Product Pipeline

As of June 30, 2017

• TAS-102 is a novel combination antitumor agent, consisting of trifluridine (FTD) and a thymidine phosphorylase inhibitor, tipiracil hydrochloride (TPI). FTD induces DNA dysfunction through incorporation into DNA, which can lead to the inhibition of tumor growth. TPI prevents degradation of FTD thereby allowing more sustained inhibitory concentrations of the FTD. TAS-102 is being developed for tumors that are refractory to multiple chemotherapies, including 5-FU refractory colorectal cancer.
• TAS-118 is an antimetabolite in which the components of S-1, i.e. tegafur (FT), gimeracil (CDHP), and oteracil potassium (Oxo), are combined with calcium folinate (LV) into one granular form. The goal of this program is to use the biomodulatory effects of LV on 5-FU to potentially enhance the antitumor effects of S-1.
• TAS-114 is an inhibitor of dUTPase, a gatekeeper protein in pyrimidine-metabolism. It is a First-In-Class molecule and is a fluoropyrimidine modulator with the potential to increase the efficacy of 5-FU-based anticancer drugs. It is being developed in combination with S-1 and capecitabine.
• TAS-115 is a novel, ATP-competitive small molecule inhibitor of c-Met and VEGFR. TAS-115 may prevent tumor growth, metastasis, and invasion through a direct effect on tumor cells and by inhibition of angiogenesis mediated by the HGF and VEGF signaling pathways. Its dual action on tumor cells and vascular endothelial cells may lead to potent antitumor effect.
• TAS-116 is a highly potent oral HSP90 inhibitor with unique tissue distribution properties. TAS-116 has the potential to demonstrate antitumor activity, while being designed to limit certain adverse events by unique tissue distribution.
• TAS-117 is a novel oral allosteric AKT inhibitor. TAS-117 selectively inhibits AKT over other kinases and has potential to inhibit malignant characteristics and chemoresistance of cancer cells induced by activation of AKT.
• TAS-119 is highly selective Aurora A inhibitor (selective over Aurora B & C). TAS-119 has the potential to enhance anti-tumor activity of taxanes through activation of the spindle assembly checkpoint.
• TAS-120 is the first covalent FGFR inhibitor that will be tested in clinic and has the potential to selectively inhibit tumor growth of cancer cells with FGFR abnormalities.
• TAS-121 is oral mutant EGFR (active and acquired resistant harboring T790M ) selective inhibitor.
• TAS3681 is a novel oral AR antagonist/AR down-regulator. It has a unique dual mechanism of action, acting as both an AR antagonist and a down-regulator of AR and AR splice variants.
• TAS4464 is a highly potent and selective NEDD8 activating enzyme inhibitor. TAS4464 has the potential to demonstrate antitumor activity through the accumulation of cullin RING ligase substrates.
• ET-743(trabectedine) is a synthetic derivative of a substance that was originally extracted from the colonial tunicate Ecteinascidia turbinata. It binds to guanine N7 in the minor groove of DNA which can lead to cell death through several pathways.
• Pro-NETU is a water-soluble phosphorylated prodrug of netupitant, a novel selective neurokinin 1 (NK1) receptor antagonist.In-licensed from Helsinn Healthcare SA.
• TAS-205 is an orally active, selective prostaglandin D synthase inhibitor. It is a First-In-Class molecule which inhibits PGD2 synthesis followed by progressive muscular dysfunction.
• TAS-303 is selective norepinephrine reuptake inhibitor.