MedKoo product information:

 AI-850

Description of AI-850: AI-850 is Acusphere's patented formulation of paclitaxel, the active ingredient in the cancer drugs, Taxol® (Bristol-Myers Squibb Company) and Abraxane® (Celgene Corporation). AI-850, is a cremaphor-free formulation of paclitaxel. Cremaphor is an oil used in the Taxol formulation to dissolve paclitaxel. Because of the Cremaphor, Taxol has many side effects that require premedication and it must be infused slowly over a three hour period. AI-850 eliminates the side effects associated with Cremaphor and can be injected as a bolus. The worldwide rights to AI-850 were licensed to Cephalon in 2008. (source: http://www.acusphere.com/pipeline/pipe_ai850.html).

Current developer:     Acusphere Inc., Cephalon.

AI-850 is Acusphere's patented formulation of paclitaxel, the active ingredient in the cancer drugs, Taxol® (Bristol-Myers Squibb Company) and Abraxane® (Celgene Corporation). AI-850, is a cremaphor-free formulation of paclitaxel. Cremaphor is an oil used in the Taxol formulation to dissolve paclitaxel. Because of the Cremaphor, Taxol has many side effects that require premedication and it must be infused slowly over a three hour period. AI-850 eliminates the side effects associated with Cremaphor and can be injected as a bolus. The worldwide rights to AI-850 were licensed to Cephalon in 2008. (source: http://www.acusphere.com/pipeline/pipe_ai850.html).

Phase I results: Twenty-two patients received 56 courses of AI-850 at five dose cohorts ranging from 36 to 250 mg/m(2). Grade 4 neutropenia, either exceeding 5 days or complicated by fever, was dose limiting in two of six patients at 250 mg/m(2) AI-850. Three patients experienced grade 2 to 4 infusion-related adverse reactions. Toxicities, including fatigue, alopecia, nausea and vomiting, neuropathy, anorexia, and myalgia, were mild to moderate, reversible, and not dose related. Pharmacokinetics of free and total paclitaxel showed biexponential plasma decay and dose proportionality for maximum plasma paclitaxel concentration and area under the concentration versus time curve. Antitumor activity was documented in two patients with endometrial and tongue carcinomas. CONCLUSIONS: The administration of AI-850 as a brief infusion once every 3 weeks was feasible at doses up to 205 mg/m(2). The potential of AI-850 as an alternative to other approved paclitaxel formulations requires further clinical evaluation. (source: Clin Cancer Res. 2007 Jun 1;13(11):3293-301.).

 1: Mita AC, Olszanski AJ, Walovitch RC, Perez RP, MacKay K, Tuck DP, Simmons C, Hammond S, Mita MM, Beeram M, Stone AJ, Rowinsky EK, Lewis LD. Phase I and pharmacokinetic study of AI-850, a novel microparticle hydrophobic drug delivery  system for paclitaxel. Clin Cancer Res. 2007 Jun 1;13(11):3293-301. PubMed PMID:  17545535.

2: Straub JA, Chickering DE, Lovely JC, Zhang H, Shah B, Waud WR, Bernstein H. Intravenous hydrophobic drug delivery: a porous particle formulation of paclitaxel (AI-850). Pharm Res. 2005 Mar;22(3):347-55. PubMed PMID: 15835739.