| Description | Delamanid (OPC-67683) is an anti-tuberculosis agent derived from the nitro-dihydro-imidazooxazole class of compounds that inhibits mycolic acid synthesis of bacterial cell wall. |
| In vitro | In vitro：抑制结核分枝杆菌复合体细胞壁的关键成分——粘酸的合成。[1] 在体外研究中，delamanid 对药物敏感和药物耐药的结核分枝杆菌菌株显示出更强的抗菌活性。[2] Delamanid 不影响利福平、吡嗪酰胺和异烟肼的暴露水平；与delamanid 合用时，乙胺丁醇的AUCτ和Cmax值约高出25%。 |
| In vivo | In vivo：每日两次口服delamanid，剂量为30 mg kg^-1，连续5日，在VL的小鼠模型中实现了无菌治愈。[4] |
| Synonyms | 迪拉马尼, 德拉马尼, OPC-67683 |
| molecular weight | 534.48 |
| Molecular formula | C25H25F3N4O6 |
| CAS | 681492-22-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (93.55 mM) |
| References | 1. Sotgiu G et al. Delamanid (OPC-67683) for treatment of multi-drug-resistant tuberculosis. Expert Rev Anti Infect Ther. 2015 Mar;13(3):305-15. 2. Xavier AS et al. Delamanid: A new armor in combating drug-resistant tuberculosis. J Pharmacol Pharmacother. 2014 Jul;5(3):222-4 3. Mallikaarjun S et al. Delamanid Coadministered with Antiretroviral Drugs or Antituberculosis Drugs Shows No Clinically Relevant Drug-Drug Interactions in Healthy Subjects. Antimicrob Agents Chemother. 2016 Sep 23;60(10):5976-85. 4. Patterson S et al.The anti-tubercular drug delamanid as a potential oral treatment for visceral leishmaniasis. Elife. 2016 May 24;5. |
| Citations | 1. Zhang R, Luo S, Wang N, et al.Epidemiology of Nontuberculous Mycobacteria in Nanjing and MAB_0540 Mutations Associated with Clofazimine Resistance in Mycobacterium abscessus.Infection and Drug Resistance.2023: 2751-2764. 2. Santamaría-Aguirre J, Jacho D, Méndez M A, et al.Solid Lipid Nanoparticles Enhancing the Leishmanicidal Activity of Delamanid.Pharmaceutics.2023, 16(1): 41. |