title: CD101, a novel echinocandin with exceptional stability properties and enhanced aqueous solubility.
abstract: The echinocandins are an important class of antifungal agents. However, instability and, in some cases, lack of solubility have restricted their use to situations in which daily infusions are acceptable. CD101 is a novel echinocandin in development for topical and weekly i.v. administration that exhibits prolonged stability in plasma and aqueous solutions up to 40 °C. After incubation for 44 h in rat, dog, monkey and human plasma at 37 °C, the percent of CD101 remaining (91%, 79%, 94% and 93%, respectively) was consistently greater than that of anidulafungin (7%, 15%, 14% and 7%, respectively). Similarly, after incubation in phosphate-buffered saline at 37 °C, the CD101 remaining (96%) was greater than that of anidulafungin (42%). CD101 exhibited <2% degradation after long-term storage at 40 °C as a lyophilized powder (9 months) and at room temperature in 5% dextrose (15 months), 0.9% saline (12 months) and sterile water (18 months). Degradation was <7% at 40 °C in acetate and lactate buffers (6 to 9 months at pH 4.5-5.5). The chemical stability and solubility of CD101 contribute to dosing, pharmacokinetic, formulation and safety advantages over other echinocandins and should expand utility beyond daily i.v.
authors: Cidara Therapeutics, San Diego, CA, USA.|Seachaid Pharmaceuticals, Durham, NC, USA.
authors: B Radha
authors: BR
authors: Krishnan
authors: Cidara Therapeutics, San Diego, CA, USA.|Seachaid Pharmaceuticals, Durham, NC, USA.
authors: Kenneth D
authors: KD
authors: James
authors: Seachaid Pharmaceuticals, Durham, NC, USA.
authors: Karen
authors: K
authors: Polowy
authors: Seachaid Pharmaceuticals, Durham, NC, USA.
authors: B J
authors: BJ
authors: Bryant
authors: Seachaid Pharmaceuticals, Durham, NC, USA.
authors: Anu
authors: A
authors: Vaidya
authors: Seachaid Pharmaceuticals, Durham, NC, USA.
authors: Steve
authors: S
authors: Smith
authors: Seachaid Pharmaceuticals, Durham, NC, USA.
authors: Christopher P
authors: CP
authors: Laudeman
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D002021:Buffers; D004355:Drug Stability; D054714:Echinocandins / Q000737:chemistry / Q000494:pharmacology*; D006863:Hydrogen-Ion Concentration; D015394:Molecular Structure; D010710:Phosphates; D010949:Plasma / Q000737:chemistry*; D011208:Powders; D012995:Solubility; D012996:Solutions
chemical_list: D000935:Antifungal Agents; D002021:Buffers; D054714:Echinocandins; D010710:Phosphates; D011208:Powders; D012996:Solutions