Compounds > melflufen
Page last updated: 2024-11-12

melflufen

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

Description

melflufen: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9935639
CHEMBL ID4303060
SCHEMBL ID18239898
MeSH IDM0589708

Synonyms (37)

Synonym
f70c5k4786 ,
MFF ,
melphalan flufenamide
j 1
melphalan flufenamide [usan:inn]
prodrug j 1
j-1
380449-51-4
unii-f70c5k4786
ethyl (2s)-2-((2s)-2-amino-3-(4-(bis(2-chloroethyl)amino)phenyl)propanamido)-3-(4-fluorophenyl)propanoate
prodrug j-1
j-1 (prodrug)
who 9493
l-phenylalanine, 4-(bis(2-chloroethyl)amino)-l-phenylalanyl-4-fluoro-, ethyl ester
melflufen
j 1 (prodrug)
prodrug j1
j1
melphalan flufenamide [usan]
melphalan flufenamide [who-dd]
melphalan flufenamide [inn]
j1 (prodrug)
SCHEMBL18239898
DTXSID40191461
melphalan flufenamide (usan/inn)
D11865
HY-105019
CS-0024709
ethyl (s)-2-((s)-2-amino-3-(4-(bis(2-chloroethyl)amino)phenyl)propanamido)-3-(4-fluorophenyl)propanoate
380449-51-4 (free base)
Q27277739
CHEMBL4303060
pepaxti
ethyl (2s)-2-[[(2s)-2-amino-3-[4-[bis(2-chloroethyl)amino]phenyl]propanoyl]amino]-3-(4-fluorophenyl)propanoate
gtpl11605
GLXC-25713
AKOS040752993

Research Excerpts

Overview

Melflufen is a novel anticancer peptide-drug conjugate compound for patients with relapsed refractory multiple myeloma. Melflufen rapidly delivers a cytotoxic payload into tumor cells.

ExcerptReferenceRelevance
"Melflufen is a novel anticancer peptide-drug conjugate compound for patients with relapsed refractory multiple myeloma."( Growth Response and Differentiation of Bone Marrow-Derived Mesenchymal Stem/Stromal Cells in the Presence of Novel Multiple Myeloma Drug Melflufen.
Emeh, P; Eskelinen, A; Gebraad, A; Heckman, CA; Kuismanen, K; Lehmann, F; Manninen, M; Miettinen, JJ; Miettinen, S; Nupponen, NN; Ohlsbom, R; Pakarinen, TK; Slipicevic, A, 2022)		1.65
"Melflufen is a novel peptide-drug conjugate that rapidly delivers a cytotoxic payload into tumor cells. "( OCEAN: a randomized Phase III study of melflufen + dexamethasone to treat relapsed refractory multiple myeloma.
Aschan, J; Pour, L; Robak, P; Schjesvold, F; Sonneveld, P, 2020)		2.27
"Melflufen is a peptide-conjugated alkylator belonging to a novel class of compounds, representing an overcoming of L-PAM in terms of mechanism of action and effectiveness."( Spotlight on Melphalan Flufenamide: An Up-and-Coming Therapy for the Treatment of Myeloma.
Al-Janazreh, H; Canale, FA; Cutrona, G; D'Arrigo, G; Gentile, M; Martino, EA; Martino, M; Mendicino, F; Morabito, F; Morabito, L; Neri, A; Todoerti, K; Tripepi, G; Vigna, E, 2021)		1.34
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID1916663Potency index, ratio of Melphalan IC50 to test compound IC50 for cytotoxicity against patient-derived human lymphoma cells assessed as cell growth inhibition incubated for 72 hrs by FMCA assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Melphalan: Recent insights on synthetic, analytical and medicinal aspects.
AID1916662Cytotoxicity against patient-derived human lymphoma cells assessed as cell growth inhibition incubated for 72 hrs by FMCA assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Melphalan: Recent insights on synthetic, analytical and medicinal aspects.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (31)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's8 (25.81)24.3611
2020's23 (74.19)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 42.73

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index42.73 (24.57)
Research Supply Index3.64 (2.92)
Research Growth Index4.94 (4.65)
Search Engine Demand Index61.01 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (42.73)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials6 (19.35%)5.53%
Reviews7 (22.58%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other18 (58.06%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
thalidomide
Thalidomide: A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, but withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of immunological and inflammatory disorders. Thalidomide displays immunosuppressive and anti-angiogenic activity. It inhibits release of TUMOR NECROSIS FACTOR-ALPHA from monocytes, and modulates other cytokine action.. thalidomide : A racemate comprising equimolar amounts of R- and S-thalidomide.. 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione : A dicarboximide that is isoindole-1,3(2H)-dione in which the hydrogen attached to the nitrogen is substituted by a 2,6-dioxopiperidin-3-yl group.		5.5822phthalimides;
piperidones
phenylalanine
Phenylalanine: An essential aromatic amino acid that is a precursor of MELANIN; DOPAMINE; noradrenalin (NOREPINEPHRINE), and THYROXINE.. L-phenylalanine : The L-enantiomer of phenylalanine.. phenylalanine : An aromatic amino acid that is alanine in which one of the methyl hydrogens is substituted by a phenyl group.		11.96286amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
phenylalanine;
proteinogenic amino acid		algal metabolite;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
Escherichia coli metabolite;
human xenobiotic metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
cytarabine
[no description available]		3.7320beta-D-arabinoside;
monosaccharide derivative;
pyrimidine nucleoside		antimetabolite;
antineoplastic agent;
antiviral agent;
immunosuppressive agent
daunorubicin
Daunorubicin: A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of LEUKEMIA and other NEOPLASMS.. anthracycline : Anthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine.. daunorubicin : A natural product found in Actinomadura roseola.		2.1510aminoglycoside antibiotic;
anthracycline;
p-quinones;
tetracenequinones		antineoplastic agent;
bacterial metabolite
pomalidomide
3-aminophthalimidoglutarimide: structure in first source		10.9332aromatic amine;
dicarboximide;
isoindoles;
piperidones		angiogenesis inhibitor;
antineoplastic agent;
immunomodulator
lenalidomide
[no description available]		10.5822aromatic amine;
dicarboximide;
isoindoles;
piperidones		angiogenesis inhibitor;
antineoplastic agent;
immunomodulator
bortezomib
[no description available]		2.4110amino acid amide;
L-phenylalanine derivative;
pyrazines		antineoplastic agent;
antiprotozoal drug;
protease inhibitor;
proteasome inhibitor
melphalan
Melphalan: An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - MELPHALAN, the racemic mixture - MERPHALAN, and the dextro isomer - MEDPHALAN; toxic to bone marrow, but little vesicant action; potential carcinogen.. melphalan : A phenylalanine derivative comprising L-phenylalanine having [bis(2-chloroethyl)amino group at the 4-position on the phenyl ring.		12.2306L-phenylalanine derivative;
nitrogen mustard;
non-proteinogenic L-alpha-amino acid;
organochlorine compound		alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent
parthenolide, (1ar-(1ar*,4e,7as*,10as*,10br*))-isomer
[no description available]		3.5110germacranolide
dasatinib
N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).		2.13101,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
selinexor
selinexor: inhibits karyopherin XPO1		8.5110
ConditionIndicatedRelationship StrengthStudiesTrials
Kahler Disease
[description not available]		012.66315
Multiple Myeloma
A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.		114.66315
Benign Neoplasms
[description not available]		04.8821
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.		16.8821
Diffuse Large B-Cell Lymphoma
[description not available]		02.4110
Lymphoma, Large B-Cell, Diffuse
Malignant lymphoma composed of large B lymphoid cells whose nuclear size can exceed normal macrophage nuclei, or more than twice the size of a normal lymphocyte. The pattern is predominantly diffuse. Most of these lymphomas represent the malignant counterpart of B-lymphocytes at midstage in the process of differentiation.		02.4110
Brill-Symmers Disease
[description not available]		06.790
Lymphoma, Follicular
Malignant lymphoma in which the lymphomatous cells are clustered into identifiable nodules within the LYMPH NODES. The nodules resemble to some extent the GERMINAL CENTER of lymph node follicles and most likely represent neoplastic proliferation of lymph node-derived follicular center B-LYMPHOCYTES.		06.790
Recrudescence
[description not available]		06.7432
Local Neoplasm Recurrence
[description not available]		04.8821
Breast Cancer
[description not available]		07.2510
Breast Neoplasms
Tumors or cancer of the human BREAST.		02.2510
Disease Exacerbation
[description not available]		05.4422
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.0810
Angiogenesis, Pathologic
[description not available]		02.4920
Blood Diseases
[description not available]		03.511
Hematologic Diseases
Disorders of the blood and blood forming tissues.		03.511
Cancer of the Urinary Tract
[description not available]		02.1310
Germinoblastoma
[description not available]		02.1310
Lymphoma
A general term for various neoplastic diseases of the lymphoid tissue.		07.1310
Cancer of Ovary
[description not available]		02.1310
Peritoneal Carcinomatosis
[description not available]		02.1310
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.		02.1310
Peritoneal Neoplasms
Tumors or cancer of the PERITONEUM.		02.1310
Acute Myelogenous Leukemia
[description not available]		02.1510
Leukemia, Myeloid, Acute
Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.		02.1510