
| ramipril Ramipril: A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.. ramipril : A dipeptide that is the prodrug for ramiprilat, the active metabolite obtained by hydrolysis of the ethyl ester group. An angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.. quark : Quarks comprise one of two classes of the fundamental particles. Quarks possess fractional electric charges and are not observed in free state. The word "quark" first appears in James Joyce's Finnegans Wake and has been chosen by Murray Gell-Mann as a name for fundamental building blocks of particles. | 3.23 | 1 | 0 | azabicycloalkane; cyclopentapyrrole; dicarboxylic acid monoester; dipeptide; ethyl ester | bradykinin receptor B2 agonist; cardioprotective agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; matrix metalloproteinase inhibitor; prodrug |
| verteporfin (2R,2(1)S)-8-ethenyl-2(1),2(2)-bis(methoxycarbonyl)-17-(3-methoxy-3-oxopropyl)-2,7,12,18-tetramethyl-2,2(1)-dihydrobenzo[b]porphyrin-13-propanoic acid : The 2(1),2(2),17-trimethyl ester of (2R,2(1)S)-2(1),2(2)-dicarboxy-8-ethenyl-2,7,12,18-tetramethyl-2,2(1)-dihydrobenzo[b]porphyrin-13,17-dipropanoic acid. | 3.23 | 1 | 0 | ||
| indinavir sulfate Indinavir: A potent and specific HIV protease inhibitor that appears to have good oral bioavailability. | 3.23 | 1 | 0 | dicarboxylic acid diamide; N-(2-hydroxyethyl)piperazine; piperazinecarboxamide | HIV protease inhibitor |
| zimeldine Zimeldine: One of the SEROTONIN UPTAKE INHIBITORS formerly used for depression but was withdrawn worldwide in September 1983 because of the risk of GUILLAIN-BARRE SYNDROME associated with its use. (From Martindale, The Extra Pharmacopoeia, 29th ed, p385) | 3.23 | 1 | 0 | styrenes | |
| enalapril Enalapril: An angiotensin-converting enzyme inhibitor that is used to treat HYPERTENSION and HEART FAILURE.. enalapril : A dicarboxylic acid monoester that is ethyl 4-phenylbutanoate in which a hydrogen alpha to the carboxy group is substituted by the amino group of L-alanyl-L-proline (S-configuration). | 3.23 | 1 | 0 | dicarboxylic acid monoester; dipeptide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; geroprotector; prodrug |
| trientine hydrochloride [no description available] | 3.23 | 1 | 0 | ||
| n-methylscopolamine bromide scopolamine methobromide : A quaternary ammonium salt resulting from the reaction of the amino group of scopolamine with methyl bromide. | 3.23 | 1 | 0 | ||
| bleomycin [no description available] | 3.23 | 1 | 0 | bleomycin | antineoplastic agent; metabolite |
| enalaprilat anhydrous Enalaprilat: The active metabolite of ENALAPRIL and one of the potent, intravenously administered, ANGIOTENSIN-CONVERTING ENZYME INHIBITORS. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion.. enalaprilat dihydrate : The dihydrate form of enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor that is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is administered by intravenous injection.. enalaprilat (anhydrous) : Enalapril in which the ethyl ester group has been hydrolysed to the corresponding carboxylic acid. Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor and is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is given by intravenous injection, usually as the dihydrate. | 3.23 | 1 | 0 | dicarboxylic acid; dipeptide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| ximelagatran ximelagatran: prodrug (via hydroxylation) of melagatran & a direct thrombin inhibitor; liver toxicity concerns so AZD0837 being developed to replace this. ximelagatran : A member of the class of azetidines that is melagatran in which the carboxylic acid group has been converted to the corresponding ethyl ester and in which the amidine group has been converted into the corresponding amidoxime. A prodrug for melagatran, ximelagatran was the first orally available direct thrombin inhibitor to be brought to market as an anticoagulant, but was withdrawn in 2006 following reports of it causing liver damage. | 3.23 | 1 | 0 | amidoxime; azetidines; carboxamide; ethyl ester; hydroxylamines; secondary amino compound; secondary carboxamide; tertiary carboxamide | anticoagulant; EC 3.4.21.5 (thrombin) inhibitor; prodrug; serine protease inhibitor |
| cefuroxime [no description available] | 3.23 | 1 | 0 | 3-(carbamoyloxymethyl)cephalosporin; furans; oxime O-ether | drug allergen |
| ceftriaxone [no description available] | 3.23 | 1 | 0 | 1,2,4-triazines; 1,3-thiazoles; cephalosporin; oxime O-ether | antibacterial drug; drug allergen; EC 3.5.2.6 (beta-lactamase) inhibitor |
| cefepime Cefepime: A fourth-generation cephalosporin antibacterial agent that is used in the treatment of infections, including those of the abdomen, urinary tract, respiratory tract, and skin. It is effective against PSEUDOMONAS AERUGINOSA and may also be used in the empiric treatment of FEBRILE NEUTROPENIA.. cefepime : A cephalosporin bearing (1-methylpyrrolidinium-1-yl)methyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. | 3.23 | 1 | 0 | cephalosporin; oxime O-ether | antibacterial drug |
| pafuramidine pafuramidine: a prodrug of furamidine | 3.23 | 1 | 0 | ||
| ceftazidime [no description available] | 3.23 | 1 | 0 | cephalosporin; oxime O-ether | antibacterial drug; drug allergen; EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor |
| trandolapril trandolapril : A heterobicylic compound that is (2S,3aR,7aS)-1-[(2S)-2-aminopropanoyl]octahydro-1H-indole-2-carboxylic acid in which the hydrogen of the amino group is substituted by a (2R)-1-ethoxy-1-oxo-4-phenylbutan-2-yl group. It is a angiotensin-converting enzyme inhibitor and a prodrug used for the treatment of hypertension. | 3.23 | 1 | 0 | dicarboxylic acid monoester; dipeptide; ethyl ester; organic heterobicyclic compound; secondary amino compound; tertiary carboxamide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug |
| pregabalin Pregabalin: A gamma-aminobutyric acid (GABA) derivative that functions as a CALCIUM CHANNEL BLOCKER and is used as an ANTICONVULSANT as well as an ANTI-ANXIETY AGENT. It is also used as an ANALGESIC in the treatment of NEUROPATHIC PAIN and FIBROMYALGIA.. pregabalin : A gamma-amino acid that is gamma-aminobutyric acid (GABA) carrying an isobutyl substitutent at the beta-position (the S-enantiomer). Binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues. | 3.23 | 1 | 0 | gamma-amino acid | anticonvulsant; calcium channel blocker |
| alvimopan anhydrous alvimopan: mu opioid receptor antagonist; intended to treat constipation in patients taking opiates for pain | 3.23 | 1 | 0 | peptide | |
| aliskiren aliskiren: orally active nonpeptidic renin inhibitor. aliskiren : A monomethoxybenzene compound having a 3-methoxypropoxy group at the 2-position and a multi-substituted branched alkyl substituent at the 4-position. | 3.23 | 1 | 0 | monocarboxylic acid amide; monomethoxybenzene | antihypertensive agent |
| famotidine [no description available] | 3.23 | 1 | 0 | 1,3-thiazoles; guanidines; sulfonamide | anti-ulcer drug; H2-receptor antagonist; P450 inhibitor |
| cefotaxime Cefotaxime: Semisynthetic broad-spectrum cephalosporin.. cefotaxime : A cephalosporin compound having acetoxymethyl and [2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino side groups. | 3.23 | 1 | 0 | 1,3-thiazoles; cephalosporin; oxime O-ether | antibacterial drug; drug allergen |
| aztreonam [no description available] | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; monobactam | antibacterial drug; drug allergen; EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor |
| cefpodoxime [no description available] | 3.23 | 1 | 0 | carboxylic acid; cephalosporin | antibacterial drug |
| palonosetron Palonosetron: Isoquinoline and quinuclidine derivative that acts as a 5-HT3 RECEPTOR antagonist. It is used in the prevention of nausea and vomiting induced by cytotoxic chemotherapy, and for the prevention of post-operative nausea and vomiting.. palonosetron : An organic heterotricyclic compound that is an antiemetic used (as its hydrochloride salt) in combination with netupitant (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy. | 3.23 | 1 | 0 | azabicycloalkane; delta-lactam; organic heterotricyclic compound | antiemetic; serotonergic antagonist |
| rifaximin [no description available] | 3.23 | 1 | 0 | acetate ester; cyclic ketal; lactam; macrocycle; organic heterohexacyclic compound; rifamycins; semisynthetic derivative | antimicrobial agent; gastrointestinal drug; orphan drug |
| everolimus [no description available] | 3.23 | 1 | 0 | cyclic acetal; cyclic ketone; ether; macrolide lactam; primary alcohol; secondary alcohol | anticoronaviral agent; antineoplastic agent; geroprotector; immunosuppressive agent; mTOR inhibitor |
| ixabepilone [no description available] | 3.23 | 1 | 0 | 1,3-thiazoles; beta-hydroxy ketone; epoxide; lactam; macrocycle | antineoplastic agent; microtubule-destabilising agent |
| ceftizoxime [no description available] | 3.23 | 1 | 0 | cephalosporin | antibacterial drug |
| 1-methyl-d-lysergic acid butanolamide [no description available] | 3.23 | 1 | 0 | ergot alkaloid; monocarboxylic acid amide | serotonergic antagonist; sympatholytic agent; vasoconstrictor agent |
| nitrofurantoin Nitrofurantoin: A urinary anti-infective agent effective against most gram-positive and gram-negative organisms. Although sulfonamides and antibiotics are usually the agents of choice for urinary tract infections, nitrofurantoin is widely used for prophylaxis and long-term suppression.. nitrofurantoin : An imidazolidine-2,4-dione that is hydantoin substituted at position 1 by a [(5-nitro-2-furyl)methylene]amino group. An antibiotic that damages bacterial DNA. | 3.23 | 1 | 0 | imidazolidine-2,4-dione; nitrofuran antibiotic; organonitrogen heterocyclic antibiotic; organooxygen heterocyclic antibiotic | antibacterial drug; antiinfective agent; hepatotoxic agent |
| dantrolene [no description available] | 3.23 | 1 | 0 | ||
| cefdinir [no description available] | 3.23 | 1 | 0 | cephalosporin; ketoxime | antibacterial drug |
| etonogestrel [no description available] | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound | contraceptive drug; female contraceptive drug; progestin |
| temsirolimus [no description available] | 3.23 | 1 | 0 | macrolide lactam | |
| dutasteride Dutasteride: A 5-ALPHA-REDUCTASE INHIBITOR that is reported to inhibit both type-1 and type2 isoforms of the enzyme and is used to treat BENIGN PROSTATIC HYPERPLASIA.. dutasteride : An aza-steroid that is inasteride in which the tert-butyl group is replaced by a 2,5-bis(trifluoromethyl)phenyl group. A synthetic 4-azasteroid, dutasteride is a selective inhibitor of both the type 1 and type 2 isoforms of steroid 5alpha-reductase, an intracellular enzyme that converts testosterone to 5alpha-dihydrotestosterone. Dutasteride is used for the treatment of symptomatic benign prostatic hyperplasia in men with an enlarged prostate gland. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; aza-steroid; delta-lactam | antihyperplasia drug; EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor |
| nps2143 [no description available] | 3.15 | 1 | 0 | ||
| lu 208075 ambrisentan: an ET(A) receptor antagonist and antihypertensive agent; studied for use in pulmonary arterial hypertension | 3.23 | 1 | 0 | diarylmethane | |
| jwh-133 1,1-dimethylbutyl-1-deoxy-Delta(9)-THC: a CB2 receptor agonists; no further information available on 8/2001. JWH-133 : A dibenzopyran that is Delta(9)-tetrahydrocannabinol which is lacking the hydroxy group and in which the pentyl group at position 3 has been replaced by a 1,1-dimethylbutyl group. A potent and highly selective CB2 receptor agonist. | 3.15 | 1 | 0 | benzochromene; dibenzopyran; organic heterotricyclic compound | analgesic; anti-inflammatory agent; antineoplastic agent; apoptosis inhibitor; CB2 receptor agonist; opioid analgesic; vasodilator agent |
| bibx 1382bs BIBX 1382BS: an ErbB receptor kinase inhibitor; no further information available 4/2001 | 3.23 | 1 | 0 | substituted aniline | |
| fesoterodine fesoterodine: a muscarinic antagonist for treatment of overactive bladder | 3.23 | 1 | 0 | diarylmethane | |
| relacatib relacatib: a cathepsin K inhibitor; structure in first source | 3.15 | 1 | 0 | ||
| gemifloxacin Gemifloxacin: A naphthyridine and fluoroquinolone derivative antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used for the treatment of community-acquired pneumonia and acute bacterial infections associated with chronic bronchitis.. gemifloxacin : A 1,4-dihydro-1,8-naphthyridine with a carboxy group at the 3-position, an oxo sustituent at the 4-position, a fluoro substituent at the 5-position and a substituted pyrrolin-1-yl group at the 7-position. | 3.23 | 1 | 0 | 1,8-naphthyridine derivative; fluoroquinolone antibiotic; monocarboxylic acid; quinolone antibiotic | antibacterial drug; antimicrobial agent; topoisomerase IV inhibitor |
| dexlansoprazole Dexlansoprazole: The R-isomer of lansoprazole that is used to treat severe GASTROESOPHAGEAL REFLUX DISEASE. | 3.23 | 1 | 0 | benzimidazoles; sulfoxide | |
| fosinopril [no description available] | 3.23 | 1 | 0 | ||
| armodafinil armodafinil : A 2-[(diphenylmethyl)sulfinyl]acetamide that has R configuration at the sulfur atom. Like its racemate, modafinil, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. Peak concentration in the blood later occurs later following administration than with modafinil, so it is thought that armodafinil may be more effective than modafinil in treating people with excessive daytime sleepiness. | 3.23 | 1 | 0 | 2-[(diphenylmethyl)sulfinyl]acetamide | central nervous system stimulant; eugeroic |
| ono4819 ONO4819: prostanoid receptor EP4 agonist | 3.15 | 1 | 0 | benzyl ether | |
| sincalide Sincalide: An octapeptide hormone present in the intestine and brain. When secreted from the gastric mucosa, it stimulates the release of bile from the gallbladder and digestive enzymes from the pancreas. | 3.23 | 1 | 0 | oligopeptide | |
| tapentadol Tapentadol: An opioid analgesic, MU OPIOID RECEPTOR agonist, and noradrenaline reuptake inhibitor that is used in the treatment of moderate to severe pain, and of pain associated with DIABETIC NEUROPATHIES. | 3.23 | 1 | 0 | alkylbenzene | |
| mk-0429 [no description available] | 3.15 | 1 | 0 | ||
| pentagastrin Pentagastrin: A synthetic pentapeptide that has effects like gastrin when given parenterally. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor, and has been used as a diagnostic aid. | 3.23 | 1 | 0 | organic molecular entity | |
| cefditoren cefditoren: structure given in first source; RN given refers to the (6R-(3(Z),6alpha,7beta(Z)))-isomer. cefditoren : A broad spectrum, third-generation cephalosporin antibiotic with (Z)-2-(4-methyl-1,3-thiazol-5-yl)ethenyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. Generally administered as its orally absorbed pivaloyloxymethyl ester prodrug, it is used for the treatment of mild to moderate infections caused by susceptible strains of microorganisms in acute bacterial exacerbation of chronic bronchitis, community-acquired pneumonia, pharyngitis/tonsillitis, and uncomplicated skin and skin-structure infections. | 3.23 | 1 | 0 | carboxylic acid; cephalosporin | antibacterial drug |
| pazopanib pazopanib: a protein kinase inhibitor. pazopanib : A pyrimidine that is 5-(pyrimidin-2-yl}amino-2-methylbenzenesulfonamide substituted at position 4 by a (2,3-dimethylindazol-6-yl)(methyl)amino group. Used as its hydrochloride salt for treatment of kidney cancer. | 3.23 | 1 | 0 | aminopyrimidine; indazoles; sulfonamide | angiogenesis modulating agent; antineoplastic agent; tyrosine kinase inhibitor; vascular endothelial growth factor receptor antagonist |
| odanacatib odanacatib: a selective inhibitor of cathepsin K for the treatment of post-menopausal osteoporosis; structure in first source | 3.15 | 1 | 0 | ||
| prasugrel hydrochloride Prasugrel Hydrochloride: A piperazine derivative and PLATELET AGGREGATION INHIBITOR that is used to prevent THROMBOSIS in patients with ACUTE CORONARY SYNDROME; UNSTABLE ANGINA and MYOCARDIAL INFARCTION, as well as in those undergoing PERCUTANEOUS CORONARY INTERVENTIONS.. prasugrel hydrochloride : A racemate comprising equal amounts of (R)- and (S)-prasugrel hydrochloride. Used to prevent blood clots in people with acute coronary syndrome who are undergoing a procedure after a recent heart attack or stroke, and in people with certain disorders of the heart or blood vessels. | 3.23 | 1 | 0 | ||
| balicatib balicatib: cathepsin K inhibitor | 3.15 | 1 | 0 | ||
| saracatinib [no description available] | 3.15 | 1 | 0 | aromatic ether; benzodioxoles; diether; N-methylpiperazine; organochlorine compound; oxanes; quinazolines; secondary amino compound | anticoronaviral agent; antineoplastic agent; apoptosis inducer; autophagy inducer; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor; radiosensitizing agent |
| baci-im [no description available] | 3.23 | 1 | 0 | homodetic cyclic peptide; polypeptide; zwitterion | antibacterial agent; antimicrobial agent |
| bms 477118 [no description available] | 3.23 | 1 | 0 | adamantanes; azabicycloalkane; monocarboxylic acid amide; nitrile; tertiary alcohol | EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; hypoglycemic agent |
| nystatin a1 Nystatin: Macrolide antifungal antibiotic complex produced by Streptomyces noursei, S. aureus, and other Streptomyces species. The biologically active components of the complex are nystatin A1, A2, and A3.. nystatin : A heterogeneous mixture of polyene compounds produced by cultures of Streptomyces noursei. It mainly consists of three biologically active components designated nystatin A1, nystatin A2, and nystatin A3. It is used to treat oral and dermal fungal infections.. nystatin A1 : A polyene macrolide antibiotic; part of the nystatin complex produced by several Streptomyces species. It is an antifungal antibiotic used for the treatment of topical fungal infections caused by a broad spectrum of fungal pathogens comprising yeast-like and filamentous species. | 3.23 | 1 | 0 | nystatins | |
| N-methyl-N-[2-[[[2-[(2-oxo-1,3-dihydroindol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide [no description available] | 3.15 | 1 | 0 | sulfonamide | |
| milnacipran [no description available] | 3.23 | 1 | 0 | acetamides | |
| pf-562,271 [no description available] | 3.15 | 1 | 0 | indoles | |
| scopolamine hydrobromide [no description available] | 3.23 | 1 | 0 | ||
| bivalirudin bivalirudin: designed to bind to the alpha-thrombin catalytic site and anion-binding exosite for fibrin(ogen) recognition. bivalirudin : A synthetic peptide of 20 amino acids, comprising D-Phe, Pro, Arg, Pro, Gly, Gly, Gly, Gly, Asn, Gly, Asp, Phe, Glu, Glu, Ile, Pro, Glu, Glu, Tyr, and Leu in sequence. A congener of hirudin (a naturally occurring drug found in the saliva of the medicinal leech), it a specific and reversible inhibitor of thrombin, and is used as an anticoagulant. | 3.23 | 1 | 0 | polypeptide | anticoagulant; EC 3.4.21.5 (thrombin) inhibitor |
| enfuvirtide Enfuvirtide: A synthetic 36-amino acid peptide that corresponds to the heptad repeat sequence of HIV-1 gp41. It blocks HIV cell fusion and viral entry and is used with other anti-retrovirals for combination therapy of HIV INFECTIONS and AIDS.. enfuvirtide : A synthetic 36-amino acid peptide consisting of N-acetyltyrosyl, threonyl, seryl, leucyl, isoleucyl, histidyl, seryl, leucyl, isoleucyl, alpha-glutamyl, alpha-glutamyl, seryl, glutaminyl, asparaginyl, glutaminyl, glutaminyl, alpha-glutamyl, lysyl, asparaginyl, alpha-glutamyl, alpha-glutamyl, alpha-glutamyl, leucyl, leucyl, alpha-glutamyl, leucyl, alpha-aspartyl, lysyl, tryptophyl, alanyl, seryl, leucyl, tryptophyl, asparaginyl, tryptophyl, and phenylalaninamide residues joined in sequence. An HIV fusion inhibitor, it was the first of a novel class of antiretroviral drugs used in combination therapy for the treatment of HIV-1 infection. It interferes with entry of HIV into cells by binding to the gp41 sub-unit of the viral envelope glycoprotein, so inhibiting fusion of viral and cellular membranes. | 3.23 | 1 | 0 | ||
| ganirelix [no description available] | 3.23 | 1 | 0 | polypeptide | |
| salmon calcitonin [no description available] | 3.23 | 1 | 0 | heterodetic cyclic peptide; peptide hormone; polypeptide | bone density conservation agent; metabolite |
| ly-146032 [no description available] | 3.23 | 1 | 0 | heterodetic cyclic peptide; lipopeptide antibiotic; lipopeptide; macrocycle; macrolide | antibacterial drug; bacterial metabolite; calcium-dependent antibiotics |
| acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ilys-prolyl-alaninamide acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ILys-prolyl-alaninamide: FE-200486 is the acetate salt | 3.23 | 1 | 0 | polypeptide | |
| exenatide [no description available] | 3.23 | 1 | 0 | ||
| WAY-316606 WAY-316606 : A sulfonamide resulting from the formal condensation of the sulfonic acid group of 5-(phenylsulfonyl)-2-(trifluoromethyl)benzenesulfonic acid with the primary amino group of piperidin-4-amine. An inhibitor of secreted Frizzled-Related Protein-1 (sFRP-1). | 3.15 | 1 | 0 | (trifluoromethyl)benzenes; piperidines; secondary amino compound; sulfonamide; sulfone | secreted frizzled-related protein 1 inhibitor |
| mesna Mesna: A sulfhydryl compound used to prevent urothelial toxicity by inactivating metabolites from ANTINEOPLASTIC AGENTS, such as IFOSFAMIDE or CYCLOPHOSPHAMIDE. | 3.23 | 1 | 0 | organosulfonic acid | |
| sodium lactate Sodium Lactate: The sodium salt of racemic or inactive lactic acid. It is a hygroscopic agent used intravenously as a systemic and urinary alkalizer.. sodium lactate : An organic sodium salt having lactate as the counterion. | 3.23 | 1 | 0 | lactate salt; organic sodium salt | food acidity regulator; food preservative |
| sodium iothalamate [no description available] | 3.23 | 1 | 0 | ||
| cetrorelix cetrorelix: LHRH antagonist. cetrorelix : A synthetic ten-membered oligopeptide comprising N-acetyl-3-(naphthalen-2-yl)-D-alanyl, 4-chloro-D-phenylalanyl, 3-(pyridin-3-yl)-D-alanyl, L-seryl, L-tyrosyl, N(5)-carbamoyl-D-ornithyl, L-leucyl, L-arginyl, L-prolyl, and D-alaninamide residues coupled in sequence. A gonadotrophin-releasing hormone (GnRH) antagonist, it is used for treatment of infertility and of hormone-sensitive cancers of the prostate and breast. | 3.23 | 1 | 0 | oligopeptide | antineoplastic agent; GnRH antagonist |
| vel-0230 VEL-0230: a cathepsin K antagonist | 3.15 | 1 | 0 | ||
| ascorbic acid Ascorbic Acid: A six carbon compound related to glucose. It is found naturally in citrus fruits and many vegetables. Ascorbic acid is an essential nutrient in human diets, and necessary to maintain connective tissue and bone. Its biologically active form, vitamin C, functions as a reducing agent and coenzyme in several metabolic pathways. Vitamin C is considered an antioxidant.. L-ascorbic acid : The L-enantiomer of ascorbic acid and conjugate acid of L-ascorbate.. L-ascorbate : The L-enantiomer of ascorbate and conjugate base of L-ascorbic acid, arising from selective deprotonation of the 3-hydroxy group. Required for a range of essential metabolic reactions in all animals and plants.. vitamin C : Any member of a group of vitamers that belong to the chemical structural class called butenolides that exhibit biological activity against vitamin C deficiency in animals. The vitamers include L-ascorbic acid and its salt, ionized and oxidized forms. | 3.23 | 1 | 0 | ascorbic acid; vitamin C | coenzyme; cofactor; flour treatment agent; food antioxidant; food colour retention agent; geroprotector; plant metabolite; skin lightening agent |
| raltegravir [no description available] | 3.23 | 1 | 0 | 1,2,4-oxadiazole; dicarboxylic acid amide; hydroxypyrimidine; monofluorobenzenes; pyrimidone; secondary carboxamide | antiviral drug; HIV-1 integrase inhibitor |
| tetracycline Tetracycline: A naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis.. tetracycline : A broad-spectrum polyketide antibiotic produced by the Streptomyces genus of actinobacteria. | 3.23 | 1 | 0 | ||
| oxytetracycline, anhydrous Oxytetracycline: A TETRACYCLINE analog isolated from the actinomycete STREPTOMYCES RIMOSUS and used in a wide variety of clinical conditions.. oxytetracycline : A tetracycline used for treatment of infections caused by a variety of Gram positive and Gram negative microorganisms including Mycoplasma pneumoniae, Pasteurella pestis, Escherichia coli, Haemophilus influenzae (respiratory infections), and Diplococcus pneumoniae. | 3.23 | 1 | 0 | ||
| minocycline Minocycline: A TETRACYCLINE analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant STAPHYLOCOCCUS infections.. minocycline : A tetracycline analogue having a dimethylamino group at position 7 and lacking the methyl and hydroxy groups at position 5. | 3.23 | 1 | 0 | ||
| piroxicam [no description available] | 3.23 | 1 | 0 | benzothiazine; monocarboxylic acid amide; pyridines | analgesic; antirheumatic drug; cyclooxygenase 1 inhibitor; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-steroidal anti-inflammatory drug |
| mobic Meloxicam: A benzothiazine and thiazole derivative that acts as a NSAID and cyclooxygenase-2 (COX-2) inhibitor. It is used in the treatment of RHEUMATOID ARTHRITIS; OSTEOARTHRITIS; and ANKYLOSING SPONDYLITIS.. meloxicam : A benzothiazine that is piroxicam in which the pyridin-2-yl group is replaced by a 5-methyl-1,3-thiazol-2-yl group. A non-steroidal anti-inflammatory drug and selective inhibitor of COX-2, it is used particularly for the management of rheumatoid arthritis. | 3.23 | 1 | 0 | 1,3-thiazoles; benzothiazine; monocarboxylic acid amide | analgesic; antirheumatic drug; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| warfarin Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group. | 3.23 | 1 | 0 | benzenes; hydroxycoumarin; methyl ketone | |
| demeclocycline Demeclocycline: A TETRACYCLINE analog having a 7-chloro and a 6-methyl. Because it is excreted more slowly than tetracycline, it maintains effective blood levels for longer periods of time.. demeclocycline : Tetracycline which lacks the methyl substituent at position 7 and in which the hydrogen para- to the phenolic hydroxy group is substituted by chlorine. Like tetracycline, it is an antibiotic, but being excreted more slowly, effective blood levels are maintained for longer. It is used (mainly as the hydrochloride) for the treatment of Lyme disease, acne and bronchitis, as well as for hyponatraemia (low blood sodium concentration) due to the syndrome of inappropriate antidiuretic hormone (SIADH) where fluid restriction alone has been ineffective. | 3.23 | 1 | 0 | ||
| tipranavir tipranavir: inhibits HIV-1 protease. tipranavir : A pyridine-2-sulfonamide substituted at C-5 by a trifluoromethyl group and at the sulfonamide nitrogen by a dihydropyrone-containing m-tolyl substituent. It is an HIV-1 protease inhibitor. | 3.23 | 1 | 0 | sulfonamide | antiviral drug; HIV protease inhibitor |
| tigecycline [no description available] | 3.23 | 1 | 0 | ||
| fertinex [no description available] | 3.23 | 1 | 0 | ||
| entecavir entecavir (anhydrous) : Guanine substituted at the 9 position by a 4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl group. A synthetic analogue of 2'-deoxyguanosine, it is a nucleoside reverse transcriptase inhibitor with selective antiviral activity against hepatitis B virus. Entecavir is phosphorylated intracellularly to the active triphosphate form, which competes with deoxyguanosine triphosphate, the natural substrate of hepatitis B virus reverse transcriptase, inhibiting every stage of the enzyme's activity, although it has no activity against HIV. It is used for the treatment of chronic hepatitis B. | 3.23 | 1 | 0 | 2-aminopurines; oxopurine; primary alcohol; secondary alcohol | antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| acyclovir Acyclovir: A GUANOSINE analog that acts as an antimetabolite. Viruses are especially susceptible. Used especially against herpes.. acyclovir : An oxopurine that is guanine substituted by a (2-hydroxyethoxy)methyl substituent at position 9. Used in the treatment of viral infections. | 3.23 | 1 | 0 | 2-aminopurines; oxopurine | antimetabolite; antiviral drug |
| folic acid folcysteine: used to promote fertility in chickens. vitamin B9 : Any B-vitamin that exhibits biological activity against vitamin B9 deficiency. Vitamin B9 refers to the many forms of folic acid and its derivatives, including tetrahydrofolic acid (the active form), methyltetrahydrofolate (the primary form found in blood), methenyltetrahydrofolate, folinic acid amongst others. They are present in abundance in green leafy vegetables, citrus fruits, and animal products. Lack of vitamin B9 leads to anemia, a condition in which the body cannot produce sufficient number of red blood cells. Symptoms of vitamin B9 deficiency include fatigue, muscle weakness, and pale skin. | 3.23 | 1 | 0 | folic acids; N-acyl-amino acid | human metabolite; mouse metabolite; nutrient |
| rifampin Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160) | 3.23 | 1 | 0 | cyclic ketal; hydrazone; N-iminopiperazine; N-methylpiperazine; rifamycins; semisynthetic derivative; zwitterion | angiogenesis inhibitor; antiamoebic agent; antineoplastic agent; antitubercular agent; DNA synthesis inhibitor; EC 2.7.7.6 (RNA polymerase) inhibitor; Escherichia coli metabolite; geroprotector; leprostatic drug; neuroprotective agent; pregnane X receptor agonist; protein synthesis inhibitor |
| clozapine Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia. | 3.23 | 1 | 0 | benzodiazepine; N-arylpiperazine; N-methylpiperazine; organochlorine compound | adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; GABA antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; xenobiotic |
| dacarbazine (E)-dacarbazine : A dacarbazine in which the N=N double bond adopts a trans-configuration. | 3.23 | 1 | 0 | dacarbazine | |
| didanosine Didanosine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase; ddI is then metabolized to dideoxyadenosine triphosphate, its putative active metabolite.. didanosine : A purine 2',3'-dideoxyribonucleoside that is inosine in which the hydroxy groups at both the 2' and the 3' positions on the sugar moiety have been replaced by hydrogen. An antiviral drug, it is used as a medication to treat HIV/AIDS. | 3.23 | 1 | 0 | purine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; EC 2.4.2.1 (purine-nucleoside phosphorylase) inhibitor; geroprotector; HIV-1 reverse transcriptase inhibitor |
| ganciclovir [no description available] | 3.23 | 1 | 0 | 2-aminopurines; oxopurine | antiinfective agent; antiviral drug |
| valacyclovir Valacyclovir: A prodrug of acyclovir that is used in the treatment of HERPES ZOSTER and HERPES SIMPLEX VIRUS INFECTION of the skin and mucous membranes, including GENITAL HERPES. | 3.23 | 1 | 0 | L-valyl ester | antiviral drug |
| sildenafil sildenafil : A pyrazolo[4,3-d]pyrimidin-7-one having a methyl substituent at the 1-position, a propyl substituent at the 3-position and a 2-ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl group at the 5-position. | 3.23 | 1 | 0 | piperazines; pyrazolopyrimidine; sulfonamide | EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent |
| olanzapine Olanzapine: A benzodiazepine derivative that binds SEROTONIN RECEPTORS; MUSCARINIC RECEPTORS; HISTAMINE H1 RECEPTORS; ADRENERGIC ALPHA-1 RECEPTORS; and DOPAMINE RECEPTORS. It is an antipsychotic agent used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER; and MAJOR DEPRESSIVE DISORDER; it may also reduce nausea and vomiting in patients undergoing chemotherapy.. olanzapine : A benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4. | 3.23 | 1 | 0 | benzodiazepine; N-arylpiperazine; N-methylpiperazine | antiemetic; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; serotonin uptake inhibitor |
| vardenafil vardenafil : The sulfonamide resulting from formal condensation of the sulfo group of 4-ethoxy-3-(5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one-2-yl)benzenesulfonic acid and the secondary amino group of 4-ethylpiperazine. | 3.23 | 1 | 0 | imidazotriazine; N-alkylpiperazine; N-sulfonylpiperazine | EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; vasodilator agent |
| allopurinol Allopurinol: A XANTHINE OXIDASE inhibitor that decreases URIC ACID production. It also acts as an antimetabolite on some simpler organisms.. allopurinol : A bicyclic structure comprising a pyrazole ring fused to a hydroxy-substituted pyrimidine ring. | 3.23 | 1 | 0 | nucleobase analogue; organic heterobicyclic compound | antimetabolite; EC 1.17.3.2 (xanthine oxidase) inhibitor; gout suppressant; radical scavenger |
| citrovorum factor [no description available] | 3.23 | 1 | 0 | tetrahydrofolic acid | |
| leucovorin 5-formyltetrahydrofolic acid : A formyltetrahydrofolic acid in which the formyl group is located at position 5. | 3.23 | 1 | 0 | formyltetrahydrofolic acid | Escherichia coli metabolite; mouse metabolite |
| rifapentine rifapentine: cyclopentyl derivative of rifampicin | 3.23 | 1 | 0 | N-alkylpiperazine; N-iminopiperazine; rifamycins | antitubercular agent; leprostatic drug |
| bl 4162a anagrelide: imidazoquinazoline derivative which lowers platelet count probably by inhibiting thrombopoiesis and reduces platelet aggregation; used for thrombocythemia; structure in first source. anagrelide : A 1,5-dihydroimidazo[2,1-]quinazoline having an oxo substituent at the 2-position and chloro substituents at the 6- and 7-positions. | 3.23 | 1 | 0 | imidazoquinazoline | anticoagulant; antifibrinolytic drug; cardiovascular drug; platelet aggregation inhibitor |
| tegaserod tegaserod: a nonbenzamide 5-hydroxytryptamine(4) agonist; used in treatment of irritable bowel syndrome; marketing suspended 2007 in US due to higher incidence of MI, stroke, and unstable angina; structure given in first source | 3.23 | 1 | 0 | carboxamidine; guanidines; hydrazines; indoles | gastrointestinal drug; serotonergic agonist |
| pemetrexed pemetrexed disodium : An organic sodium salt that is the disodium salt of N-{4-[2-(2-amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl}-L-glutamic acid. Inhibits thymidylate synthase (TS), 421 dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT). | 3.23 | 1 | 0 | N-acyl-L-glutamic acid; pyrrolopyrimidine | antimetabolite; antineoplastic agent; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; EC 2.1.1.45 (thymidylate synthase) inhibitor; EC 2.1.2.2 (phosphoribosylglycinamide formyltransferase) inhibitor |
| valganciclovir Valganciclovir: A ganciclovir prodrug and antiviral agent that is used to treat CYTOMEGALOVIRUS RETINITIS in patients with AIDS, and for the prevention of CYTOMEGALOVIRUS INFECTIONS in organ transplant recipients who have received an organ from a CMV-positive donor.. valganciclovir : The L-valinyl ester of ganciclovir, into which it is rapidly converted by intestinal and hepatic esterases. It is a synthetic analogue of 2'-deoxyguanosine. | 3.23 | 1 | 0 | L-valyl ester; purines | antiviral drug; prodrug |
| aprepitant Aprepitant: A morpholine neurokinin-1 (NK1) receptor antagonist that is used in the management of nausea and vomiting caused by DRUG THERAPY, and for the prevention of POSTOPERATIVE NAUSEA AND VOMITING.. aprepitant : A morpholine-based antiemetic, which is or the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; cyclic acetal; morpholines; triazoles | antidepressant; antiemetic; neurokinin-1 receptor antagonist; peripheral nervous system drug; substance P receptor antagonist |
| fosaprepitant fosaprepitant: a pro-drug form of aprepitant. fosaprepitant : A morpholine derivative that is the (1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl ether of (3-{[(2R,3S)-3-(4-fluorophenyl)-2-hydroxymorpholin-4-yl]methyl}-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonic acid. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; cyclic acetal; morpholines; phosphoramide; triazoles | antiemetic; neurokinin-1 receptor antagonist; prodrug |
| rifabutin [no description available] | 3.23 | 1 | 0 | ||
| levomefolate calcium levomefolate calcium: an ingredient in Contraceptives, Oral, Combined. levomefolate calcium : An organic calcium salt of (6S)-5-methyltetrahydrofolic acid. | 3.23 | 1 | 0 | organic calcium salt | antidepressant |
| Condition | Indicated | Relationship Strength | Studies | Trials |
|---|---|---|---|---|
| Age-Related Osteoporosis [description not available] | 0 | 3.37 | 2 | 0 |
| Osteoporosis Reduction of bone mass without alteration in the composition of bone, leading to fractures. Primary osteoporosis can be of two major types: postmenopausal osteoporosis (OSTEOPOROSIS, POSTMENOPAUSAL) and age-related or senile osteoporosis. | 1 | 5.37 | 2 | 0 |
| Bone Loss, Osteoclastic [description not available] | 0 | 2.97 | 1 | 0 |
| Acute Liver Injury, Drug-Induced [description not available] | 0 | 3.04 | 1 | 0 |
| Chemical and Drug Induced Liver Injury A spectrum of clinical liver diseases ranging from mild biochemical abnormalities to ACUTE LIVER FAILURE, caused by drugs, drug metabolites, herbal and dietary supplements and chemicals from the environment. | 0 | 3.04 | 1 | 0 |
| Idiopathic Hypoparathyroidism A condition of low or absent PTH level and HYPOCALCEMIA. It usually occurs as part of an autoimmune syndrome. | 0 | 2.17 | 1 | 0 |
| Hypoparathyroidism A condition caused by a deficiency of PARATHYROID HORMONE (or PTH). It is characterized by HYPOCALCEMIA and hyperphosphatemia. Hypocalcemia leads to TETANY. The acquired form is due to removal or injuries to the PARATHYROID GLANDS. The congenital form is due to mutations of genes, such as TBX1; (see DIGEORGE SYNDROME); CASR encoding CALCIUM-SENSING RECEPTOR; or PTH encoding parathyroid hormone. | 1 | 4.17 | 1 | 0 |