This is a Phase 1 open-label study of SN2310 Injectable Emulsion in patients with advanced solid malignancies. The study is designed to determine the maximum tolerated dose and dose-limiting toxicity of SN2310 Injectable Emulsion, and to characterize the pharmacokinetics of SN2310 and SN-38 following intravenous administration of SN2310 Injectable Emulsion. Additionally, evaluation of side effects as a function of dose, and observation of any anti-tumor effects of SN2310 Injectable Emulsion will be made.

Start Date01 Sep 2006

Sponsor / Collaborator

Achieve Life Sciences, Inc.

100 Clinical Results associated with Tenifatecan

100 Translational Medicine associated with Tenifatecan

100 Patents (Medical) associated with Tenifatecan

Literatures (Medical) associated with Tenifatecan

20 Apr 2020·Pharmaceutical Development and TechnologyQ4 · MEDICINE

Development and evaluation of paclitaxel nanoemulsion for cancer therapy

Q4 · MEDICINE

Article

Author: Kamal, Mohammad M. ; Nazzal, Sami ; Pallerla, Sandeep ; Abu Fayyad, Ahmed ; Darwish, Rana ; Shakhwar, Sara

Tocosol™ is a tocopherol-based paclitaxel (PTX) nanoemulsion consisting of α-tocopherol (α-T) isomer of vitamin E as a solubilizer and vitamin E TPGS as the primary emulsifier. Despite its positive attributes in early clinical studies, it failed the pivotal phase III clinical trials. The long-term goal of this work was to reformulate Tocosol™. In this study, Tocosol™ formulation was optimized by replacing the α-T isomer with the more pharmacological active isomer γ-tocotrienol (γ-T₃), and the surfactant vitamin E TPGS was replaced with in-house designed PEGylated γ-T₃ surfactant. The reformulated paclitaxel γ-T₃/PEGylated γ-T₃ -based nanoemulsion was significantly more active against pancreatic tumor cell lines than α-T/Vitamin E TPGS based formulation (IC₅₀ = 0.5 μM and 1.1 μM, respectively). Furthermore, the reformulated product showed an average size of 220 ± 6 nm with surface charge equal to -42 ± 2 mV. The optimized product was physically and chemically stable over 6 months per ICH storage condition guidelines.

01 Jan 2018·International Journal of PharmaceuticsQ2 · MEDICINE

Development and in-vitro characterization of nanoemulsions loaded with paclitaxel/γ-tocotrienol lipid conjugates

Q2 · MEDICINE

Article

Author: Abu-Fayyad, Ahmed ; Cody, Robert ; Dragoi, Ana-Maria ; Cardelli, James ; Kamal, Mohammad M ; Carroll, Jennifer L ; Nazzal, Sami

Vitamin E TPGS is a tocopherol (α-T) based nonionic surfactant that was used in the formulation of the Tocosol™ paclitaxel nanoemulsion, which was withdrawn from phase III clinical trials. Unlike tocopherols, however, the tocotrienol (T₃) isomers of vitamin E were found to have innate anticancer activity and were shown to potentiate the antitumor activity of paclitaxel. The primary objective of the present study was therefore to develop a paclitaxel nanoemulsions by substituting α-T oil core of Tocosol™ with γ-T₃ in, and vitamin E TPGS with PEGylated γ-T₃ as the shell, and test the nanoemulsions against Bx-PC-3 and PANC-1 pancreatic tumor cells. A secondary objective was to test the activity of paclitaxel when directly conjugated with the γ-T₃ isomer of vitamin E. The synthesis of the conjugates was confirmed by NMR and mass spectroscopy. Developed nanoemulsions were loaded with free or lipid conjugated paclitaxel. Nanoemulsions droplets were <300 nm with fastest release observed with formulations loaded with free paclitaxel when γ-T₃ was used as the core. Substituting α-T with γ-T₃ was also found to potentiate the anticancer activity of the nanoemulsions. Although marginal increase in activity was observed when nanoemulsions were loaded with free paclitaxel, a significant increase in activity was observed when lipid conjugates were used. The results from this study suggest that the developed paclitaxel nanoemulsions with either γ-T₃, PEGylated γ-T₃, or paclitaxel lipid conjugates may represent a more promising option for paclitaxel delivery in cancer chemotherapy.

01 Oct 2011·Journal of Pharmaceutical SciencesQ3 · MEDICINE

Pharmacokinetics of SN2310, an Injectable Emulsion that Incorporates a New Derivative of SN-38 in Patients with Advanced solid Tumors

Q3 · MEDICINE

Article

Author: Suzanne Jones ; Leng Pheng ; Howard A. Burris ; Kirsten Anderson ; My My Trinh ; David Porubek ; Serina Warner ; Jean-Francois Marier

SN2310 is an injectable emulsion composed of vitamin E, a succinate derivative, as well as 7-ethyl-10-hydroxycamptothecin (SN-38), the active metabolite of irinotecan. Single intravenous doses of 15, 20, 25, and 30 mg/m(2) of SN2310 emulsion were administered in a total of 26 patients with advanced solid malignancies. Serial blood samples were collected and concentrations of SN2310, SN-38, and SN-38 glucuronide were assayed. Mean systemic clearance of SN2310 ranged between 1.91 and 2.02 L/h/m(2) . Peak concentrations of SN-38 were observed at the end of infusion, suggesting a fast metabolic conversion of SN2310 to its active form, SN-38. Mean t1/2 values of SN-38 across the 20-30 mg/m(2) dose levels (131-199 h) were 33-55-fold longer than those observed for SN2310. The systemic exposure of SN-38 increased in a proportional manner over the dose range studied. SN2310 emulsion displayed an improved safety profile as compared with irinotecan. The most significant safety risk was neutropenia. Considering the rapid formation of SN-38, the proportional increase in exposure levels, and its longer elimination half-life, less frequent dosing of SN2310 emulsion may be considered for the treatment of patients with advanced solid malignancies.

100 Deals associated with Tenifatecan

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R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Advanced Malignant Solid Neoplasm	Phase 1	US	Achieve Life Sciences, Inc.	01 Sep 2006
Breast Cancer	Phase 1	US	Achieve Life Sciences, Inc.	01 Sep 2006
Colorectal Cancer	Phase 1	US	Achieve Life Sciences, Inc.	01 Sep 2006
Lung Cancer	Phase 1	US	Achieve Life Sciences, Inc.	01 Sep 2006
Pancreatic Cancer	Phase 1	US	Achieve Life Sciences, Inc.	01 Sep 2006
Pelvic Neoplasms	Phase 1	US	Achieve Life Sciences, Inc.	01 Sep 2006

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