U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Status:
Investigational
Source:
NCT01423851: Phase 1/Phase 2 Interventional Completed Primary Myelofibrosis
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


NS-018 is a potent inhibitor of Janus kinase 2 (JAK2) enzyme activity and Src-family kinases. It was developed as an oral therapy for the treatment of myelofibrosis. Overall NS-018 has been used in trials studying the treatment of primary myelofibrosis, post-polycythemia vera myelofibrosis, and post-essential thrombocythemia. NS-018 is a highly active JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). NS-018 also inhibits Src-family kinases, especially SRC and FYN, and weakly inhibits ABL and FLT3 with 45- and 90-fold selectivity for JAK2, respectively. NS-018 shows potent inhibitory activity against cell lines JAK2V617F or MPLW515L mutations or the TEL-JAK2 fusion gene.
Status:
Investigational
Source:
NCT00331721: Phase 2 Interventional Terminated Stroke
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Enecadin (NS 7 or ZK 228326) is a voltage-dependent sodium and calcium channel blocker. Enecadin is a neuroprotective agent demonstrated efficacy in animal models of ischemic injury of brain, spinal cord and retina. Enecadin was undergoing phase II development in stroke with PAION in Germany. Enecadin development has been discontinued.
Status:
US Previously Marketed
Source:
Sycotrol by Reed & Carnrick
(1959)
Source URL:
First approved in 1959
Source:
Sycotrol by Reed & Carnrick
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Piperilate is an antispasmodic, antimuscarinic agent. It is a muscarinic cholinergic receptor antagonist.
Status:
Investigational
Source:
NCT01423851: Phase 1/Phase 2 Interventional Completed Primary Myelofibrosis
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


NS-018 is a potent inhibitor of Janus kinase 2 (JAK2) enzyme activity and Src-family kinases. It was developed as an oral therapy for the treatment of myelofibrosis. Overall NS-018 has been used in trials studying the treatment of primary myelofibrosis, post-polycythemia vera myelofibrosis, and post-essential thrombocythemia. NS-018 is a highly active JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). NS-018 also inhibits Src-family kinases, especially SRC and FYN, and weakly inhibits ABL and FLT3 with 45- and 90-fold selectivity for JAK2, respectively. NS-018 shows potent inhibitory activity against cell lines JAK2V617F or MPLW515L mutations or the TEL-JAK2 fusion gene.
Status:
Investigational
Source:
NCT00331721: Phase 2 Interventional Terminated Stroke
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Enecadin (NS 7 or ZK 228326) is a voltage-dependent sodium and calcium channel blocker. Enecadin is a neuroprotective agent demonstrated efficacy in animal models of ischemic injury of brain, spinal cord and retina. Enecadin was undergoing phase II development in stroke with PAION in Germany. Enecadin development has been discontinued.
Status:
US Previously Marketed
Source:
Sycotrol by Reed & Carnrick
(1959)
Source URL:
First approved in 1959
Source:
Sycotrol by Reed & Carnrick
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Piperilate is an antispasmodic, antimuscarinic agent. It is a muscarinic cholinergic receptor antagonist.