Page last updated: 2024-12-06

thymopentin

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

Description

Thymopentin: Synthetic pentapeptide corresponding to the amino acids 32-36 of thymopoietin and exhibiting the full biological activity of the natural hormone. It is an immunomodulator which has been studied for possible use in the treatment of rheumatoid arthritis, AIDS, and other primary immunodeficiencies. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID451417
CHEMBL ID156025
CHEBI ID135870
SCHEMBL ID44001
MeSH IDM0024918

Synonyms (51)

Synonym
sintomodulina
MLS000069768
smr000058921
orf-15244
timunox
SMP1_000105
D06117
thymopentin (usan/inn)
thymopentin
arg-lys-asp-val-tyr
arg-lys-asp-val-tyr; rkdvy
rkdvy
tp-5
CHEBI:135870
hg-thymopentin
thymopoetin 32-36-pentapeptide
immunox
oristar thymopentin
CHEMBL156025
nsc-760116
pentapeptide-1
sh-pentapeptide-1
HMS3264A15
dtxcid7026609
cas-69558-55-0
tox21_112420
dtxsid9046609 ,
pharmakon1600-01506200
nsc760116
HMS2231E14
AKOS015994638
SCHEMBL44001
HS-2029
mfcd00214200
thymopentin acetate (tp-5)
thymopentin, >=97% (hplc)
(6s,9s,12s,15s,18s)-1,6-diamino-9-(4-aminobutyl)-12-(carboxymethyl)-18-(4-hydroxybenzyl)-1-imino-15-isopropyl-7,10,13,16-tetraoxo-2,8,11,14,17-pentaazanonadecan-19-oic acid
HY-N7122
CS-0020412
2,8,11,14,17-pentaazanonadecan-19-oic acid
12-(carboxymethyl)-18-(4-hydroxybenzyl)-1-
thymopentin,(s)
(6s,9s,12s,15s,18s)-1,6-diamino-9-(4-aminobutyl)-
imino-15-isopropyl-7,10,13,16-tetraoxo-
Q7799637
BRD-K52097716-001-01-1
l-tyrosine, l-arginyl-l-lysyl-l-a-aspartyl-l-valyl-
CCG-270365
S3668
(6s,9s,12s,15s,18s)-1,6-diamino-9-(4-aminobutyl)-12-(carboxymethyl)-18-(4-hydroxybenzyl)-1-imino-15-isopropyl-7,10,13,16-tetraoxo-2,8,11,14,17-pentaazanonadecan-19-oicacid
tp-5 acetate

Research Excerpts

Toxicity

The safety data collected from 196 patients treated with thymopentin during the clinical development of this compound in Europe are reviewed and compared with the incidence of adverse drug reactions experienced when using a commercial nonsteroid anti-inflammatory drug. The overall conclusion in that thymopsin is a safe compound.

ExcerptReferenceRelevance
" The overall conclusion in that thymopentin is a safe compound."( Thymopentin: safety overview.
Friedmann, N, 1985
)
0.27
"The safety data collected from 196 patients treated with thymopentin during the clinical development of this compound in Europe are reviewed and compared with the incidence of adverse drug reactions experienced when using a commercial nonsteroid anti-inflammatory drug."( Safety of thymopentin. Data from European clinical studies.
Stocker, H; Weiss, P, 1985
)
0.27
" The treatment groups did not differ significantly with respect to changes in CD4 counts or p24 antigen levels or with respect to clinical adverse experiences or laboratory abnormalities."( Safety and efficacy of thymopentin in zidovudine (AZT)-treated asymptomatic HIV-infected subjects with 200-500 CD4 cells/mm3: a double-blind placebo-controlled trial.
Beall, G; Blick, G; Calabrese, LH; Conant, MA; Fisher, A; Galpin, JE; Goldstein, G; Grossman, HA; Hirsch, RL; Stampone, P, 1995
)
0.29
" No thymopentin-related adverse events occurred."( A double-blind, placebo-controlled clinical trial to evaluate the safety and efficacy of thymopentin as an adjunctive treatment in atopic dermatitis.
Cohen, DE; Jondreau, L; Kenny, C; Shupack, JL; Soter, NA; Stiller, MJ, 1994
)
0.29
"Thymopentin may be a safe effective adjunct to therapy in patients with severe atopic dermatitis."( A double-blind, placebo-controlled clinical trial to evaluate the safety and efficacy of thymopentin as an adjunctive treatment in atopic dermatitis.
Cohen, DE; Jondreau, L; Kenny, C; Shupack, JL; Soter, NA; Stiller, MJ, 1994
)
0.29

Pharmacokinetics

Thymopentin is widely used in the clinic and represents a promising target for drug design. bioanalytical and pharmacokinetic data are limited due to its enzymatic instability.

ExcerptReferenceRelevance
" The pharmacokinetics following intramuscular injection of the multivesicular liposome of thymopentin labeled with fluorescein isothiocyanate in rats showed that the peak concentration of thymopentin was lower and elimination of it was slower significantly than that of thymopentin labeled with fluorescein isothiocyanate solution in the same dose."( [Preparation of sustained release multivesicular liposome for thymopentin and preliminary study on its pharmacokinetics in rats].
Jiao, YH; Mu, HJ; Sun, KX; Wang, T; Yao, DG; Yuan, ZZ, 2008
)
0.35
" Pharmacodynamic studies were carried out in immunosuppressed rats using the ratio of CD4(+)/CD8(+) cells, determined by flow cytometry, as an index of immunity."( Preparation, characterization and in vivo pharmacodynamic evaluation of thymopentin loaded poly(lactide acid)/poly(lactide-co-glycolide acid) implants.
Jin, L; Liu, Y; Lu, W; Wei, G; Xu, L, 2010
)
0.36
" In addition, FITC-TP5-loaded MVLs was prepared for pharmacokinetic studies that after subcutaneous administration, the fluorescence signal lasted for about 5 days in plasma demonstrating that the rate of drug release from MVLs was very slow."( Multivesicular liposomes for the sustained release of thymopentin: stability, pharmacokinetics and pharmacodynamics.
Gong, T; Huang, Y; Peng, Q; Sun, X; Zhang, Z; Zuo, J, 2012
)
0.38
" Additionally, VPGs loaded with 5-hydroxy-fluorescein-thymopetin (5-FAM-TP5-VPGs) were developed and their pharmacokinetic profile was investigated in vivo."( Vesicular phospholipid gels using low concentrations of phospholipids for the sustained release of thymopentin: pharmacokinetics and pharmacodynamics.
Chen, L; Gong, T; Li, W; Sun, X; Zhang, Y; Zhang, Z; Zhong, Y, 2013
)
0.39
" Thymopentin is widely used in the clinic and represents a promising target for drug design but bioanalytical and pharmacokinetic data are limited due to its enzymatic instability."( Determination of thymopentin in beagle dog blood by liquid chromatography with tandem mass spectrometry and its application to a preclinical pharmacokinetic study.
Cai, L; Fang, C; Fawcett, JP; Gao, Y; Gu, J; Shi, M; Sun, H; Sun, Y; Wang, C; Yang, Y; Zhou, X, 2015
)
0.42

Compound-Compound Interactions

Lamivudine in combination with thymopentin can exert great and lasting effects on HBV and is effective in normalization of ALT.

ExcerptReferenceRelevance
"Lamivudine in combination with thymopentin can exert great and lasting effects on HBV and is effective in normalization of ALT."( [Therapeutic effects of Lamivudine in combination with Thymopentin on chronic hepatitis B].
Shi, W; Tang, S; Zhang, W, 2002
)
0.31
"To evaluate the efficacy and safety of high doses of thymopentin (10 mg/d) combined with transartery chemoembolization for primary liver cancer."( [Study on the efficacy and safety of high dose thymopentin combined with trans-artery chemoembolization for primary liver cancer].
Li, T; Li, ZW; Wen, HC, 2007
)
0.34
"Transartery chemoembolization combined with high dose of thymopentin in the treatment for primary liver cancer is effective and safe, and can significantly improve the immune function and the chemotherapy tolerance."( [Study on the efficacy and safety of high dose thymopentin combined with trans-artery chemoembolization for primary liver cancer].
Li, T; Li, ZW; Wen, HC, 2007
)
0.34

Bioavailability

ExcerptReferenceRelevance
"Peptides, although high efficacy and specificity in their physiological function, usually have low therapeutical activities due to their poor bioavailability when administrated orally."( Research on thymopentin loaded oral N-trimethyl chitosan nanoparticles.
He, Q; Song, QG; Yuan, XJ; Zhang, ZR, 2006
)
0.33
"Thymopentin (Tp5) was loaded in poly-butylcyanoacrylate (PBCA) nanoparticles (NP) in order to enhance the oral bioavailability of Tp5."( Preparation and evaluation of poly-butylcyanoacrylate nanoparticles for oral delivery of thymopentin.
He, W; Jiang, X; Zhang, ZR, 2008
)
0.35
" TP5 solution, the bioavailability and therapeutic efficacy of TP5 were remarkably strengthened after the pulmonary administration of the microparticles."( Inhalable microparticles as carriers for pulmonary delivery of thymopentin-loaded solid lipid nanoparticles.
Gong, T; Li, YZ; Liu, J; Sun, X; Zhang, ZR; Zuo, J, 2010
)
0.36
"05), and the improvement of bioavailability was dose-dependent."( Box-Behnken optimization design and enhanced oral bioavailability of thymopentin-loaded poly (butyl cyanoacrylate) nanoparticles.
Cao, F; Huang, A; Jin, X; Ping, Q; Su, Z, 2011
)
0.37
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" These findings suggest that using select inhibitors and lipid-based nanocarriers can decrease peptide degradation and may improve oral bioavailability of TP5 following oral administration."( Exploring ex vivo peptideolysis of thymopentin and lipid-based nanocarriers towards oral formulations.
Chen, S; Kang, D; Liu, M; Loh, J; Proft, T; Svirskis, D; Wen, J, 2022
)
0.72

Dosage Studied

In 25 patients with cervical, uterine and ovarian cancer with a depletion of T-helper cells and a lack of reactivity in the LMI-Test a course of immunotherapy with thymopentin (Timunox, Cilag Biotech) was performed.

ExcerptRelevanceReference
" This may reflect an innate incapacity of these cells to express this antigen or dosage requirements in excess of those tested."( Lack of T6 induction on human corneal Langerhans cells in vitro.
Chandler, JW; Seto, SK, 1990
)
0.28
" Transmucosal delivery may offer advantages over other routes, but published data have shown relatively poor efficacy when dosed nasally."( An aminoboronic acid derivative inhibits thymopentin metabolism by mucosal membrane aminopeptidases.
Aungst, BJ; Hussain, MA; Koval, CA; Shenvi, AB, 1990
)
0.28
"In 25 patients with cervical, uterine and ovarian cancer with a depletion of T-helper cells and a lack of reactivity in the LMI-Test a course of immunotherapy with thymopentin (Timunox, Cilag Biotech) at a dosage of 100 mg/die for 2 weeks and subsequently 100 mg 3 x/week for 4 weeks was performed and a comparison was made with a control group of 59 patients receiving no immunotherapy."( [The effect of immunotherapy with thymopentin on the parameters of cellular immunity and the clinical course of gynecologic tumor patients].
Krebs, D; Mallmann, P, 1989
)
0.28
" The Authors give the preliminary results of a pilot study carried out on 12 patients with LAS/ARC treated with Thymopentin at a dosage of 50 mg by intra muscular injection on alternate days for cycles of 30 days."( Thymopentin (TP-5) therapy during lymphadenopathy syndrome (LAS/ARC): preliminary report.
Boni, P; Chiodo, F; Colangeli, V; Costigliola, P; Pintori, C; Ricchi, E, 1987
)
0.27
" TP-5 was administered three times weekly at a dosage of 50 mg subcutaneously in 6 patients, 50 mg intravenously in 1 patient, and 100 mg subcutaneously in 1 patient."( Treatment of cutaneous T-cell lymphomas with TP-5. Evaluation of the clinical effect in 8 patients.
Braun-Falco, O; Burg, G; Przybilla, B; Schmoeckel, C, 1983
)
0.27
" Three trials were performed: a six month double-blind trial comparing TP-5 administered subcutaneously to placebo at 3 different dosages, an open longterm study in which the same dosage of the drug was administered subcutaneously, and a shortterm (3 weeks) double-blind trial in which the drug was given intravenously at a high dosage (100 mg/day)."( Thymopoietin pentapeptide (thymopentin, TP-5) in the treatment of rheumatoid arthritis. A compilation of several short- and longterm clinical studies.
Goldstein, G; Mielants, H; Newdeck, E; Power, D; Spiro, T; Verbruggen, G; Veys, EM, 1984
)
0.27
" A single dosage (0."( Synthetic immunomodulators for prevention of fatal infections in a burned guinea pig model.
Alexander, JW; Gonce, SJ; Loose, LD; Miskell, P; Stinnett, JD; Tenney, CL, 1983
)
0.27
" Our experiments did not show any great differences in the overall efficacy of the two drugs, although they showed quite a different dose-response effect."( Effect of synthetic thymic hormones on the cocaine-induced inhibition of the primary immune response in mice.
Di Francesco, P; Falchetti, R; Favalli, C; Garaci, E; Gaziano, R; Lanzilli, G; Ravagnan, G, 1993
)
0.29
" The most frequently used dosing regimen is 50 mg SC three times a week for 6 weeks, which may be repeated after 3-6 months."( Thymopentin prophylactic treatment in patients with recurrent respiratory infections.
Sundal, E,
)
0.13
" The main adverse effect is haemolytic anaemia, which necessitates careful monitoring and adjustment of dosage in many cases."( Tolerability of treatments for viral hepatitis.
Boyer, N; Gervais, A; Marcellin, P, 2001
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
oligopeptideA peptide containing a relatively small number of amino acids.
[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)
Chain A, Beta-lactamaseEscherichia coli K-12Potency10.00000.044717.8581100.0000AID485341
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (8)

Assay IDTitleYearJournalArticle
AID45840Ability to bound CEM cell measured as competition for displacement of radiolabeled Thymopentin from the receptor1997Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15
Stabilized analogs of thymopentin. 2. 1,2- and 3,4-ketomethylene pseudopeptides.
AID45838Binding efficacy expressed as counts remaining after competition was subtracted from total of Thymopentin and divided by the counts reduced by authentic Thymopentin1997Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15
Stabilized analogs of thymopentin. 2. 1,2- and 3,4-ketomethylene pseudopeptides.
AID9963The plasma half life of compound was determined on heparin prepared by mouse plasma. 1997Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15
Stabilized analogs of thymopentin. 2. 1,2- and 3,4-ketomethylene pseudopeptides.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (387)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990166 (42.89)18.7374
1990's122 (31.52)18.2507
2000's39 (10.08)29.6817
2010's46 (11.89)24.3611
2020's14 (3.62)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 (%)
Trials97 (21.80%)5.53%
Reviews27 (6.07%)6.00%
Case Studies20 (4.49%)4.05%
Observational0 (0.00%)0.25%
Other301 (67.64%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (9)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Phase III Study of Thymopentin in Patients After Curative Resection of Small [NCT00460681]Phase 3220 participants (Anticipated)Interventional2007-02-28Recruiting
Double Blind Study of Thymopentin Effects on HIV-1 Infectivity of Blood Mononuclear Cells and Semen in HIV Infected Patients [NCT00002049]0 participants InterventionalCompleted
Double-Blind Study of Timunox (Thymopentin) in Asymptomatic HIV-Infected Patients Receiving Either Mono (AZT or ddI) or Combination (AZT/ddI or AZT/ddC) Anti-Retroviral Therapy [NCT00002109]Phase 30 participants InterventionalCompleted
Double Blind Study of Thymopentin Effects on HIV-1 Infectivity of Blood Mononuclear Cells and Semen in HIV Infected Patients [NCT00002289]0 participants InterventionalCompleted
A Study of Thymopentin Effects on HIV-1 Infectivity of Blood Mononuclear Cells and Semen in HIV Infected Patients [NCT00002050]0 participants InterventionalCompleted
Double-Blind Study of the Effect of Timunox (Thymopentin) on Lymphoproliferative Responses and Virus Load in HIV-Infected Subjects Receiving Nucleoside Analog Antiretroviral Therapy [NCT00002332]Phase 260 participants InterventionalCompleted
Double Blind Study of Thymopentin Effects on Patients With HIV-1 Infection [NCT00002066]0 participants InterventionalCompleted
Double Blind Study of Thymopentin Effects on Patients With HIV-1 Infection [NCT00002051]0 participants InterventionalCompleted
The Prospective Clinical Study of Precision PRaG Therapy in Elderly Patients With Advanced Solid Malignant Tumors(PRaG9.0) [NCT06112041]Phase 229 participants (Anticipated)Interventional2023-10-25Not yet recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]