Identification

Name
Semaglutide
Accession Number
DB13928
Type
Small Molecule
Groups
Approved, Investigational
Description

Semaglutide is a once-daily glucagon-like peptide-1 analog that differs to others by the presence of an acyl group with a steric diacid at Lys26 and a large synthetic spacer and modified by the presence of a α-aminobutyric acid in position 8 which gives stability against the dipeptidylpeptidase-4.[1] The stability of semaglutide by the acylation permits a high-affinity albumin binding and gives it a long plasma half-life which allows the once-daily dosage. It was developed by the Danish pharmaceutical company Novo Nordisk and FDA approved on December 5, 2017.[6]

Structure
Thumb
Synonyms
Not Available
External IDs
NN-9535 / NN9535 / NNC 0113-0217 / NNC-0113-0217
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
OzempicSolution1.34 mgSubcutaneousNovo Nordisk2018-02-22Not applicableCanada
OzempicInjection, solution1.34 mg/1mLSubcutaneousNovo Nordisk2017-12-06Not applicableUs
OzempicSolution1.34 mgSubcutaneousNovo Nordisk2018-02-22Not applicableCanada
OzempicInjection, solution1.34 mg/1mLSubcutaneousNovo Nordisk2017-12-06Not applicableUs
Categories
UNII
53AXN4NNHX
CAS number
910463-68-2
Weight
Average: 4113.641
Monoisotopic: 4111.11537713
Chemical Formula
C187H291N45O59
InChI Key
DLSWIYLPEUIQAV-CCUURXOWSA-N
InChI
InChI=1S/C187H291N45O59/c1-18-105(10)154(180(282)208-108(13)159(261)216-133(86-114-89-200-119-50-40-39-49-117(114)119)170(272)218-129(82-102(4)5)171(273)228-152(103(6)7)178(280)215-121(53-44-72-199-186(192)193)162(264)201-91-141(242)209-120(52-43-71-198-185(190)191)161(263)204-94-151(257)258)230-172(274)131(83-111-45-33-31-34-46-111)219-167(269)126(64-69-149(253)254)214-166(268)122(51-41-42-70-195-144(245)98-290-79-78-289-76-74-197-145(246)99-291-80-77-288-75-73-196-139(240)66-61-127(183(285)286)211-140(241)54-37-29-27-25-23-21-19-20-22-24-26-28-30-38-55-146(247)248)212-158(260)107(12)206-157(259)106(11)207-165(267)125(60-65-138(189)239)210-142(243)92-202-163(265)123(62-67-147(249)250)213-168(270)128(81-101(2)3)217-169(271)130(85-113-56-58-116(238)59-57-113)220-175(277)135(95-233)223-177(279)137(97-235)224-179(281)153(104(8)9)229-174(276)134(88-150(255)256)221-176(278)136(96-234)225-182(284)156(110(15)237)231-173(275)132(84-112-47-35-32-36-48-112)222-181(283)155(109(14)236)227-143(244)93-203-164(266)124(63-68-148(251)252)226-184(287)187(16,17)232-160(262)118(188)87-115-90-194-100-205-115/h31-36,39-40,45-50,56-59,89-90,100-110,118,120-137,152-156,200,233-238H,18-30,37-38,41-44,51-55,60-88,91-99,188H2,1-17H3,(H2,189,239)(H,194,205)(H,195,245)(H,196,240)(H,197,246)(H,201,264)(H,202,265)(H,203,266)(H,204,263)(H,206,259)(H,207,267)(H,208,282)(H,209,242)(H,210,243)(H,211,241)(H,212,260)(H,213,270)(H,214,268)(H,215,280)(H,216,261)(H,217,271)(H,218,272)(H,219,269)(H,220,277)(H,221,278)(H,222,283)(H,223,279)(H,224,281)(H,225,284)(H,226,287)(H,227,244)(H,228,273)(H,229,276)(H,230,274)(H,231,275)(H,232,262)(H,247,248)(H,249,250)(H,251,252)(H,253,254)(H,255,256)(H,257,258)(H,285,286)(H4,190,191,198)(H4,192,193,199)/t105-,106-,107-,108-,109+,110+,118-,120-,121-,122-,123-,124-,125-,126-,127+,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,152-,153-,154-,155-,156-/m0/s1
IUPAC Name
17-{[(1R)-3-[(2-{2-[({2-[2-({[(5S)-5-[(2S)-2-[(2S)-2-[(2S)-2-{2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S,3R)-2-[(2S)-2-[(2S,3R)-2-{2-[(2S)-2-{2-[(2S)-2-amino-3-(1H-imidazol-4-yl)propanamido]-2-methylpropanamido}-4-carboxybutanamido]acetamido}-3-hydroxybutanamido]-3-phenylpropanamido]-3-hydroxybutanamido]-3-hydroxypropanamido]-3-carboxypropanamido]-3-methylbutanamido]-3-hydroxypropanamido]-3-hydroxypropanamido]-3-(4-hydroxyphenyl)propanamido]-4-methylpentanamido]-4-carboxybutanamido]acetamido}-4-carbamoylbutanamido]propanamido]propanamido]-5-{[(1S)-1-{[(1S)-1-{[(1S,2S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-4-carbamimidamido-1-[({[(1S)-4-carbamimidamido-1-[(carboxymethyl)carbamoyl]butyl]carbamoyl}methyl)carbamoyl]butyl]carbamoyl}-2-methylpropyl]carbamoyl}-3-methylbutyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}ethyl]carbamoyl}-2-methylbutyl]carbamoyl}-2-phenylethyl]carbamoyl}-3-carboxypropyl]carbamoyl}pentyl]carbamoyl}methoxy)ethoxy]ethyl}carbamoyl)methoxy]ethoxy}ethyl)carbamoyl]-1-carboxypropyl]carbamoyl}heptadecanoic acid
SMILES
CC[C@H](C)[C@H](NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@@H](NC(=O)CCCCCCCCCCCCCCCCC(O)=O)C(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)CC1=CNC=N1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(O)=O

Pharmacology

Indication

Semaglutide is indicated to improve glycemic control in adults with type 2 diabetes mellitus as an adjunct of diet and exercise. The approved therapeutic doses are 0.5 mg and 1 mg.[7] Diabetes mellitus type 2 is a long-term metabolic disorder characterized by high blood sugar, insulin resistance and lack of insulin. Its onset is determined by the loss ability of beta cells to respond to an increased plasma glucose. This disease is predominantly caused by lifestyle factors like overweight and obesity. The key feature on type 2 diabetes is the presence of insulin resistance which reduced the capacity of insulin to exert its functions at normal at any given concentration. The secretion of insulin is stimulated by the action of incretins in the gut like glucagon-like peptide 1, which also delays gastric emptying and induces satiety, and glucose-dependent insulinotropic polypeptide.[5]

Associated Conditions
Pharmacodynamics

In clinical trials, semaglutide reduced significantly the glycated hemoglobin (HbA1c) compared to other medications like sitagliptin, exenatide and insulin glargine U100. The HbA1c protein is a standard measure of high glucose as in normal conditions the hemoglobin forms 1-deoxyfructose. In the trials, it was also showed the ability of semaglutide to reduce the body weight.[7] After 12 weeks of treatment, semaglutide lowered fasting and postprandial glucose concentrations by increasing insulin production and decreasing glucagon secretion. It also lowered fasting triglycerides and VLDL cholesterol.[6]

Mechanism of action

Drugs like semaglutide affect the glucose control through several different mechanisms like the increase of insulin secretion, slow of gastric emptying, and reduction of postprandial glucagon and food intake. The glucose homeostasis depends on hormones like insulin and amylin secreted in pancreatic beta cells, glucagon secreted in pancreatic alpha cells and gastrointestinal peptides like glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide. When glucose is administered orally, GLP-1 will stimulate the synthesis of insulin by stimulating pancreatic islets, it will also slow the gastric emptying, inhibit post-meal glucagon release and reduce food intake. GLP-1 has a major role in glucose management and semaglutide presents an analog structure which allows it to perform all the activities of GLP-1.[3] The innovative section of semaglutide is the presence of structural modifications (amino acid substitution at position 8) that generate superior stability against dipeptidyl peptidase-4 which is an enzyme that degrades incretins like GLP-1. The structure of semaglutide (lysine acylation with a spacer and C-18 fatty di-acid at position 26) also permits an increased and specific binding to plasma albumin; as well as a modification (amino acid substitution at position 34) that prevents C-18 fatty di-acid binding in wrong sites. All these characteristics donate semaglutide with an extended half-life, increasing patient compliance and quality of life.[2]

TargetActionsOrganism
AGlucagon-like peptide 1 receptor
agonist
Human
Absorption

Semaglutide absorption generated, in pharmacokinetic trials, the values of Cmax of 10.9 nmol/L, AUC of 3123.4 nmol h/L and a t max of 56 h.[4]

Volume of distribution

The blood distribution of semaglutide is negligible representing a 55% of the drug resting in the plasma while the rest 45% of the drug is on the hematocrit. The volume of distribution of semaglutide is 9.4 L.[4]

Protein binding

The plasma protein binding is one of the improved characteristics of semaglutide. This capacity of binding specifically and with high affinity to plasma albumin provides semaglutine with a higher stability.[2] Thus, it is highly bound to plasma protein where it is possible to find 99% of the administered dose in the bound-state.[8]

Metabolism

The metabolism of semaglutide is slowly but extensively metabolized prior to excretion. This was observed as 83% of the administered dose found in the plasma is composed of the unchanged drug. As a product of the metabolism, six different metabolites were identified in human plasma in which the major metabolite, named P3, accounted for 7.7% of the administered dose, thus indicating a component below the relative exposure limit in the safety assessment. The metabolites were formed following proteolytic cleavage of the peptide backbone and beta-oxidation of the fatty acid side chain. The known enzymes to be involved in the degradation of semaglutide are dipeptidyl peptidase (DPP-4) and neural endopeptidase (NEP). DPP-4 inactivates semaglutide truncating the N-terminal sequence and NEP hydrolyze peptide bonds.[4]

Route of elimination

In pharmacokinetic studies, the administered dose of semaglutide was not completely recovered in the excreta and represented only 75.1% of the dose. From this recovered dose, the main elimination route was the urine by corresponding to 53%, followed by an 18.6% found in the feces and a minor amount eliminated through the expired air of 3.2%. From the excreted dose in the urine, there was observed the presence of 22 components of semaglutide where the intact form represented only 3.1% of the administered dose. In the case of the feces, there were seven components and there was no evidence of intact semaglutide.[4]

Half life

One of the major properties of semaglutide is its long half-life of 168 h.[4]

Clearance

The clearance rate of semaglutide is 0.039 L/h.[4]

Toxicity

In preclinical toxicity studies with semaglutide, there was observed the presence of mild c-cell hyperplasia, nests and dilated ultimobranchial ducts after three months of exposure with a 17X of the clinical dose. There was also reports of liver necrosis and centrilobular hypertrophy mainly in man in the same doses. Some ECG abnormalities and multifocal vacuolation and degeneration were observed in high dose studies (27X).[8]

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
2,4-thiazolidinedioneThe risk or severity of hypoglycemia can be increased when 2,4-thiazolidinedione is combined with Semaglutide.
5-(2-methylpiperazine-1-sulfonyl)isoquinolineThe therapeutic efficacy of Semaglutide can be increased when used in combination with 5-(2-methylpiperazine-1-sulfonyl)isoquinoline.
AcarboseThe risk or severity of hypoglycemia can be increased when Acarbose is combined with Semaglutide.
AcetazolamideThe therapeutic efficacy of Semaglutide can be increased when used in combination with Acetazolamide.
AcetohexamideSemaglutide may increase the hypoglycemic activities of Acetohexamide.
Acetyl sulfisoxazoleThe therapeutic efficacy of Semaglutide can be increased when used in combination with Acetyl sulfisoxazole.
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Semaglutide.
AgmatineThe risk or severity of hypoglycemia can be increased when Agmatine is combined with Semaglutide.
AICA ribonucleotideThe risk or severity of hypoglycemia can be increased when AICA ribonucleotide is combined with Semaglutide.
AlaproclateThe risk or severity of hypoglycemia can be increased when Alaproclate is combined with Semaglutide.
Food Interactions
Not Available

References

General References
  1. Gotfredsen CF, Molck AM, Thorup I, Nyborg NC, Salanti Z, Knudsen LB, Larsen MO: The human GLP-1 analogs liraglutide and semaglutide: absence of histopathological effects on the pancreas in nonhuman primates. Diabetes. 2014 Jul;63(7):2486-97. doi: 10.2337/db13-1087. Epub 2014 Mar 7. [PubMed:24608440]
  2. Blundell J, Finlayson G, Axelsen M, Flint A, Gibbons C, Kvist T, Hjerpsted JB: Effects of once-weekly semaglutide on appetite, energy intake, control of eating, food preference and body weight in subjects with obesity. Diabetes Obes Metab. 2017 Sep;19(9):1242-1251. doi: 10.1111/dom.12932. Epub 2017 May 5. [PubMed:28266779]
  3. Lee YS, Jun HS: Anti-diabetic actions of glucagon-like peptide-1 on pancreatic beta-cells. Metabolism. 2014 Jan;63(1):9-19. doi: 10.1016/j.metabol.2013.09.010. Epub 2013 Oct 17. [PubMed:24140094]
  4. Jensen L, Helleberg H, Roffel A, van Lier JJ, Bjornsdottir I, Pedersen PJ, Rowe E, Derving Karsbol J, Pedersen ML: Absorption, metabolism and excretion of the GLP-1 analogue semaglutide in humans and nonclinical species. Eur J Pharm Sci. 2017 Jun 15;104:31-41. doi: 10.1016/j.ejps.2017.03.020. Epub 2017 Mar 16. [PubMed:28323117]
  5. Barnett A. (2012). Type 2 diabetes (2nd ed.). Oxford.
  6. FDA Reports [Link]
  7. Novo Nordisk News [Link]
  8. FDA Reports [Link]
External Links
ChemSpider
34985066
ChEMBL
CHEMBL3616752
Wikipedia
Semaglutide
AHFS Codes
  • 68:20.06 — Incretin Mimetics

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentHepatobiliary disorders / Non-Alcoholic Fatty Liver Disease (NAFLD)1
1Active Not RecruitingTreatmentType 2 Diabetes Mellitus2
1CompletedBasic ScienceDiabetes Mellitus (DM) / Healthy Volunteers1
1CompletedTreatmentBMI >30 kg/m2 / Diabetes Mellitus (DM) / Healthy Volunteers / Metabolism and Nutrition Disorder1
1CompletedTreatmentDiabetes Mellitus (DM) / Healthy Volunteers13
1CompletedTreatmentDiabetes Mellitus (DM) / Healthy Volunteers / Type 2 Diabetes Mellitus9
1CompletedTreatmentDiabetes Mellitus (DM) / Hepatic Impaired / Type 2 Diabetes Mellitus1
1CompletedTreatmentDiabetes Mellitus (DM) / Impaired Renal Function / Type 2 Diabetes Mellitus1
1CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus9
1CompletedTreatmentType 2 Diabetes Mellitus1
1RecruitingTreatmentBMI >27 kg/m2 / BMI >30 kg/m21
1RecruitingTreatmentMetabolism and Nutrition Disorders / Overweight or Obesity1
1RecruitingTreatmentObesity and Overweight1
2Active Not RecruitingTreatmentHepatobiliary disorders / Non-Alcoholic Steatohepatitis1
2CompletedTreatmentBMI >30 kg/m2 / Metabolism and Nutrition Disorder1
2CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus3
2Not Yet RecruitingTreatmentParkinson's Disease (PD)1
3Active Not RecruitingTreatmentBMI >27 kg/m2 / BMI >30 kg/m21
3Active Not RecruitingTreatmentBMI >30 kg/m2 / Metabolism and Nutrition Disorder1
3Active Not RecruitingTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus2
3CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus21
3RecruitingTreatmentBMI >27 kg/m2 / BMI >30 kg/m23
3RecruitingTreatmentMetabolism and Nutrition Disorder / Overweight or Obesity1
3RecruitingTreatmentType 2 Diabetes Mellitus1
4RecruitingTreatmentType 2 Diabetes Mellitus1
Not AvailableEnrolling by InvitationNot AvailableDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus1
Not AvailableEnrolling by InvitationNot AvailableType 2 Diabetes Mellitus2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Injection, solutionSubcutaneous1.34 mg/1mL
SolutionSubcutaneous1.34 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8672898No2014-03-182022-01-02Us
US8684969No2014-04-012025-10-20Us
US9132239No2015-09-152032-02-01Us
US8920383No2014-12-302026-07-17Us
US6899699No2005-05-312022-01-02Us
US9108002No2015-08-182026-01-20Us
US8114833No2012-02-142025-08-13Us
US9486588No2016-11-082022-01-02Us
US9457154No2016-10-042027-09-27Us
USRE46363No2017-04-112026-08-03Us
US9687611No2017-06-272027-02-27Us
US9775953No2017-10-032026-07-17Us
US8129343No2012-03-062029-01-29Us
US8536122No2013-09-172026-03-20Us
US8579869No2013-11-122023-06-30Us
US7762994No2010-07-272024-05-23Us
US9861757No2018-01-092026-01-20Us
US9616180No2017-04-112026-01-20Us

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
logP-17ChemAxon
pKa (Strongest Acidic)2.74ChemAxon
pKa (Strongest Basic)12.26ChemAxon
Physiological Charge-4ChemAxon
Hydrogen Acceptor Count67ChemAxon
Hydrogen Donor Count57ChemAxon
Polar Surface Area1646.18 Å2ChemAxon
Rotatable Bond Count149ChemAxon
Refractivity1047.99 m3·mol-1ChemAxon
Polarizability427.73 Å3ChemAxon
Number of Rings6ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Transmembrane signaling receptor activity
Specific Function
This is a receptor for glucagon-like peptide 1. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
Gene Name
GLP1R
Uniprot ID
P43220
Uniprot Name
Glucagon-like peptide 1 receptor
Molecular Weight
53025.22 Da
References
  1. Lee YS, Jun HS: Anti-diabetic actions of glucagon-like peptide-1 on pancreatic beta-cells. Metabolism. 2014 Jan;63(1):9-19. doi: 10.1016/j.metabol.2013.09.010. Epub 2013 Oct 17. [PubMed:24140094]
  2. Durante C, Russo D, Verrienti A, Filetti S: XL184 (cabozantinib) for medullary thyroid carcinoma. Expert Opin Investig Drugs. 2011 Mar;20(3):407-413. doi: 10.1517/13543784.2011.559163. [PubMed:21314233]
  3. Barnett A. (2012). Type 2 diabetes (2nd ed.). Oxford.

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Virus receptor activity
Specific Function
Cell surface glycoprotein receptor involved in the costimulatory signal essential for T-cell receptor (TCR)-mediated T-cell activation. Acts as a positive regulator of T-cell coactivation, by bindi...
Gene Name
DPP4
Uniprot ID
P27487
Uniprot Name
Dipeptidyl peptidase 4
Molecular Weight
88277.935 Da
References
  1. Blundell J, Finlayson G, Axelsen M, Flint A, Gibbons C, Kvist T, Hjerpsted JB: Effects of once-weekly semaglutide on appetite, energy intake, control of eating, food preference and body weight in subjects with obesity. Diabetes Obes Metab. 2017 Sep;19(9):1242-1251. doi: 10.1111/dom.12932. Epub 2017 May 5. [PubMed:28266779]
  2. Jensen L, Helleberg H, Roffel A, van Lier JJ, Bjornsdottir I, Pedersen PJ, Rowe E, Derving Karsbol J, Pedersen ML: Absorption, metabolism and excretion of the GLP-1 analogue semaglutide in humans and nonclinical species. Eur J Pharm Sci. 2017 Jun 15;104:31-41. doi: 10.1016/j.ejps.2017.03.020. Epub 2017 Mar 16. [PubMed:28323117]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Zinc ion binding
Specific Function
Thermolysin-like specificity, but is almost confined on acting on polypeptides of up to 30 amino acids (PubMed:15283675, PubMed:8168535). Biologically important in the destruction of opioid peptide...
Gene Name
MME
Uniprot ID
P08473
Uniprot Name
Neprilysin
Molecular Weight
85513.225 Da
References
  1. Jensen L, Helleberg H, Roffel A, van Lier JJ, Bjornsdottir I, Pedersen PJ, Rowe E, Derving Karsbol J, Pedersen ML: Absorption, metabolism and excretion of the GLP-1 analogue semaglutide in humans and nonclinical species. Eur J Pharm Sci. 2017 Jun 15;104:31-41. doi: 10.1016/j.ejps.2017.03.020. Epub 2017 Mar 16. [PubMed:28323117]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inhibitor
General Function
Triglyceride lipase activity
Specific Function
The primary function of this lipase is the hydrolysis of triglycerides of circulating chylomicrons and very low density lipoproteins (VLDL). Binding to heparin sulfate proteogylcans at the cell sur...
Gene Name
LPL
Uniprot ID
P06858
Uniprot Name
Lipoprotein lipase
Molecular Weight
53162.07 Da
References
  1. FDA Reports [Link]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Not Available
Gene Name
AMY1A
Uniprot ID
P04745
Uniprot Name
Alpha-amylase 1
Molecular Weight
57767.49 Da
References
  1. FDA Reports [Link]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Blundell J, Finlayson G, Axelsen M, Flint A, Gibbons C, Kvist T, Hjerpsted JB: Effects of once-weekly semaglutide on appetite, energy intake, control of eating, food preference and body weight in subjects with obesity. Diabetes Obes Metab. 2017 Sep;19(9):1242-1251. doi: 10.1111/dom.12932. Epub 2017 May 5. [PubMed:28266779]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. FDA Reports [Link]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
Molecular Weight
77402.175 Da
References
  1. FDA Reports [Link]

Drug created on December 06, 2017 10:44 / Updated on December 10, 2018 13:39