Page last updated: 2024-12-09

soblidotin

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

Description

soblidotin: a dolastatin 10 derivative; RN refers to (2S-(1(1R*(R*),2S*),2R*(1S*,2S*)))-isomer; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

soblidotin : A tetrapeptide derivative of dolastatin 10. It is an inhibitor of tubulin polymerization which exhibits potent antitumor activity. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID6918315
CHEMBL ID3989512
CHEBI ID32135
SCHEMBL ID4966327
MeSH IDM0275856

Synonyms (34)

Synonym
tzt-1027
soblidotin
yhi-501
nsc-654663
auristatin pe
149606-27-9
n(2)-(n,n-dimethyl-valyl)-n-(2-methoxy-4-(2-(1-methoxy-2-methyl-3-oxo-3-((2-phenylethyl)amino)propyl)-1-pyrrolidinyl)-1-(1-methylpropyl)-4-oxobutyl)-n-methyl-valinamide
l-valinamide, n,n-dimethyl-l-valyl-n-(2-methoxy-4-(2-(1-methoxy-2-methyl-3-oxo-3-((2-phenylethyl)amino)propyl)-1-pyrrolidinyl)-1-(1-methylpropyl)-4-oxobutyl)-n-methyl-, (2s-(1(1r*(r*),2s*),2r*(1s*,2s*)))-
l-valinamide, n,n-dimethyl-l-valyl-n-((1s,2r)-2-methoxy-4-((2s)-2-((1r,2r)-1-methoxy-2-methyl-3-oxo-3-((2-phenylethyl)amino)propyl)-1-pyrrolidinyl)-1-((1s)-1-methylpropyl)-4-oxobutyl)-n-methyl-
n(sup 2)-(n,n-dimethyl-l-valyl)-n(sup 1)-((1s,2r)-2-methoxy-4-((2s)-2-((1r,2r)-1-methoxy-2-methyl-3-oxo-3-((2-phenylethyl)amino)propyl)-1-pyrrolidinyl)-1-((1s)-1-methylpropyl)-4-oxobutyl)-n(sup 1)-methyl-l-valinamide
tzt 1027
unii-dqc51a0wqh
soblidotin [inn]
dqc51a0wqh ,
SCHEMBL4966327
n(sup 2)-(n,n-dimethyl-l-valyl)-n(sup 1)-((1s,2r)-2-methoxy-4-((2s)-2-((1r,2r)-1-methoxy-2-methyl-3-oxo-3-((2-phenylethyl)amino)propyl)-1-pyrrolidinyl)-1-((1s)-1-methylpropyl)-4-oxobutyl)-n1-methyl-l-valinamide
n2-(n,n-dimethyl-l-valyl)-n1-((1s,2r)-2-methoxy-4-((2s)-2-((1r,2r)-1-methoxy-2-methyl-3-oxo-3-((2-phenylethyl)amino)propyl)-1-pyrrolidinyl)-1-((1s)-1-methylpropyl)-4-oxobutyl)-n1-methyl-l-valinamide
soblidotin [jan]
soblidotin [who-dd]
HY-14672
CS-6022
CHEBI:32135
CHEMBL3989512
DB12677
(2s)-2-[[(2s)-2-(dimethylamino)-3-methylbutanoyl]amino]-n-[(3r,4s,5s)-3-methoxy-1-[(2s)-2-[(1r,2r)-1-methoxy-2-methyl-3-oxo-3-(2-phenylethylamino)propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-n,3-dimethylbutanamide
auristatin pe;tzt-1027
NCGC00509861-02
l-valinamide, n,n-dimethyl-l-valyl-n-[(1s,2r)-2-methoxy-4-[(2s)-2-[(1r,2r)-1-methoxy-2-methyl-3-oxo-3-[(2-phenylethyl)amino]propyl]-1-pyrrolidinyl]-1-[(1s)-1-methylpropyl]-4-oxobutyl]-n-methyl-
Q27276538
MS-31167
ZFA60627
EX-A5590
DTXSID901031350
AKOS040741182

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" The pharmacokinetic evaluation revealed a T(1/2) of approximately 7 h and linear kinetics."( Phase I and pharmacokinetic study of TZT-1027, a novel synthetic dolastatin 10 derivative, administered as a 1-hour intravenous infusion every 3 weeks in patients with advanced refractory cancer.
Atsumi, R; Beutel, G; Bolte, O; Cheverton, P; Ganser, A; Hofmann, M; Jenner, A; Oguma, T; Otto, D; Satomi, M; Schöffski, P; Thate, B; Wanders, J, 2004
)
0.32
" For pharmacokinetic analysis, plasma sampling was done during the first and second course and assayed using a validated high-performance liquid chromatographic assay with mass spectrometric detection."( Phase I and pharmacokinetic study of the dolastatin 10 analogue TZT-1027, given on days 1 and 8 of a 3-week cycle in patients with advanced solid tumors.
Boot, I; de Jonge, MJ; Lems, A; Planting, AS; Satomi, M; van der Gaast, A; van Doorn, L; Verweij, J; Wanders, J, 2005
)
0.33

Compound-Compound Interactions

ExcerptReferenceRelevance
" In the present study we investigated the effect of bryostatin 1 alone and in combination with novel anti-tubulin agents (dolastatin 10 and auristatin PE) and the chemotherapeutic vincristine on the inhibitor of apoptosis protein cIAP-1."( Modulation of cIAP-1 by novel antitubulin agents when combined with bryostatin 1 results in increased apoptosis in the human early pre-B acute lymphoblastic leukemia cell line Reh.
Al-Katib, AM; Mohammad, RM; Nabha, SM; Pettit, GR; Wall, NR, 1999
)
0.3

Dosage Studied

ExcerptRelevanceReference
" No correlation between body surface area and absolute CL of TZT-1027 was established, vindicating that a flat dosing regimen might be used in the future."( Phase I and pharmacokinetic study of the dolastatin 10 analogue TZT-1027, given on days 1 and 8 of a 3-week cycle in patients with advanced solid tumors.
Boot, I; de Jonge, MJ; Lems, A; Planting, AS; Satomi, M; van der Gaast, A; van Doorn, L; Verweij, J; Wanders, J, 2005
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
microtubule-destabilising agentAny substance that interacts with tubulin to inhibit polymerisation of microtubules.
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
apoptosis inducerAny substance that induces the process of apoptosis (programmed cell death) in multi-celled organisms.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
tetrapeptideAny molecule that contains four amino-acid residues connected by peptide linkages.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (1)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency10.00000.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (1)

Assay IDTitleYearJournalArticle
AID1896114Cytotoxicity against human Panel NCI-60 (60 carcinoma cell lines) assessed as cell growth inhibition2022Journal of natural products, 03-25, Volume: 85, Issue:3
Discovery and Development of Dolastatin 10-Derived Antibody Drug Conjugate Anticancer Drugs.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (57)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's11 (19.30)18.2507
2000's40 (70.18)29.6817
2010's5 (8.77)24.3611
2020's1 (1.75)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials8 (12.50%)5.53%
Reviews6 (9.38%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other50 (78.13%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase II Study of Intravenous TZT-1027, Administered Weekly Times Two, Every Three Weeks, to Patients With Advanced or Metastatic Soft Tissue Sarcomas (STS) With Prior Exposure to Anthracycline-Based Chemotherapy [NCT00064220]Phase 20 participants Interventional2003-04-30Completed
A Phase II Study Of Intravenous TZT-1027, Administered Weekly Times Two, Every Three Weeks, To Patients With Progressive Locally Advanced Or Metastatic Non-Small Cell Lung Cancer (NSCLC) Following Treatment With Platinum-Based Chemotherapy [NCT00061854]Phase 20 participants Interventional2003-04-30Completed
Phase I Study of Soblidotin and Gemcitabine in Patients With Locally Advanced or Metastatic Solid Tumors [NCT00072228]Phase 10 participants InterventionalWithdrawn
[information is prepared from clinicaltrials.gov, extracted Sep-2024]