PASIREOTIDE DIASPARTATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C58H66N10O9.2C4H7NO4
Molecular Weight	1313.4116
Optical Activity	UNSPECIFIED
Defined Stereocenters	9 / 9
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

N[C@@H](CC(O)=O)C(O)=O.N[C@@H](CC(O)=O)C(O)=O.[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=NEEFMPSSNFRRNC-HQUONIRXSA-N

InChI=1S/C58H66N10O9.2C4H7NO4/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;2*5-2(4(8)9)1-3(6)7/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);2*2H,1,5H2,(H,6,7)(H,8,9)/t43-,46+,47+,48-,49+,50+,51+;2*2-/m100/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

Molecular Formula	C4H7NO4
Molecular Weight	133.1027
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
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 2678	9.3 nM [IC50]
Somatostatin receptor 2 6 Target ID: CHEMBL1804 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf	Agonist 2678	1.0 nM [IC50]
Somatostatin receptor 3 3 Target ID: CHEMBL2028 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf	Agonist 2678	1.5 nM [IC50]
Somatostatin receptor 5 5 Target ID: CHEMBL1792 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf	Agonist 2678	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 8429	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 1737	inducer 389 inhibitor 1767	inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1461 UGT1A1 204 MRP2 383 BSEP 402 CYP2B6 810 OATP1B1 788 OATP1B3 706 CYP1A2 1524 CYP2C8 911 CYP2C19 1478 CYP2E1 882 CYP3A4/5 278 K+ channels 70 L-type Ca2+ channels 28 Nav1.5 97 BCRP 699 OCT1 512 OATP2B1 123	P-gp 1537 BCRP 561 OCT1 327 OATP1B1 406 OATP1B3 350 OATP2B1 104 CYP3A5 395	CYP1A2 701 CYP2B6 547 CYP2C8 168 CYP2C19 293 CYP3A 129 CYP1A1 108 CYP1B1 51 CYP2J2 3 P-gp 257 MRP2 111 UGT1A1 69

Drug as perpetrator

Target	Modality	Activity
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000ClinPharmR.pdf Page: 5.0	no
CYP1A1 218	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP1B1 67	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP2B6 1001	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP2C19 1553	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP2C8 965	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP2J2 19	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
CYP3A 298	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
L-type Ca2+ channels 30	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 52.0	no
MRP2 475	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 18.0	no
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 18.0	no
OATP2B1 126	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000ClinPharmR.pdf Page: 5.0	no
OCT1 543	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000ClinPharmR.pdf Page: 5.0	no
P-gp 1650	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	no
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 78.0	no
K+ channels 70	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 48.0	unlikely [IC50 >30 uM]
CYP2C9 1819	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	unlikely
UGT1A1 254	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 80.0	unlikely
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 77.0	weak [IC50 10 uM]
CYP3A4/5 335	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 77.0	weak [IC50 10 uM]
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 77.0	weak [IC50 25 uM]
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 77.0	weak [IC50 50 uM]
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 18.0	weak [IC50 80 uM]
CYP2E1 970	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 77.0	weak [IC50 >100 uM]
UGT1A1 254	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 324.0	weak [IC50 >59 uM]
BSEP 403	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 324.0	yes [IC50 10 uM]
MRP2 475	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 324.0	yes [IC50 10 uM]
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 324.0	yes [IC50 5 uM]
CYP2D6 1891	inhibitor 3277 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 1537	substrate 3367 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 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf Page: 12.0	no
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf Page: 12.0	no
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf Page: 12.0	no
OATP2B1 104	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf Page: 12.0	no
OCT1 327	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf Page: 12.0	no
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 324.0	weak
CYP3A5 395	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 324.0	weak

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
Nav1.5 100	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/200677Orig1s000PharmR.pdf Page: 52.0
hERG 1647	inhibitor 1626 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

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 `Sat Dec 16 18:32:03 UTC 2023` Edited by `admin` on `Sat Dec 16 18:32:03 UTC 2023`
Record UNII	I4P76SY3N4
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

PASIREOTIDE DIASPARTATE

Common Name

English

PASIREOTIDE DIASPARTATE [ORANGE BOOK]

Common Name

English

PASIREOTIDE DIASPARTATE [EMA EPAR]

Common Name

English

SIGNIFOR

Brand Name

English

Pasireotide diaspartate [WHO-DD]

Common Name

English

PASIREOTIDE (AS DIASPARTATE)

Common Name

English

CYCLO((2R)-2-PHENYLGLYCYL-D-TRYPTOPHYL-L-LYSYL-O-(PHENYLMETHYL)-L-TYROSYL-L-PHENYLALANYL-(4R)-4-((((2-AMINOETHYL)AMINO)CARBONYL)OXY)-L-PROLYL), L-ASPARTATE (1:2)

Common Name

English

Classification Tree Code System Code

EMA ASSESSMENT REPORTS

SIGNIFOR (AUTHORIZED: PITUITARY ACTH HYPERSECRETION)