st 1968

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

namitecan: has antineoplastic activity; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	10950142
CHEMBL ID	419186
SCHEMBL ID	5065702
SCHEMBL ID	24685130
MeSH ID	M0524553

Synonyms (24)

Synonym
CHEMBL419186
st-1968 ,
(4s)-11-((e)-((2-aminoethoxy)imino)methyl)-4-ethyl-4-hydroxy-1,12-dihydro-14h-pyrano(3',4':6,7)indolizino(1,2-b)quinoline-3,14(4h)-dione
372105-27-6
st 1968
x34z8n66t3 ,
namitecan
unii-x34z8n66t3
namitecan [inn]
st1968
namitecan [who-dd]
SCHEMBL5065702
DTXSID90190707
HY-14821
CS-6708
DB12124
(19s)-10-[(e)-2-aminoethoxyiminomethyl]-19-ethyl-19-hydroxy-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4,6,8,10,15(20)-heptaene-14,18-dione
A936712
(4s)-11-{(e)-[(2-aminoethoxy)imino]methyl}-4-ethyl-4-hydroxy-1h-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4h,12h)-dione
MS-27779
SCHEMBL24685130
292621-05-7
(s)-4-ethyl-4-hydroxy-3,14-dioxo-3,4,12,14-tetrahydro-1h-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-11-carbaldehyde o-(2-aminoethyl) oxime
AKOS040742269

Research Excerpts

Pharmacokinetics

Excerpt	Reference	Relevance
" This study was initiated to build an integrated pharmacokinetic (PK) and pharmacodynamic (PD) population model of namitecan to guide future clinical development."	( Integrative population pharmacokinetic and pharmacodynamic dose finding approach of the new camptothecin compound namitecan (ST1968). Barbieri, P; Cresta, S; Delmonte, A; Fasolo, A; Gallerani, E; Gianni, L; Hess, D; Joerger, M; Pace, S; Sessa, C, 2015)	0.42
"15 l h(-1), with a long terminal half-life of 48 h."	( Integrative population pharmacokinetic and pharmacodynamic dose finding approach of the new camptothecin compound namitecan (ST1968). Barbieri, P; Cresta, S; Delmonte, A; Fasolo, A; Gallerani, E; Gianni, L; Hess, D; Joerger, M; Pace, S; Sessa, C, 2015)	0.42

Dosage Studied

Excerpt	Relevance	Reference
" Data simulations were used to interrogate various dosing regimens and give dosing recommendations."	( Integrative population pharmacokinetic and pharmacodynamic dose finding approach of the new camptothecin compound namitecan (ST1968). Barbieri, P; Cresta, S; Delmonte, A; Fasolo, A; Gallerani, E; Gianni, L; Hess, D; Joerger, M; Pace, S; Sessa, C, 2015)	0.42
" A distinct relationship was found between drug exposure and haematological toxicity, supporting flat-dosing once every 3 weeks as the most adequate dosing regimen."	( Integrative population pharmacokinetic and pharmacodynamic dose finding approach of the new camptothecin compound namitecan (ST1968). Barbieri, P; Cresta, S; Delmonte, A; Fasolo, A; Gallerani, E; Gianni, L; Hess, D; Joerger, M; Pace, S; Sessa, C, 2015)	0.42
" Due to frequent skipping of day 8 dosing for cytopenias, the study was expanded to test namitecan dosing on day 1 every 21 days (D1-Q21) at a starting dose of 17."	( Phase-I dose finding and pharmacokinetic study of the novel hydrophilic camptothecin ST-1968 (namitecan) in patients with solid tumors. Barbieri, P; Delmonte, A; Gallerani, E; Hess, D; Joerger, M; Pace, S; Sessa, C, 2015)	0.42
"5, 20 mg dosing cohorts), 29 patients into the D1-21D group (17."	( Phase-I dose finding and pharmacokinetic study of the novel hydrophilic camptothecin ST-1968 (namitecan) in patients with solid tumors. Barbieri, P; Delmonte, A; Gallerani, E; Hess, D; Joerger, M; Pace, S; Sessa, C, 2015)	0.42

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (2)

Assay ID	Title	Year	Journal	Article
AID332046	Cytotoxicity against human H460 cells	2008	Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9	Synthesis and cytotoxic activity of new 9-substituted camptothecins.
AID146690	Cytotoxicity against human non-small-cell lung carcinoma cell line H460 (NSCLC-H460)	2001	Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20	Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	5 (35.71)	29.6817
2010's	9 (64.29)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.07

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	20.07 (24.57)
Research Supply Index	2.83 (2.92)
Research Growth Index	4.44 (4.65)
Search Engine Demand Index	19.78 (26.88)
Search Engine Supply Index	3.00 (0.95)

This Compound (20.07)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	2 (14.29%)	5.53%
Reviews	1 (7.14%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	11 (78.57%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
pyrroles 1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.	2.07	1	0	pyrrole; secondary amine
camptothecin NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source	7.05	13	2	delta-lactone; pyranoindolizinoquinoline; quinoline alkaloid; tertiary alcohol	antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor; genotoxin; plant metabolite
topotecan Topotecan: An antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA TOPOISOMERASES, TYPE I.. topotecan : A pyranoindolizinoquinoline used as an antineoplastic agent. It is a derivative of camptothecin and works by binding to the topoisomerase I-DNA complex and preventing religation of these 328 single strand breaks.	2.95	4	0	pyranoindolizinoquinoline	antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor
irinotecan [no description available]	2.74	3	0	carbamate ester; delta-lactone; N-acylpiperidine; pyranoindolizinoquinoline; ring assembly; tertiary alcohol; tertiary amino compound	antineoplastic agent; apoptosis inducer; EC 5.99.1.2 (DNA topoisomerase) inhibitor; prodrug
arginyl-glycyl-aspartic acid arginyl-glycyl-aspartic acid: amino acid sequence of basic unit of widespread cellular recognition system	2.05	1	0	oligopeptide
sn 38 SN-38 : A member of the class of pyranoindolizinoquinolines that is (4S)-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14-dione bearing two additional ethyl substituents at positions 4 and 11 as well as two additional hydroxy substituents at positions 4 and 9. It is the active metabolite of irinotecan and is ~1000 times more active than irinotecan itself.	2.42	2	0	delta-lactone; phenols; pyranoindolizinoquinoline; tertiary alcohol	antineoplastic agent; apoptosis inducer; drug metabolite; EC 5.99.1.2 (DNA topoisomerase) inhibitor
su 11248 [no description available]	2.07	1	0	monocarboxylic acid amide; pyrroles	angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; immunomodulator; neuroprotective agent; vascular endothelial growth factor receptor antagonist
st 1481 ST 1481: structure in first source	2.42	2	0

Condition	Relationship Strength	Studies	Trials
Carcinoma, Epidermoid [description not available]	2.97	4	0
Carcinoma, Squamous Cell A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)	2.97	4	0
Benign Neoplasms [description not available]	3.5	1	1
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	3.5	1	1
Cancer of Ovary [description not available]	2.45	2	0
Ovarian Neoplasms Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.	2.45	2	0
Sarcoma, Epithelioid [description not available]	2.07	1	0
Rhabdomyosarcoma A malignant solid tumor arising from mesenchymal tissues which normally differentiate to form striated muscle. It can occur in a wide variety of sites. It is divided into four distinct types: pleomorphic, predominantly in male adults; alveolar (RHABDOMYOSARCOMA, ALVEOLAR), mainly in adolescents and young adults; embryonal (RHABDOMYOSARCOMA, EMBRYONAL), predominantly in infants and children; and botryoidal, also in young children. It is one of the most frequently occurring soft tissue sarcomas and the most common in children under 15. (From Dorland, 27th ed; Holland et al., Cancer Medicine, 3d ed, p2186; DeVita Jr et al., Cancer: Principles & Practice of Oncology, 3d ed, pp1647-9)	2.07	1	0
Sarcoma A connective tissue neoplasm formed by proliferation of mesodermal cells; it is usually highly malignant.	2.07	1	0
Cerebral Primitive Neuroectodermal Tumor [description not available]	2.07	1	0
Benign Cerebellar Neoplasms [description not available]	2.07	1	0
Arachnoidal Cerebellar Sarcoma, Circumscribed [description not available]	2.07	1	0
Medulloblastoma A malignant neoplasm that may be classified either as a glioma or as a primitive neuroectodermal tumor of childhood (see NEUROECTODERMAL TUMOR, PRIMITIVE). The tumor occurs most frequently in the first decade of life with the most typical location being the cerebellar vermis. Histologic features include a high degree of cellularity, frequent mitotic figures, and a tendency for the cells to organize into sheets or form rosettes. Medulloblastoma have a high propensity to spread throughout the craniospinal intradural axis. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2060-1)	2.07	1	0
Neuroblastoma A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51)	2.07	1	0
Neuroectodermal Tumors, Primitive A group of malignant tumors of the nervous system that feature primitive cells with elements of neuronal and/or glial differentiation. Use of this term is limited by some authors to central nervous system tumors and others include neoplasms of similar origin which arise extracranially (i.e., NEUROECTODERMAL TUMORS, PRIMITIVE, PERIPHERAL). This term is also occasionally used as a synonym for MEDULLOBLASTOMA. In general, these tumors arise in the first decade of life and tend to be highly malignant. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, p2059)	2.07	1	0
Experimental Neoplasms [description not available]	2.03	1	0
Cancer of Prostate [description not available]	2.04	1	0
Prostatic Neoplasms Tumors or cancer of the PROSTATE.	2.04	1	0

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