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Th1156 details

Primary information
ID 1664
ThPP ID Th1156
Therapeutic Peptide/Protein Name Abarelix
Sequence N.A. view full sequnce in fasta
Functional Classification IIIc
Molecular Weight 1416.063
Chemical Formula C72H95ClN14O14
Isoelectric Point N.A.
Hydrophobicity N.A.
Melting Point (℃) N.A.
Half Life 13.2 Â± 3.2 days
Description Synthetic decapeptide antagonist to gonadotropin releasing hormone (GnRH). It is marketed by Praecis Pharmaceuticals as Plenaxis. Praecis announced in June 2006 that it was voluntarily withdrawing the drug from the market.
Indication/Disease For palliative treatment of advanced prostate cancer.
Pharmacodynamics Used in the palliative treatment of advanced prostate cancer. Abarelix is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis
Mechanism of Action Abarelix binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion
Toxicity The maximum tolerated dose of abarelix has not been determined. The maximum dose used in clinical studies was 150 mg. There have been no reports of accidental overdose with abarelix.
Metabolism In vitro hepatocyte (rat, monkey, human) studies and in vivo studies in rats and monkeys showed that the major metabolites of abarelix were formed via hydrolysis of peptide bonds. No significant oxidative or conjugated metabolites of abarelix were found either in vitro or in vivo.
Absorption Following IM administration of 100 mg, abarelix is absorbed slowly with a mean peak concentration of 43.4 ng/mL observed approximately 3 days after the injection
Volume of Distribution N.A.
Clearance N.A.
Categories Anti-Testosterone Agents
Patents Number US5968895
Date of Issue 11/12/96
Date of Expiry 11/12/13
Drug Interaction Tacrolimus, Thiothixene, Toremifene, Trimipramine, Voriconazole, Vorinostat, Ziprasidone, Zuclopenthixol- All above drugs cause Additive QTc Prolongation and increases the risk of severe ventricular arrythmias
Target Gonadotropin-releasing hormone receptor
Information of corresponding available drug in the market
Brand Name Plenaxis
Company Speciality european pharma
Brand Discription Plenaxis is a synthetic decapeptide with potent antagonistic activity against naturally occurring gonadotropin releasing-hormone (GnRH). Plenaxis inhibits gonadotropin and related androgen production by directly and competitively blocking GnRH receptors in the pituitary.
Prescribed for Plenaxis is indicated for the palliative treatment of men with advanced symptomatic prostate cancer, in whom LHRH agonist therapy is not appropriate and who refuse surgical castration, and have one or more of the following: (1) risk of neurological compromise due to metastases, (2) ureteral or bladder outlet obstruction due to local encroachment or metastatic disease, or (3) severe bone pain from skeletal metastases persisting on narcotic analgesia.
Chemical Name Abarelix is chemically described as acetyl-D-Î²-naphthylalanyl-D-4-chlorophenylalanyl- D-3-pyridylalanyl-L-seryl-L-N-methyl-tyrosyl-D-asparagyl-L-leucyl-L-N(Îµ)-isopropyllysyl- L-prolyl-D-alanyl-amide.
Formulation The single-dose vial contains 113 mg of anhydrous free base abarelix peptide (net) supplied in an abarelix CMC complex. This complex also contains 19.1 to 31 mg of CMC. After the vial is reconstituted with 2.2 mL of 0.9% sodium chloride injection
Physcial Appearance Abarelix for injectable suspension is supplied as a white to off-white sterile dry powder
Route of Administration Intramuscular Injection
Recommended Dosage The recommended dose of Plenaxis is 100 mg administered intramuscularly to the buttock on Day 1, 15, 29 (week 4) and every 4 weeks thereafter.
Contraindication Plenaxis is not indicated in women or pediatric patients. In addition, Plenaxis may cause fetal harm if administered to a pregnant woman.
Side Effects Diarrhea, Dizziness, Flushing of Skin, Headache, Constipation, Sleep Disturbance
Useful Link http://www.rxlist.com/plenaxis-drug.htm
PubMed ID 21904569
3-D Structure N.A.

Primary information
ID 1665
ThPP ID Th1156
Therapeutic Peptide/Protein Name Abarelix
Sequence N.A. view full sequnce in fasta
Functional Classification IIIc
Molecular Weight N.A.
Chemical Formula N.A.
Isoelectric Point N.A.
Hydrophobicity N.A.
Melting Point (℃) N.A.
Half Life 13.2 Â± 3.2 days
Description N.A.
Indication/Disease N.A.
Pharmacodynamics N.A.
Mechanism of Action N.A.
Toxicity N.A.
Metabolism N.A.
Absorption N.A.
Volume of Distribution N.A.
Clearance N.A.
Categories N.A.
Patents Number US6423686
Date of Issue 07/06/95
Date of Expiry 07/06/15
Drug Interaction N.A.
Target N.A.
Information of corresponding available drug in the market
Brand Name N.A.
Company N.A.
Brand Discription N.A.
Prescribed for N.A.
Chemical Name N.A.
Formulation N.A.
Physcial Appearance N.A.
Route of Administration N.A.
Recommended Dosage N.A.
Contraindication N.A.
Side Effects N.A.
Useful Link N.A.
PubMed ID 21904569
3-D Structure N.A.

OSDDlinux

Raghava's Group

IMTECH

CSIR

CRDD
CPPSITE 2.0

Primary information
ID	1664
ThPP ID	Th1156
Therapeutic Peptide/Protein Name	Abarelix
Sequence	N.A. view full sequnce in fasta
Functional Classification	IIIc
Molecular Weight	1416.063
Chemical Formula	C72H95ClN14O14
Isoelectric Point	N.A.
Hydrophobicity	N.A.
Melting Point (℃)	N.A.
Half Life	13.2 Â± 3.2 days
Description	Synthetic decapeptide antagonist to gonadotropin releasing hormone (GnRH). It is marketed by Praecis Pharmaceuticals as Plenaxis. Praecis announced in June 2006 that it was voluntarily withdrawing the drug from the market.
Indication/Disease	For palliative treatment of advanced prostate cancer.
Pharmacodynamics	Used in the palliative treatment of advanced prostate cancer. Abarelix is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis
Mechanism of Action	Abarelix binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion
Toxicity	The maximum tolerated dose of abarelix has not been determined. The maximum dose used in clinical studies was 150 mg. There have been no reports of accidental overdose with abarelix.
Metabolism	In vitro hepatocyte (rat, monkey, human) studies and in vivo studies in rats and monkeys showed that the major metabolites of abarelix were formed via hydrolysis of peptide bonds. No significant oxidative or conjugated metabolites of abarelix were found either in vitro or in vivo.
Absorption	Following IM administration of 100 mg, abarelix is absorbed slowly with a mean peak concentration of 43.4 ng/mL observed approximately 3 days after the injection
Volume of Distribution	N.A.
Clearance	N.A.
Categories	Anti-Testosterone Agents
Patents Number	US5968895
Date of Issue	11/12/96
Date of Expiry	11/12/13
Drug Interaction	Tacrolimus, Thiothixene, Toremifene, Trimipramine, Voriconazole, Vorinostat, Ziprasidone, Zuclopenthixol- All above drugs cause Additive QTc Prolongation and increases the risk of severe ventricular arrythmias
Target	Gonadotropin-releasing hormone receptor
Information of corresponding available drug in the market
Brand Name	Plenaxis
Company	Speciality european pharma
Brand Discription	Plenaxis is a synthetic decapeptide with potent antagonistic activity against naturally occurring gonadotropin releasing-hormone (GnRH). Plenaxis inhibits gonadotropin and related androgen production by directly and competitively blocking GnRH receptors in the pituitary.
Prescribed for	Plenaxis is indicated for the palliative treatment of men with advanced symptomatic prostate cancer, in whom LHRH agonist therapy is not appropriate and who refuse surgical castration, and have one or more of the following: (1) risk of neurological compromise due to metastases, (2) ureteral or bladder outlet obstruction due to local encroachment or metastatic disease, or (3) severe bone pain from skeletal metastases persisting on narcotic analgesia.
Chemical Name	Abarelix is chemically described as acetyl-D-Î²-naphthylalanyl-D-4-chlorophenylalanyl- D-3-pyridylalanyl-L-seryl-L-N-methyl-tyrosyl-D-asparagyl-L-leucyl-L-N(Îµ)-isopropyllysyl- L-prolyl-D-alanyl-amide.
Formulation	The single-dose vial contains 113 mg of anhydrous free base abarelix peptide (net) supplied in an abarelix CMC complex. This complex also contains 19.1 to 31 mg of CMC. After the vial is reconstituted with 2.2 mL of 0.9% sodium chloride injection
Physcial Appearance	Abarelix for injectable suspension is supplied as a white to off-white sterile dry powder
Route of Administration	Intramuscular Injection
Recommended Dosage	The recommended dose of Plenaxis is 100 mg administered intramuscularly to the buttock on Day 1, 15, 29 (week 4) and every 4 weeks thereafter.
Contraindication	Plenaxis is not indicated in women or pediatric patients. In addition, Plenaxis may cause fetal harm if administered to a pregnant woman.
Side Effects	Diarrhea, Dizziness, Flushing of Skin, Headache, Constipation, Sleep Disturbance
Useful Link	http://www.rxlist.com/plenaxis-drug.htm
PubMed ID	21904569
3-D Structure	N.A.

Primary information
ID	1665
ThPP ID	Th1156
Therapeutic Peptide/Protein Name	Abarelix
Sequence	N.A. view full sequnce in fasta
Functional Classification	IIIc
Molecular Weight	N.A.
Chemical Formula	N.A.
Isoelectric Point	N.A.
Hydrophobicity	N.A.
Melting Point (℃)	N.A.
Half Life	13.2 Â± 3.2 days
Description	N.A.
Indication/Disease	N.A.
Pharmacodynamics	N.A.
Mechanism of Action	N.A.
Toxicity	N.A.
Metabolism	N.A.
Absorption	N.A.
Volume of Distribution	N.A.
Clearance	N.A.
Categories	N.A.
Patents Number	US6423686
Date of Issue	07/06/95
Date of Expiry	07/06/15
Drug Interaction	N.A.
Target	N.A.
Information of corresponding available drug in the market
Brand Name	N.A.
Company	N.A.
Brand Discription	N.A.
Prescribed for	N.A.
Chemical Name	N.A.
Formulation	N.A.
Physcial Appearance	N.A.
Route of Administration	N.A.
Recommended Dosage	N.A.
Contraindication	N.A.
Side Effects	N.A.
Useful Link	N.A.
PubMed ID	21904569
3-D Structure	N.A.

Updated version of this database is available at ThpDB2

Detailed description page of THPdb