TABLE 2
CaSR NAMs previously developed for systemic use and tested in humans potentially available for repurposing as inhaled asthma drugs
Development compound table illustrating compound code, development company, chemical structure, molecular weight (MW), crystal structures, developmental stages and number of patients, duration, and references to the clinical trials. NPSP-795, Ronacaleret, JTT-305, and AXT-914 crystal structures were generated as part of the current studies.
| Code | Company | MW (g/mol) | Crystal Structure; PubChem CID | Development Stage | StdInChlKey; NCT; References |
|---|---|---|---|---|---|
| NPSP795/SB-423562 (amino-alcohol) NPSP790/SB-423557 (ester prodrug) NPSP795/SHP635 (amino-alcohol) | NPS/GlaxoSmithKline (osteoporosis); NPS (autosomal dominant hypocalcemia type 1) | 436.5 |  | Phase I (n = 28; i.v.; two study sessions 7 days apart) (n = 50; oral; >two study sessions 7 days apart); phase II (n = 7; 17 days; i.v.) | NJBFJCJKWWIKRD-HSZRJFAPSA-N; https://pubmed.ncbi.nlm.nih.gov/19786130 NCT02204579; https://pubmed.ncbi.nlm.nih.gov/31063613 |
| 9910902 | |||||
| Ronacaleret/SB-751689 (amino-alcohol) | GlaxoSmithKline (osteoporosis) | 447.5 |  | Phase II (n = 569; 12 mo; oral) | FQJISUPNMFRIFZ-HXUWFJFHSA-N; NCT00471237; https://pubmed.ncbi.nlm.nih.gov/23756230 |
| 10345214 | |||||
| JTT-305/MK-5442; Encaleret (amino alcohol) | Japan Tobacco/Merck (osteoporosis) | 514 |  | Phase II (n = 526; 12 mo; oral) | UNFHDRVFEQPUEL-DENIHFKCSA-N; NCT00996801; https://pubmed.ncbi.nlm.nih.gov/26556736 |
| 46917559 | |||||
| AXT914 (quinazolin-2-one) | Novartis (osteoporosis) | 487.4 | Not applicable. | Phase II (n = 105; 4 wk; oral) | NCT00417261; https://pubmed.ncbi.nlm.nih.gov/24769332 |