pf-05231023

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

Description

PF-05231023: consists of a humanized monoclonal antibody linked to two molecules of (des-His1,Ala129Cys)FGF21 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	57654311
SCHEMBL ID	4400652
MeSH ID	M000613734

Synonyms (19)

Synonym
SCHEMBL4400652
AC-31459
HY-113697
CS-0063000
mal-amido-peg2-c2-amido-ph-c2-co-azd
1037589-69-7
pf-05231023
3-(2,5-dioxopyrrol-1-yl)-n-[2-[2-[3-oxo-3-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]propoxy]ethoxy]ethyl]propanamide
3-(2,5-dioxo-2,5-dihydro-1h-pyrrol-1-yl)-n-(2-(2-(3-oxo-3-((4-(3-oxo-3-(2-oxoazetidin-1-yl)propyl)phenyl)amino)propoxy)ethoxy)ethyl)propanamide
EX-A3150
dkl4esk12f ,
1h-pyrrole-1-propanamide, 2,5-dihydro-2,5-dioxo-n-(2-(2-(3-oxo-3-((4-(3-oxo-3-(2-oxo-1-azetidinyl)propyl)phenyl)amino)propoxy)ethoxy)ethyl)-
pf-05231023 crosslinking agent
unii-dkl4esk12f
2,5-dihydro-2,5-dioxo-n-(2-(2-(3-oxo-3-((4-(3-oxo-3-(2-oxo-1-azetidinyl)propyl)phenyl)amino)propoxy)ethoxy)ethyl)-1h-pyrrole-1-propanamide
D87156
MS-29782
pf 5231023
AKOS040742395

Research Excerpts

Pharmacokinetics

Excerpt	Reference	Relevance
" Here we report PF-05231023, a long-acting FGF21 analogue which is unique in that the half-life and subcutaneous (s."	( Pharmacokinetics (PK), pharmacodynamics (PD) and integrated PK/PD modeling of a novel long acting FGF21 clinical candidate PF-05231023 in diet-induced obese and leptin-deficient obese mice. Bernardo, B; Brenner, MB; Calle, R; Chabot, JR; Logan, A; Talukdar, S; Vage, C; Weng, Y; Yan, Q; Zhu, Y, 2015)	0.97
" Physiologically based pharmacokinetic models incorporating serum stability data and an extravascular extraction term based on differential bioavailability of intact NT and CT of FGF21 in monkeys improved accuracy of human PK predictions relative to Dedrick scaling."	( Mechanistic investigation of the preclinical pharmacokinetics and interspecies scaling of PF-05231023, a fibroblast growth factor 21-antibody protein conjugate. Calle, RA; Giragossian, C; Li, J; Liras, J; Logan, A; Pelletier, K; Piché-Nicholas, N; Rajadhyaksha, M; Vage, C; Weng, Y, 2015)	0.64

Bioavailability

Excerpt	Reference	Relevance
") bioavailability of the intact C-terminus are significantly different from those of the intact N-terminus (2 vs."	( Pharmacokinetics (PK), pharmacodynamics (PD) and integrated PK/PD modeling of a novel long acting FGF21 clinical candidate PF-05231023 in diet-induced obese and leptin-deficient obese mice. Bernardo, B; Brenner, MB; Calle, R; Chabot, JR; Logan, A; Talukdar, S; Vage, C; Weng, Y; Yan, Q; Zhu, Y, 2015)	0.62
" Intact CT of FGF21 displayed approximately 5-fold faster systemic plasma clearance (CL), an approximately 2-fold lower steady-state volume of distribution, and at least 5-fold lower bioavailability compared with NT."	( Mechanistic investigation of the preclinical pharmacokinetics and interspecies scaling of PF-05231023, a fibroblast growth factor 21-antibody protein conjugate. Calle, RA; Giragossian, C; Li, J; Liras, J; Logan, A; Pelletier, K; Piché-Nicholas, N; Rajadhyaksha, M; Vage, C; Weng, Y, 2015)	0.64

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

Research

Studies (11)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	10 (90.91)	24.3611
2020's	1 (9.09)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 25.17

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	25.17 (24.57)
Research Supply Index	2.71 (2.92)
Research Growth Index	4.54 (4.65)
Search Engine Demand Index	26.67 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (25.17)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	3 (27.27%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	8 (72.73%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
palmitic acid Palmitic Acid: A common saturated fatty acid found in fats and waxes including olive oil, palm oil, and body lipids.. hexadecanoic acid : A straight-chain, sixteen-carbon, saturated long-chain fatty acid.	2.21	1	long-chain fatty acid; straight-chain saturated fatty acid	algal metabolite; Daphnia magna metabolite; EC 1.1.1.189 (prostaglandin-E2 9-reductase) inhibitor; plant metabolite
guanethidine Guanethidine: An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues.. guanethidine : A member of the class of guanidines in which one of the hydrogens of the amino group has been replaced by a 2-azocan-1-ylethyl group.. guanethidine sulfate : A organic sulfate salt composed of two molecules of guanethidine and one of sulfuric acid.	2.17	1	azocanes; guanidines	adrenergic antagonist; antihypertensive agent; sympatholytic agent
cardiovascular agents Cardiovascular Agents: Agents that affect the rate or intensity of cardiac contraction, blood vessel diameter, or blood volume.	2.17	1
leptin Leptin: A 16-kDa peptide hormone secreted from WHITE ADIPOCYTES. Leptin serves as a feedback signal from fat cells to the CENTRAL NERVOUS SYSTEM in regulation of food intake, energy balance, and fat storage.	7.11	1

Condition	Relationship Strength	Studies	Trials
Fatty Liver, Nonalcoholic [description not available]	2.6	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	3.11	4	0
Cirrhosis, Liver [description not available]	2.6	1	0
Liver Cirrhosis Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.	2.6	1	0
Obesity A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).	6.4	7	2
Non-alcoholic Fatty Liver Disease Fatty liver finding without excessive ALCOHOL CONSUMPTION.	2.6	1	0
Diabetes Mellitus, Adult-Onset [description not available]	4.78	3	2
Insulin Sensitivity [description not available]	2.55	2	0
Diabetes Mellitus, Type 2 A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.	4.78	3	2
Insulin Resistance Diminished effectiveness of INSULIN in lowering blood sugar levels: requiring the use of 200 units or more of insulin per day to prevent HYPERGLYCEMIA or KETOSIS.	2.55	2	0
Blood Pressure, High [description not available]	4.87	2	1
Hypertension Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.	4.87	2	1
Hypertriglyceridemia A condition of elevated levels of TRIGLYCERIDES in the blood.	4.45	1	1
Alloxan Diabetes [description not available]	2.17	1	0
Autoimmune Diabetes [description not available]	2.17	1	0
Diabetes Mellitus, Type 1 A subtype of DIABETES MELLITUS that is characterized by INSULIN deficiency. It is manifested by the sudden onset of severe HYPERGLYCEMIA, rapid progression to DIABETIC KETOACIDOSIS, and DEATH unless treated with insulin. The disease may occur at any age, but is most common in childhood or adolescence.	2.17	1	0
Diabetic Retinopathy Disease of the RETINA as a complication of DIABETES MELLITUS. It is characterized by the progressive microvascular complications, such as ANEURYSM, interretinal EDEMA, and intraocular PATHOLOGIC NEOVASCULARIZATION.	2.17	1	0
Electrolytes Substances that dissociate into two or more ions, to some extent, in water. Solutions of electrolytes thus conduct an electric current and can be decomposed by it (ELECTROLYSIS). (Grant & Hackh's Chemical Dictionary, 5th ed)	2.17	1	0
Weight Reduction [description not available]	3.91	2	1
Weight Loss Decrease in existing BODY WEIGHT.	3.91	2	1
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	3.92	2	1

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