research exemption peptides

8/12/2019 Research Exemption Peptides

1/4

1-800-777-4779

E-mail: [email protected]

Phone: 502-266-8787

Fax: 502-267-1329

P.O. Box 99703

Louisville, KY 40269-0703 USA

PeptidesInternational, Inc.

Over the past two decades,there have been many pep-tide drugs approved fortreating a variety of diseases.

Once the product has achieved regula-tory approval by having completed andpassed clinical trials determining it tobe safe and effective, it becomes a marketed Brand drug.Manufacturers of generic peptide drugs are able to utilizethe original manufacturers approval provided that they canshow that the generic peptide drug is bioequivalent to theapproved Brand drug. The generic producer is able to runtheir clinical trials, tests and studies on their generic peptide

without infringing upon the original manufacturers pat-ented drug before the patent has expired by way of the Bolarexemption in Europe and the UK (including Canada) andMerck vs. Integrafor the USA.

Some of the most important of these peptide drugs are avail-able from Peptides International and include:

Bivalirudin, BIV-3767-PI: This peptide drug is a direct andreversible thrombin inhibitor. Originally derived fromhiruidin, the salivary anticlot protein found in leeches, this20 residue peptide congener inhibits both circulating andclot bound thrombin as well as inhibiting platelet activationand aggregation in a highly specific and reversible man-ner. Bivalirudin clinical studies demonstrated consistentpositive outcomes in patients with stable angina, unstableangina (UA), non-ST segment elevation myocardial infarc-tion (NSTEMI).

Enfuvirtide, ENF-3787-PI: This 36 residue peptide blocks theentry of the HIV virus by binding to the virus gp41 protein.This prevents a conformational change in gp41 which is nec-essary for the virus to fuse and form the entry pore for thecapsid of the virus into the CD4+ T-cell, and keeps it fromentering the cell. This peptide drug has been used success-fully in HIV patients as part of a combination therapy withprotease and reverse transcriptase inhibitors.

Eptifibatide, EPT-3786-PI: Originally derived from a pro-

tein obtained from the venom of Southeastern PygmyRattlesnake, this cyclic heptapeptide is an anti-platelet drugwhich binds to the glycoprotein IIb-IIIa. The drug has avery short half life and is used to reduce the risk of acutecardiac ischemic events in patients with unstable anginaor in patients with non-ST-segment elevation myocardialinfarction.

Exenatide- Exendin-4,PEX-3784-PI:This 39 residue peptidewas originally isolated from the saliva of the Gila Monster.

The peptide is a GLP-1 (glucagon likepeptide) agonist and is an insulin secretagogue with glucoregulatory effects. Ihas been used extensively in treatingtype II diabetes in combination with metformin and pioglitazone.

Linaclotide, LIN-3796-PI: This disulfide-rich peptide is anagonist of gaunylate cyclase 2c. It is currently approved as anorally delivered treatment for chronic constipation.

Liraglutide,PGL-3781-PI:This peptide is a long acting GLP-1agonist and is an acylated variant of human GLP-1 (7-37)The selective fatty acylation of the peptide increases the

half life to 11-15 hours following a sub-cutaneous injectionallowing for once daily injection. This peptide drug has beenwidely used to treat type II diabetes.

Lixisenatide - Lyxumia, LIX-3799-PI:This peptide is a GLP-1receptor agonist. Originally discovered by Zealand Pharmait was licensed and developed by Sanofi for its use in thetreatment of Type 2 diabetes. GLP-1 is a natually occuringpeptide, released shortly after a meal has been consumed.

Semaglutide, GLP-3875-PI: We are proud to introduceresearch-grade semaglutide. Semaglutide is a glucagon-likepeptide (GLP-1) analogue and a GLP-1 receptor agonist. Noonly does it have a half-life of up to one week, it has beenused in type 2 diabetes research for its ability to stimulate

insulin production while suppressing glucagon secretion ina glucose-dependent manner. Semaglutide has an increasedalbumin affinity and exhibits a three-fold decrease in GLP-1receptor affinity when compared to liraglutide.1Recent studies in patients with Type II Diabetes suggest that semaglutide may also have an improved cardiovascular outcome inthose patients who are at risk for a cardiac event.2

TeduglutideTED-3880-PI: This is a 33 amino acid, glucagonlike peptide-2 (GLP-2) analog, used for the treatment ofshort bowel syndrome. It does this by promoting mucosagrowth and possibly restoring gastric emptying and secretion. Idiffers from the natural GLP-2 by an alanine that habeen replaced with a glycine.

Tetracosactide - ACTH (Human,1-24)PAC-4109-v:This peptide drug is derived from the N-terminal 24 amino acidsfrom the naturally occurring peptide hormone ACTH (adrenocorticotropin hormone). This peptide hormone inducesan increase in the levels of circulating glucocorticoids andis primarily used as a diagnostic for proper function of theadrenal glands. It has also been classified as a doping agenor performance enhancing drug (PED) in cycling.

Research Exemption (Generic) PeptidesPlease Note: These are FDA-regulatedproducts. It is the responsibility of thecustomer to ensure that they are complyingwith Federal rules. Peptides Internationalcannot be liable for infringement of rightsmade by the user.


2/4

1-800-777-4779


Phone: 502-266-8787

Fax: 502-267-1329

P.O. Box 99703


Peptides International, Inc.

CODE PRODUCT QTY USD

PAC-4109-v ACTH (Human,1-24) (Tetracosactide)

Adrenocorticotropic Hormone (Human, 1-24)

H-SYSMEHFRWGKPVGKKRRPVKVYP-OH

Increases the Circulating Level of Glucocorticoids

0.5 mg

vial

275

BIV-3767-PI Bivalirudin

H-f PRPGGGGNGDFEEIPEEYL-OH

Specific, Reversible, Direct ThrombinInhibitor

C. Michael and G. Mckendall,Am. J. Health-System Pharma., 60, 18 (2003).TE. Warkentin, Thromb. Haemost., 99, 830, 18 (2010).

1 mg

5 mg

44

200

PBN-4212-v BNP-32 (Human)(Nesiritide)

B-Type (Brain) Natriuretic Peptide-32 (Human)

H-SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH-OH

(Disulfide bridged)

Cardiac Hormone

0.5 mgvial

490

PCN-4289-v -Conotoxin MVIIA (Ziconotide)

(Marine Snail, Conus magus)

H-CKGKGAKCSRLMYDCCTGSCRSGKC-NH2

(Reported disulfide bonds between Cys1-Cys16, Cys8-Cys20, and Cys15-Cys25)

Reversible N-type Ca2+Channel Blocker

0.5 mg

vial

375

ENF-3787-PI Enfurirtide

Ac-YTSLIHSLIEESQNQQEKNEQELLELDK WASLWNWF-NH2

H.B. Fung and Y.Guo, Clin. Ther., 26, 352 (2004).R. Manfredi and S. Sabbatani, Curr. Med. Chem., 13, 2369 (2006).

1 mg

5 mg110

450

EPT-3786-PI Eptifibatide

[Mpa-Har-GDWP-C]-NH2

(Disulfide bridged)

Platelet Aggregation Inhibitor

J.F. Granada and N.S. Kleiman,Am. J. Cardiovasc. Drugs, 4, 31 (2004).

M.P. Curran and G.M. Keating, Biodrugs, 20, 63 (2006).

1 mg

5 mg48

150

Teriparatide - Parathyroid Hormone (Human, 1-34) PTH-4068-s: This 34 residue parathyroid hormone (PTH 1-34) hasbeen used to treat osteoporosis. This peptide is derived fromPTH-1-84. PTH 1-34 is the primary regulator of calcium andphosphate metabolism in bone and kidney. PTH increasescalcium levels by stimulating bone resorption. When usedintermittently, the effect stimulates osteoblasts more thanosteoclasts, thereby resulting in new bone formation.

Nesiritide - BNP-32 (Human),PBN-4212-v: This drug is a 32residue B-type natriuretic peptide. This peptide is normallyproduced by the ventricular myocardium. Nesiritide worksto facilitate cardiovascular fluid homeostasis through coun-

ter-regulation of the renin-angiotensin-aldoesterone system,

stimulating cyclic guanosine monophosphate, leading tosmooth muscle cell relaxation.

Ziconotide - -Conotoxin MVII-A, PCN-4289-v: This 25residue 3 disulfide peptide is a non-opioid, non-NSAIDdrug used to treat patients with chronic intractable painOriginally derived from the cone snail, Conus magus, thispeptide is a potent blocker of N-type Ca+2channels.

1. J. Lau, et al.,J. Med. Chem., 58, 7370 (2015).Retrieved from http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.5b00726

2. S.P. Marso, et al., N. Engl. J. Med., 375, 1834 (2016).Retrieved from http://www.nejm.org/doi/full/10.1056/NEJMoa1607141#t=article

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3/4

1-800-777-4779


Phone: 502-266-8787

Fax: 502-267-1329

P.O. Box 99703


PeptidesInternational, Inc.

CODE PRODUCT QTY USD

PEX-3784-PI Exendin-4 (Exenatide)

H-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2

Glucagon-Like-Peptide-1 (GLP-1) Receptor AgonistR. Gke, et al., J Biol Chem., 268, 19650 (1993).

B. Thorens, et al., Diabetes, 42, 1678 (1993).

A. Alcntara, et al.,Arch. Biochem Biophys, 341, 1, (1997).

1 mg

5 mg450

1800

LIN-3796-PI LinaclotideH-Cys-Cys-Glu-Tyr-Cys-Cys-Asn-Pro-Ala-Cys-Thr-Gly-Cys-Tyr-OH

(Disulfde bonds between Cys1-Cys6, Cys2-Cys10, Cys5-Cys13)

(M.W. 1526.76) C59

H79

N15

O21

S6[851199-59-2]

Peptide Agonist of Guanylate Cyclase 2C

W.D. Chey, et al., Am. J. Gastroenterol., 107, 1702 (2012).

S. Rao, et al., Am. J. Gastroenterol., 107, 1714 ((2012).

J.M. Johnston, et al., The Amer. J. of Gastroent., 104, 125 (2009).A.J. Lembo, et al., N. Eng. J. Med., 365, 527 (2011).

G.F. Longstreth, et al., Gastroenterology, 130, 1480 (2006).

1 mg5 mg

625

2500

PGL-3781-PI Liraglutide

Lys(-Glu-palmitoyl)26

,Arg34

-GLP-1 (7-37)

H-HAEGTFTSDVSSYLEGQAA-K(-E-palmitoyl)-EFIAWLVRGRG-OH

Glucagon-Like-Peptide-1 (GLP-1) Receptor Agonist

J.J.Neumiller, J. Am. Pharm. Assoc., 49, S16 (2009)

M.C.Rossi and A.Nicolucci,Acta Biomed., 80, 93 (2009)

C.F.Deacon, Vasc. Health Risk Manag., 5, 199 (2009)

1 mg

5 mg225

900

LIX-3799-PI Lixisenatide

H-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-

Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Ser-Lys-Lys-Lys-Lys-Lys-Lys-NH2

H-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKKK-NH2

(M.W. 4858.49) C215

H347

N61

O65

S [827033-10-3]


M. Christensen,et al.,IDrugs,12,503 (2009).

1 mg

5 mg450

1800

PCI-3738-PI OctreotidePhe-Cys-Phe-Trp-Lys-Thr-Cys-Thr-ol(Disulfide bond between Cys2-Cys7)

(M.W. 1019.24) C49H66N10O10S2 [83150-76-9]Somatostatin Analog

1 mg

5 mg70

280

PTH-4068-v Parathyroid Hormone (Human, 1-34) (Teriparatide)

H-SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNF-OH

Stimulates Bone Formation & Increases Bone Mineral Density (BMD)

0.5 mg

vial

370

GLU-3875-PI Semaglutide

H-His-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys[(AEEA)2--Glu-N-(17-carboxy-1-

oxoheptadecyl)]-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly-OH

(M.W. 4113.67) C187

H291

N45

O59

[910463-68-2]


J. Lau, et al., J. Med. Chem., 58, 7370 (2015). Retrieved from http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.5b00726

S.P. Marso, et al., N. Engl. J. Med., 375, 1834 (2016). Retrieved from http://www.nejm.org/doi/full/10.1056/NEJMoa1607141#t=article

0.5 mg

1 mg

225

325

TED-3880-PI Teduglutide

(Trifluoroacetate Form)

H-His-Gly-Asp-Gly-Ser-Phe-Ser-Asp-Glu-Met-Asn-Thr-Ile-Leu-Asp-Asn-Leu-Ala-Ala-Arg-Asp-Phe-Ile-Asn-Trp-Leu-Ile-Gln-Thr-

Lys-Ile-Thr-Asp-OH

(M.W. 3752.08) C164

H252

N44

O55

S [197922-42-2]

Glucagon-like Peptide 2 Analog Used to Treat Short Bowel Syndrome

P. Jeppesen,et al., Gut, 54, 1224 (2005).

P. Jeppesen, Therap. Adv. Gastroenterol., 5, 159 (2012).

1 mg

5 mg 4251675

Research Exemption (Generic) Peptides


4/4

1-800-777-4779


Phone: 502-266-8787

Fax: 502-267-1329

P.O. Box 99703


Peptides International, Inc.

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