PASIREOTIDE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C58H66N10O9
Molecular Weight	1047.2062
Optical Activity	UNSPECIFIED
Defined Stereocenters	7 / 7
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[H][C@@]12C[C@H](CN1C(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC4=CC=C(OCC5=CC=CC=C5)C=C4)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC6=CNC7=C6C=CC=C7)NC(=O)[C@@H](NC2=O)C8=CC=CC=C8)OC(=O)NCCN

InChI

InChIKey=VMZMNAABQBOLAK-DBILLSOUSA-N

InChI=1S/C58H66N10O9/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/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)/t43-,46+,47+,48-,49+,50+,51+/m1/s1

HIDE SMILES / InChI

Molecular Formula	C58H66N10O9
Molecular Weight	1047.2062
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 2662	9.3 nM [IC50]
Somatostatin receptor 2 6 Target ID: CHEMBL1804 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf	Agonist 2662	1.0 nM [IC50]
Somatostatin receptor 3 3 Target ID: CHEMBL2028 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf	Agonist 2662	1.5 nM [IC50]
Somatostatin receptor 5 5 Target ID: CHEMBL1792 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf	Agonist 2662	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 8360	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 1.35544321E12

C_max

Value	Dose	Analyte	Population
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
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
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 unknown	Homo sapiens population: unhealthy age: sex: food status:
16.2 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01673646	60 mg 1 times / month multiple, intramuscular dose: 60 mg route of administration: intramuscular experiment type: multiple co-administered:	PASIREOTIDE unknown	Homo sapiens population: unhealthy age: sex: food status:
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 unknown	Homo sapiens population: unhealthy age: sex: food status:
17.3 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01673646	40 mg 1 times / month multiple, intramuscular dose: 40 mg route of administration: intramuscular experiment type: multiple co-administered:	PASIREOTIDE unknown	Homo sapiens population: unhealthy age: sex: food status:
7.18999999999999 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 unknown	Homo sapiens population: unhealthy age: sex: food status:
8.22999999999999 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01673646	20 mg 1 times / month multiple, intramuscular dose: 20 mg route of administration: intramuscular experiment type: multiple co-administered:	PASIREOTIDE unknown	Homo sapiens population: unhealthy age: sex: food status:

AUC

Value	Dose	Co-administered	Analyte	Population
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
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

T_1/2

Value	Dose	Co-administered	Analyte	Population
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
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

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 n = 6 Health Status: healthy Age Group: 18–40 years Sex: M Population Size: 6 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 n = 6 Health Status: healthy Age Group: 18–40 years Sex: M Population Size: 6 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 n = 1 Health Status: healthy Age Group: 27 years Sex: M Population Size: 1 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 (starting) 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 Page: p. 71-72	unhealthy, 40 years n = 82 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 82 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf Page: p. 71-72	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 Page: p. 71-72
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 Page: p. 71-72	unhealthy, 40 years n = 80 Health Status: unhealthy Condition: Cushing’s disease Age Group: 40 years Sex: M+F Population Size: 80 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000MedR.pdf Page: p. 71-72	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 Page: p. 71-72
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) n = 13 Health Status: unhealthy Condition: neuroendocrine tumors Age Group: 58.0 years (range: 42–78 years) Sex: M+F Population Size: 13 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) n = 16 Health Status: unhealthy Condition: neuroendocrine tumors Age Group: 60.0 years (range: 44–76 years) Sex: M+F Population Size: 16 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 1709	inducer 383 inhibitor 1752	inhibitor 1837	inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1437 UGT1A1 204 MRP2 367 BSEP 401 CYP2B6 799 OATP1B1 781 OATP1B3 700 CYP1A2 1509 CYP2C8 901 CYP2C19 1463 CYP2E1 876 CYP3A4/5 273 K+ channels 56 L-type Ca2+ channels 26 Nav1.5 95 BCRP 691 OCT1 506 OATP2B1 122	P-gp 1527 BCRP 555 OCT1 322 OATP1B1 403 OATP1B3 347 OATP2B1 103 CYP3A5 391	CYP1A2 689 CYP2B6 538 CYP2C8 168 CYP2C19 290 CYP3A 126 CYP1A1 109 CYP1B1 52 CYP2J2 3 P-gp 257 MRP2 111 UGT1A1 69

Drug as perpetrator

Target	Modality	Activity
BCRP 765	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000ClinPharmR.pdf Page: 5.0	no
CYP1A1 218	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP1A2 1673	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP1B1 68	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP2B6 985	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP2C19 1537	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP2C8 955	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP2J2 19	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP3A 295	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
L-type Ca2+ channels 28	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 52.0	no
MRP2 459	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
OATP1B1 796	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 18.0	no
OATP1B3 709	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 18.0	no
OATP2B1 125	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000ClinPharmR.pdf Page: 5.0	no
OCT1 523	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000ClinPharmR.pdf Page: 5.0	no
P-gp 1626	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
P-gp 1626	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 78.0	no
K+ channels 56	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 48.0	unlikely [IC50 >30 uM]
CYP2C9 1803	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	unlikely
UGT1A1 254	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	unlikely
CYP1A2 1673	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 77.0	weak [IC50 10 uM]
CYP3A4/5 330	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 77.0	weak [IC50 10 uM]
CYP2C19 1537	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 77.0	weak [IC50 25 uM]
CYP2C8 955	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 77.0	weak [IC50 50 uM]
CYP2B6 985	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 18.0	weak [IC50 80 uM]
CYP2E1 964	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 77.0	weak [IC50 >100 uM]
UGT1A1 254	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 324.0	weak [IC50 >59 uM]
BSEP 402	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 324.0	yes [IC50 10 uM]
MRP2 459	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 324.0	yes [IC50 10 uM]
CYP2C9 1803	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 324.0	yes [IC50 5 uM]
CYP2D6 1875	inhibitor 3240 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 1527	substrate 3326 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 555	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf Page: 12.0	no
OATP1B1 403	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf Page: 12.0	no
OATP1B3 347	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf Page: 12.0	no
OATP2B1 103	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf Page: 12.0	no
OCT1 322	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf Page: 12.0	no
CYP3A4 1709	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 324.0	weak
CYP3A5 391	substrate 3326 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 98	inhibitor 1613 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 52.0
hERG 1632	inhibitor 1613 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
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
eNovation Chemicals	D678245	https://www.enovationchem.com/ProductDetails.asp?ProductID=D678245

PubMed

Title	Date	PubMed
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 Oct	12239124
Functional activity of the multiligand analog SOM230 at human recombinant somatostatin receptor subtypes supports its usefulness in neuroendocrine tumors.	2004	15477717
Medicinal chemistry of somatostatin analogs leading to the DTPA and DOTA conjugates of the multi-receptor-ligand SOM230.	2005	16625840
New aspects in the diagnosis and treatment of Cushing disease.	2006	16809932
Agonist-biased signaling at the sst2A receptor: the multi-somatostatin analogs KE108 and SOM230 activate and antagonize distinct signaling pathways.	2010 Jan	19910453
Ligand-dependent mechanisms of sst2A receptor trafficking: role of site-specific phosphorylation and receptor activation in the actions of biased somatostatin agonists.	2011 Jun	21493671
Involvement of bone morphogenetic protein activity in somatostatin actions on ovarian steroidogenesis.	2013 Mar	23137853

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 `Thu Jul 06 22:14:31 UTC 2023` Edited by `admin` on `Thu Jul 06 22:14:31 UTC 2023`
Record UNII	98H1T17066
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

PASIREOTIDE

Official Name

English

pasireotide [INN]

Common Name

English

CYCLO((4R)-4-(2-AMINOETHYLCARBAMOYLOXY)-L-PROLYL-L-PHENYLGLYCYL-D-TRYPTOPHYL-L-LYSYL-4-O-BENZYL-L-TYROSYL-L-PHENYLALANYL-)

Common Name

English

PASIREOTIDE [VANDF]

Common Name

English

PASIREOTIDE [MI]

Common Name

English

PASIREOTIDE [MART.]

Common Name

English

SOM230

Code

English

Pasireotide [WHO-DD]

Common Name

English

PASIREOTIDE [USAN]

Common Name

English

SOM-230

Code

English

Classification Tree Code System Code

WHO-VATC

QH01CB05