PASIREOTIDE PAMOATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C58H66N10O9.C23H16O6
Molecular Weight	1435.5789
Optical Activity	UNSPECIFIED
Defined Stereocenters	7 / 7
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)C1=CC2=CC=CC=C2C(CC3=C(O)C(=CC4=CC=CC=C34)C(O)=O)=C1O.[H][C@@]56C[C@H](CN5C(=O)[C@H](CC7=CC=CC=C7)NC(=O)[C@H](CC8=CC=C(OCC9=CC=CC=C9)C=C8)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC%10=CNC%11=C%10C=CC=C%11)NC(=O)[C@@H](NC6=O)C%12=CC=CC=C%12)OC(=O)NCCN

InChI

InChIKey=HSXBEUMRBMAVDP-QKXVGOHISA-N

InChI=1S/C58H66N10O9.C23H16O6/c59-27-13-12-22-46-52(69)64-47(30-38-23-25-42(26-24-38)76-36-39-16-6-2-7-17-39)53(70)66-49(31-37-14-4-1-5-15-37)57(74)68-35-43(77-58(75)61-29-28-60)33-50(68)55(72)67-51(40-18-8-3-9-19-40)56(73)65-48(54(71)63-46)32-41-34-62-45-21-11-10-20-44(41)45;24-20-16(14-7-3-1-5-12(14)9-18(20)22(26)27)11-17-15-8-4-2-6-13(15)10-19(21(17)25)23(28)29/h1-11,14-21,23-26,34,43,46-51,62H,12-13,22,27-33,35-36,59-60H2,(H,61,75)(H,63,71)(H,64,69)(H,65,73)(H,66,70)(H,67,72);1-10,24-25H,11H2,(H,26,27)(H,28,29)/t43-,46+,47+,48-,49+,50+,51+;/m1./s1

HIDE SMILES / InChI

Molecular Formula	C23H16O6
Molecular Weight	388.3704
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	C58H66N10O9
Molecular Weight	1047.2084
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	7 / 7
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf | https://www.ncbi.nlm.nih.gov/pubmed/23605695

Pasireotide is a synthetic long-acting cyclic hexapeptide with somatostatin-like activity. It is marketed as a diaspartate salt called Signifor, indicated for the treatment of adult patients with Cushing’s disease for whom pituitary surgery is not an option or has not been curative. SIGNIFOR is an injectable cyclohexapeptide somatostatin analogue. Pasireotide exerts its pharmacological activity via binding to somatostatin receptors (ssts). Pasireotide binds and activates the hsst receptors resulting in inhibition of ACTH secretion, which leads to decreased cortisol secretion.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Somatostatin receptor 1 3 Target ID: CHEMBL1917 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf	Agonist 2752	9.3 nM [IC50]
Somatostatin receptor 2 6 Target ID: CHEMBL1804 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf	Agonist 2752	1.0 nM [IC50]
Somatostatin receptor 3 3 Target ID: CHEMBL2028 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf	Agonist 2752	1.5 nM [IC50]
Somatostatin receptor 5 5 Target ID: CHEMBL1792 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf	Agonist 2752	0.16 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Cushing’s disease 13 Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/002052/WC500128058.pdf https://www.ncbi.nlm.nih.gov/pubmed/23605695	Primary		Approved 8583	SIGNIFOR Approved Use SIGNIFOR is a somatostatin analog indicated for the treatment of adult patients with Cushing’s disease for whom pituitary surgery is not an option or has not been curative. Launch Date 2012

C_max

Value	Dose	Analyte	Population
8.23 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01673646	20 mg 1 times / 4 weeks multiple, intramuscular dose: 20 mg route of administration: intramuscular experiment type: multiple co-administered:	PASIREOTIDE plasma	Homo sapiens population: unhealthy age: ADULT sex: FEMALE / MALE food status: UNKNOWN
17.3 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01673646	40 mg 1 times / 4 weeks multiple, intramuscular dose: 40 mg route of administration: intramuscular experiment type: multiple co-administered:	PASIREOTIDE plasma	Homo sapiens population: unhealthy age: ADULT sex: FEMALE / MALE food status: UNKNOWN
16.2 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01673646	60 mg 1 times / 4 weeks multiple, intramuscular dose: 60 mg route of administration: Intramuscular experiment type: MULTIPLE co-administered:	PASIREOTIDE plasma	Homo sapiens population: unhealthy age: ADULT sex: FEMALE / MALE food status: UNKNOWN
7.19 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01673646	20 mg single, intramuscular dose: 20 mg route of administration: intramuscular experiment type: single co-administered:	PASIREOTIDE plasma	Homo sapiens population: unhealthy age: ADULT sex: FEMALE / MALE food status: UNKNOWN
10.3 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01673646	40 mg single, intramuscular dose: 40 mg route of administration: intramuscular experiment type: single co-administered:	PASIREOTIDE plasma	Homo sapiens population: unhealthy age: ADULT sex: FEMALE / MALE food status: UNKNOWN
17 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01673646	60 mg single, intramuscular dose: 60 mg route of administration: intramuscular experiment type: single co-administered:	PASIREOTIDE plasma	Homo sapiens population: unhealthy age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24800725/	60 mg single, subcutaneous dose: 60 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:	PASIREOTIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
38.7 ng/mL REVIEW https://pubmed.ncbi.nlm.nih.gov/29032486/	0.6 mg 2 times / day steady-state, subcutaneous dose: 0.6 mg route of administration: Subcutaneous experiment type: STEADY-STATE co-administered:	PASIREOTIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
4090 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24800725/	60 mg single, subcutaneous dose: 60 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:		PASIREOTIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
161.1 ng × h/mL REVIEW https://pubmed.ncbi.nlm.nih.gov/29032486/	0.6 mg 2 times / day steady-state, subcutaneous dose: 0.6 mg route of administration: Subcutaneous experiment type: STEADY-STATE co-administered:		PASIREOTIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
12 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24800725/	60 mg single, subcutaneous dose: 60 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:		PASIREOTIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4.4 h REVIEW https://pubmed.ncbi.nlm.nih.gov/29032486/	0.6 mg 2 times / day steady-state, subcutaneous dose: 0.6 mg route of administration: Subcutaneous experiment type: STEADY-STATE co-administered:		PASIREOTIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
1500 ug single, subcutaneous Highest studied dose Dose: 1500 ug Route: subcutaneous Route: single Dose: 1500 ug Sources: https://pubmed.ncbi.nlm.nih.gov/22713526	healthy, 18–40 years Health Status: healthy Age Group: 18–40 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/22713526	Sources: https://pubmed.ncbi.nlm.nih.gov/22713526
750 ug 2 times / day steady, subcutaneous Highest studied dose Dose: 750 ug, 2 times / day Route: subcutaneous Route: steady Dose: 750 ug, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/22713526	healthy, 18–40 years Health Status: healthy Age Group: 18–40 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/22713526	Sources: https://pubmed.ncbi.nlm.nih.gov/22713526
0.9 mg 2 times / day multiple, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: multiple Dose: 0.9 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/24088755	healthy, 27 years Health Status: healthy Age Group: 27 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/24088755	Disc. AE: Xanthoma... AEs leading to discontinuation/dose reduction: Xanthoma (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/24088755
0.6 mg 2 times / day steady, subcutaneous Recommended Dose: 0.6 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.6 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf	unhealthy, 40 years Health Status: unhealthy Age Group: 40 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf	Disc. AE: Diarrhea, Nausea... AEs leading to discontinuation/dose reduction: Diarrhea (1.2%) Nausea (1.2%) Fatigue (1.2%) Cholelithiasis (1.2%) GGT increased (3.7%) Hepatic enzyme increased (1.2%) Lipase increased (1.2%) Hyperglycemia (2.4%) Tremor (1.2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
0.9 mg 2 times / day steady, subcutaneous Recommended Dose: 0.9 mg, 2 times / day Route: subcutaneous Route: steady Dose: 0.9 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf	unhealthy, 40 years Health Status: unhealthy Age Group: 40 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf	Disc. AE: Diarrhea, Nausea... AEs leading to discontinuation/dose reduction: Diarrhea (2.5%) Nausea (1.3%) Fatigue (1.3%) Pituitary tumor benign (1.3%) GGT increased (2.5%) Cranial nerve paralysis (1.3%) Confusion state (1.3%) Hyperglycemia (3.8%) Tongue paralysis (1.3%) Adrenal insufficiency (1.3%) Fecal incontinence (1.3%) Asthenia (1.3%) ALT increased (1.3%) AST increased (1.3%) Immunoglobulin E increased (1.3%) QT interval prolonged (1.3%) Urinary incontinence (1.3%) Urticaria (1.3%) Hot flush (1.3%) Hypotension (1.3%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf
80 mg 1 times / day steady, intramuscular Dose: 80 mg, 1 times / day Route: intramuscular Route: steady Dose: 80 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28721067	unhealthy, 58.0 years (range: 42–78 years) Health Status: unhealthy Age Group: 58.0 years (range: 42–78 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28721067	Disc. AE: Diarrhea, Lipase increased... AEs leading to discontinuation/dose reduction: Diarrhea (4 patients) Lipase increased (4 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/28721067
120 mg 1 times / day steady, intramuscular MTD Dose: 120 mg, 1 times / day Route: intramuscular Route: steady Dose: 120 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28721067	unhealthy, 60.0 years (range: 44–76 years) Health Status: unhealthy Age Group: 60.0 years (range: 44–76 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28721067	Disc. AE: Gamma-glutamyltransferase increased, Hyperglycemia... Other AEs: Hyperglycemia, Abdominal pain... AEs leading to discontinuation/dose reduction: Gamma-glutamyltransferase increased (4 patients) Hyperglycemia (4 patients) Other AEs: Hyperglycemia (grade 3-4, 6.3%) Abdominal pain (grade 3-4, 7.7%) Blood alkaline phosphatase increased (grade 3-4, 7.7%) Sources: https://pubmed.ncbi.nlm.nih.gov/28721067
2.1 mg 2 times / day multiple, subcutaneous Overdose Dose: 2.1 mg, 2 times / day Route: subcutaneous Route: multiple Dose: 2.1 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf	healthy Health Status: healthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf	Other AEs: Diarrhea... Other AEs: Diarrhea Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946	inducer 440 inhibitor 2438	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1741 UGT1A1 246 MRP2 499 BSEP 550 CYP2B6 926 OATP1B1 1079 OATP1B3 961 CYP1A2 2153 CYP2C8 1057 CYP2C19 2057 CYP2E1 1060 CYP3A4/5 296 K+ channels 73 L-type Ca2+ channels 28 Nav1.5 116 BCRP 910 OCT1 620 OATP2B1 157	P-gp 2052 BCRP 697 OCT1 393 OATP1B1 503 OATP1B3 435 OATP2B1 122 CYP3A5 446	CYP1A2 832 CYP2B6 669 CYP2C8 198 CYP2C19 329 CYP3A 142 CYP1A1 151 CYP1B1 71 CYP2J2 3 P-gp 301 MRP2 146 UGT1A1 78

Drug as perpetrator

Target	Modality	Activity
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000ClinPharmR.pdf Page: 5.0	no
CYP1A1 272	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP1B1 93	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP2C8 1117	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP2J2 36	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP3A 317	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
L-type Ca2+ channels 30	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 52.0	no
MRP2 625	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 18.0	no
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 18.0	no
OATP2B1 162	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000ClinPharmR.pdf Page: 5.0	no
OCT1 656	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000ClinPharmR.pdf Page: 5.0	no
P-gp 1932	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 78.0	no
K+ channels 73	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 48.0	unlikely [IC50 >30 uM]
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	unlikely
UGT1A1 303	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	unlikely
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 77.0	weak [IC50 10 uM]
CYP3A4/5 357	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 77.0	weak [IC50 10 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 77.0	weak [IC50 25 uM]
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 77.0	weak [IC50 50 uM]
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 18.0	weak [IC50 80 uM]
CYP2E1 1146	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 77.0	weak [IC50 >100 uM]
UGT1A1 303	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 324.0	weak [IC50 >59 uM]
BSEP 554	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 324.0	yes [IC50 10 uM]
MRP2 625	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 324.0	yes [IC50 10 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 324.0	yes [IC50 5 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 324.0	yes [IC50 5 uM]

Drug as victim

Target	Modality	Activity	Clinical evidence
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf Page: 12.0	likely	yes (co-administration study) Comment: verapamil increased pasireotide permeation Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf Page: 12.0
BCRP 697	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf Page: 12.0	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf Page: 12.0	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf Page: 12.0	no
OATP2B1 122	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf Page: 12.0	no
OCT1 393	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf Page: 12.0	no
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 324.0	weak
CYP3A5 446	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 324.0	weak

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
Nav1.5 119	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 52.0
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 42.0

Sourcing

Vendor/Aggregator	ID	URL
AA Blocks	AA00C6E9	https://www.aablocks.com/goods/Goods/detail?id=AA00C6E9
Achemtek	0102-014407	http://www.achemtek.com/396091-73-9
Alsachim	3608	http://www.alsachim.com/product-C6134-glo.bal-view.html
BioCrick	BCC5300	http://www.biocrick.com/Pasireotide-BCC5300.html
Chem Scene	CS-2328	http://www.chemscene.com/396091-73-9.html
eNovation Chemicals	D678245	https://www.enovationchem.com/ProductDetails.asp?ProductID=D678245
Lab Network	LN02181389	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN02181389
MedChem Express	HY-16381	https://www.medchemexpress.com/pasireotide.html
MuseChem	I003446	https://www.musechem.com/product/I003446.html
Smolecule	S538667	http://www.smolecule.com/products/s538667
THE BioTek	bt-278884	https://www.thebiotek.com/product/inhibitors/bt-278884

PubMed

Title	Date	PubMed
Involvement of bone morphogenetic protein activity in somatostatin actions on ovarian steroidogenesis.	2013-03	23137853
Ligand-dependent mechanisms of sst2A receptor trafficking: role of site-specific phosphorylation and receptor activation in the actions of biased somatostatin agonists.	2011-06	21493671
Agonist-biased signaling at the sst2A receptor: the multi-somatostatin analogs KE108 and SOM230 activate and antagonize distinct signaling pathways.	2010-01	19910453
New aspects in the diagnosis and treatment of Cushing disease.	2006	16809932
Medicinal chemistry of somatostatin analogs leading to the DTPA and DOTA conjugates of the multi-receptor-ligand SOM230.	2005	16625840
Functional activity of the multiligand analog SOM230 at human recombinant somatostatin receptor subtypes supports its usefulness in neuroendocrine tumors.	2004	15477717
SOM230: a new somatostatin peptidomimetic with potent inhibitory effects on the growth hormone/insulin-like growth factor-I axis in rats, primates, and dogs.	2002-10	12239124

Patents

Sample Use Guides

In Vivo Use Guide

Recommended initial dosage is either 0.6 mg or 0.9 mg by subcutaneous injection twice a day; recommended dosage range is 0.3 mg to 0.9 mg twice a day

Route of Administration: Other

In Vitro Use Guide

Primary cultures from normal human and rat adrenals were incubated with 10-100 nM Pasireotide with and without 10nM ACTH. Dose-response studies with 1 nM-1 uM Pasireotide were performed on rat adrenals. Cortisol/corticosterone levels in medium were measured after 4 and 24h. Pasireotide (10nM) significantly increased corticosteroid levels after 24h incubation in both human (36.4 ± 0.43 ng/well vs 27.7 ± 3.17 ng/well, p<0.05) and rat (16.2 ± 1.16 ng/well vs 11.6 ± 0.92 ng/well p<0.05) adrenals; lesser effects were observed with 100 nM Pasireotide (33.4 ± 2.59 ng/well vs 27.7 ± 3.17 ng/well p<0.05; 13.4 ± 0.82 ng/well vs 11.6 ± 0.92 ng/well, N.S. vs baseline secretion for human and rat adrenals, respectively). Dose-response curves confirmed maximal effect at 10nM Pasireotide.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 22:38:12 GMT 2025` Edited by `admin` on `Mon Mar 31 22:38:12 GMT 2025`
Record UNII	04F55A7UZ3
Record Status	`FAILED`
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Name

Type

Language

PASIREOTIDE PAMOATE

Common Name

English

PASIREOTIDE EMBONATE

Preferred Name

English

SIGNIFOR LAR

Brand Name

English

Pasireotide embonate [WHO-DD]

Common Name

English

PASIREOTIDE PAMOATE [JAN]

Common Name

English

PASIREOTIDE PAMOATE [ORANGE BOOK]

Common Name

English

SOM230 PAMOATE

Code

English

SOM-230 PAMOATE

Code

English

CYCLO((2S)-2-PHENYLGLYCYL-D-TRYPTOPHYL-L-LYSYL-O-(PHENYLMETHYL)-L-TYROSYL-L-PHENYLALANYL-(4R)-4-((((2-AMINOETHYL)AMINO)CARBONYL)OXY)-L-PROLYL), 4,4'-METHYLENEBIS(3-HYDROXY-2-NAPHTHALENECARBOXYLATE) (1:1)

Systematic Name

English

Code System Code Type Description

EVMPD

SUB129748