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treprostinil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
prostaglandins	2720	81846-19-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: treprost treprostinil uniprost treprostinil sodium 15AU81 LRX-15 UT-15 treprostinil diolamine	Treprostinil is a prostacyclin analogue. The major pharmacologic actions of treprostinil are direct vasodilation of pulmonary and systemic arterial vascular beds and inhibition of platelet aggregation. Molecular weight: 390.52 Formula: C23H34O5 CLOGP: 3.72 LIPINSKI: 0 HAC: 5 HDO: 3 TPSA: 86.99 ALOGS: -4.73 ROTB: 10 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

treprost
treprostinil
uniprost
treprostinil sodium
15AU81
LRX-15
UT-15
treprostinil diolamine

Treprostinil is a prostacyclin analogue. The major pharmacologic actions of treprostinil are direct vasodilation of pulmonary and systemic arterial vascular beds and inhibition of platelet aggregation.

Molecular weight: 390.52
Formula: C23H34O5
CLOGP: 3.72
LIPINSKI: 0
HAC: 5
HDO: 3
TPSA: 86.99
ALOGS: -4.73
ROTB: 10

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
4.30	mg	P

ADMET properties:

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Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	6.15 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	4 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	10.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	0.82 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.23 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.09 %	Lombardo F, Berellini G, Obach RS

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Approvals:

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Date	Agency	Company
April 3, 2020	EMA	SciPharm Sarl
Dec. 23, 2022	PMDA	Mochida Pharmaceutical Co., Ltd.
May 21, 2002	FDA	UNITED THERAP

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FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Dyspnoea	3214.76	17.21	4989	115360	656324	62712349
Infusion site pain	2705.02	17.21	1065	119284	15804	63352869
Fluid retention	2099.08	17.21	1343	119006	58343	63310330
Pulmonary arterial hypertension	1670.36	17.21	828	119521	21749	63346924
Headache	1625.84	17.21	3642	116707	629599	62739074
Hypervolaemia	1546.00	17.21	848	119501	27565	63341108
Right ventricular failure	1543.32	17.21	720	119629	16468	63352205
Pain in jaw	1379.74	17.21	918	119431	42578	63326095
Infusion site erythema	1373.62	17.21	591	119758	11088	63357585
Pulmonary hypertension	1323.20	17.21	843	119506	36280	63332393

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Dyspnoea	1060.03	23.10	1584	34195	375198	34545954
Infusion site pain	1004.83	23.10	300	35479	3551	34917601
Fluid retention	770.80	23.10	426	35353	26461	34894691
Right ventricular failure	665.38	23.10	272	35507	8512	34912640
Headache	661.64	23.10	913	34866	199722	34721430
Pulmonary arterial hypertension	639.47	23.10	264	35515	8475	34912677
Pulmonary hypertension	584.34	23.10	326	35453	20598	34900554
Hypervolaemia	558.35	23.10	310	35469	19399	34901753
Pain in jaw	550.18	23.10	268	35511	12772	34908380
Infusion site erythema	490.12	23.10	153	35626	2120	34919032

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Dyspnoea	3410.05	17.50	5406	123309	851619	78764054
Infusion site pain	2758.68	17.50	988	127727	13188	79602485
Fluid retention	2563.18	17.50	1523	127192	68286	79547387
Pulmonary arterial hypertension	2080.72	17.50	983	127732	27383	79588290
Hypervolaemia	1849.95	17.50	1038	127677	41652	79574021
Right ventricular failure	1849.24	17.50	855	127860	22642	79593031
Headache	1794.79	17.50	3516	125199	650256	78965417
Pulmonary hypertension	1603.80	17.50	987	127728	47093	79568580
Pain in jaw	1540.86	17.50	948	127767	45203	79570470
Infusion site erythema	1430.45	17.50	548	128167	8912	79606761

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	B01AC21	BLOOD AND BLOOD FORMING ORGANS ANTITHROMBOTIC AGENTS ANTITHROMBOTIC AGENTS Platelet aggregation inhibitors excl. heparin
CHEBI has role	CHEBI:35554	cardiovascular agent
CHEBI has role	CHEBI:35620	vasodilator agents
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:50427	platelet aggregation inhibitors
CHEBI has role	CHEBI:55347	vitamin K antagonists
CHEBI has role	CHEBI:85234	human blood serum metabolites
FDA CS	M0017817	Prostaglandins I
FDA EPC	N0000175416	Prostacycline Vasodilator
FDA PE	N0000009909	Vasodilation

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Pulmonary arterial hypertension	indication	11399002
Thromboembolic pulmonary hypertension	indication	233947005
Disorder of lung	contraindication	19829001	DOID:850
Low blood pressure	contraindication	45007003
Blood coagulation disorder	contraindication	64779008	DOID:1247
Kidney disease	contraindication	90708001	DOID:557
Disease of liver	contraindication	235856003	DOID:409

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.4	acidic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
0.016MG/INH	TYVASO DPI	UNITED THERAP	N214324	May 23, 2022	RX	POWDER	INHALATION	10716793	May 14, 2027	METHOD OF TREATING PULMONARY HYPERTENSION BY ADMINISTERING TREPROSTINIL OR A SALT THEREOF BY INHALATION USING A DEVICE
0.032MG/INH	TYVASO DPI	UNITED THERAP	N214324	May 23, 2022	RX	POWDER	INHALATION	10716793	May 14, 2027	METHOD OF TREATING PULMONARY HYPERTENSION BY ADMINISTERING TREPROSTINIL OR A SALT THEREOF BY INHALATION USING A DEVICE
0.048MG/INH	TYVASO DPI	UNITED THERAP	N214324	May 23, 2022	RX	POWDER	INHALATION	10716793	May 14, 2027	METHOD OF TREATING PULMONARY HYPERTENSION BY ADMINISTERING TREPROSTINIL OR A SALT THEREOF BY INHALATION USING A DEVICE
0.064MG/INH	TYVASO DPI	UNITED THERAP	N214324	May 23, 2022	RX	POWDER	INHALATION	10716793	May 14, 2027	METHOD OF TREATING PULMONARY HYPERTENSION BY ADMINISTERING TREPROSTINIL OR A SALT THEREOF BY INHALATION USING A DEVICE
0.6MG/ML	TYVASO	UNITED THERAP	N022387	July 30, 2009	RX	SOLUTION	INHALATION	10376525	May 14, 2027	METHOD OF TREATING PULMONARY HYPERTENSION BY ADMINISTERING TREPROSTINIL OR A SALT THEREOF BY INHALATION USING A DEVICE
0.6MG/ML	TYVASO	UNITED THERAP	N022387	July 30, 2009	RX	SOLUTION	INHALATION	10716793	May 14, 2027	METHOD OF TREATING PULMONARY HYPERTENSION BY ADMINISTERING TREPROSTINIL OR A SALT THEREOF BY INHALATION USING A DEVICE
0.6MG/ML	TYVASO	UNITED THERAP	N022387	July 30, 2009	RX	SOLUTION	INHALATION	9358240	May 5, 2028	METHOD OF TREATING PULMONARY HYPERTENSION BY ADMINISTERING TREPROSTINIL OR A SALT THEREOF BY INHALATION USING A DEVICE
100MG/20ML (5MG/ML)	REMODULIN	UNITED THERAP	N208276	July 30, 2018	DISCN	SOLUTION	INTRAVENOUS, SUBCUTANEOUS	9713599	Dec. 16, 2024	A METHOD OF TREATING PULMONARY HYPERTENSION COMPRISING PARENTERALLY ADMINISTERING A FORMULATION COMPRISING A) 0.1 TO 5% W/V OF TREPROSTINIL OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF AND B) A CITRATE BUFFER
10MG/ML	REMODULIN	UNITED THERAP	N021272	May 21, 2002	RX	INJECTABLE	IV (INFUSION), SUBCUTANEOUS	9199908	May 24, 2024	ADMINISTRATION OF REMODULIN DILUTED FOR INTRAVENOUS INFUSION WITH STERILE WATER FOR INJECTION OR 0.9% SODIUM CHLORIDE INJECTION PRIOR TO ADMINISTRATION
10MG/ML	REMODULIN	UNITED THERAP	N021272	May 21, 2002	RX	INJECTABLE	IV (INFUSION), SUBCUTANEOUS	10695308	Dec. 16, 2024	A METHOD OF TREATING A HUMAN PATIENT SUFFERING FROM PULMONARY HYPERTENSION

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
0.6MG/ML	TYVASO	UNITED THERAP	N022387	July 30, 2009	RX	SOLUTION	INHALATION	March 31, 2024	INDICATION FOR THE TREATMENT OF PULMONARY HYPERTENSION ASSOCIATED WITH INTERSTITIAL LUNG DISEASE TO IMPROVE EXERCISE ABILITY
EQ 0.125MG BASE	ORENITRAM	UNITED THERAP	N203496	Dec. 20, 2013	RX	TABLET, EXTENDED RELEASE	ORAL	Oct. 18, 2026	INDICATED FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION (PAH) (WHO GROUP 1) TO DELAY DISEASE PROGRESSION
EQ 0.25MG BASE	ORENITRAM	UNITED THERAP	N203496	Dec. 20, 2013	RX	TABLET, EXTENDED RELEASE	ORAL	Oct. 18, 2026	INDICATED FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION (PAH) (WHO GROUP 1) TO DELAY DISEASE PROGRESSION
EQ 1MG BASE	ORENITRAM	UNITED THERAP	N203496	Dec. 20, 2013	RX	TABLET, EXTENDED RELEASE	ORAL	Oct. 18, 2026	INDICATED FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION (PAH) (WHO GROUP 1) TO DELAY DISEASE PROGRESSION
EQ 2.5MG BASE	ORENITRAM	UNITED THERAP	N203496	Dec. 20, 2013	RX	TABLET, EXTENDED RELEASE	ORAL	Oct. 18, 2026	INDICATED FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION (PAH) (WHO GROUP 1) TO DELAY DISEASE PROGRESSION
EQ 5MG BASE	ORENITRAM	UNITED THERAP	N203496	Oct. 7, 2016	RX	TABLET, EXTENDED RELEASE	ORAL	Oct. 18, 2026	INDICATED FOR THE TREATMENT OF PULMONARY ARTERIAL HYPERTENSION (PAH) (WHO GROUP 1) TO DELAY DISEASE PROGRESSION

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Prostacyclin receptor	GPCR	P43119	PI2R_HUMAN	AGONIST	EC50	8.72	IUPHAR	CHEMBL
Prostaglandin E2 receptor EP1 subtype	GPCR	P34995	PE2R1_HUMAN	AGONIST	Ki	6.70	IUPHAR
Prostaglandin E2 receptor EP3 subtype	GPCR	P43115	PE2R3_HUMAN	AGONIST	Ki	5.60	IUPHAR
Prostaglandin E2 receptor EP2 subtype	GPCR	P43116	PE2R2_HUMAN	AGONIST	Ki	8.40	IUPHAR
Prostaglandin E2 receptor EP4 subtype	GPCR	P35408	PE2R4_HUMAN	AGONIST	EC50	6.70	IUPHAR
Prostaglandin D2 receptor	GPCR	Q13258	PD2R_HUMAN	AGONIST	Ki	8.40	IUPHAR

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External reference:

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ID	Source
009648	NDDF
009649	NDDF
015333	NDDF
16706	MMSL
1927409	RXNORM
26646	MMSL
289480-64-4	SECONDARY_CAS_RN
30181	MMSL
385681001	SNOMEDCT_US
385682008	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Treprostinil	HUMAN PRESCRIPTION DRUG LABEL	1	0703-0666	INJECTION, SOLUTION	20 mg	INTRAVENOUS	ANDA	26 sections
Treprostinil	HUMAN PRESCRIPTION DRUG LABEL	1	0703-0666	INJECTION, SOLUTION	20 mg	INTRAVENOUS	ANDA	26 sections
Treprostinil	HUMAN PRESCRIPTION DRUG LABEL	1	0703-0676	INJECTION, SOLUTION	50 mg	INTRAVENOUS	ANDA	26 sections
Treprostinil	HUMAN PRESCRIPTION DRUG LABEL	1	0703-0676	INJECTION, SOLUTION	50 mg	INTRAVENOUS	ANDA	26 sections
Treprostinil	HUMAN PRESCRIPTION DRUG LABEL	1	0703-0686	INJECTION, SOLUTION	100 mg	INTRAVENOUS	ANDA	26 sections
Treprostinil	HUMAN PRESCRIPTION DRUG LABEL	1	0703-0686	INJECTION, SOLUTION	100 mg	INTRAVENOUS	ANDA	26 sections
Treprostinil	HUMAN PRESCRIPTION DRUG LABEL	1	0703-0696	INJECTION, SOLUTION	200 mg	INTRAVENOUS	ANDA	26 sections
Treprostinil	HUMAN PRESCRIPTION DRUG LABEL	1	0703-0696	INJECTION, SOLUTION	200 mg	INTRAVENOUS	ANDA	26 sections
Treprostinil	HUMAN PRESCRIPTION DRUG LABEL	1	0781-3420	INJECTION	20 mg	SUBCUTANEOUS	ANDA	26 sections
Treprostinil	HUMAN PRESCRIPTION DRUG LABEL	1	0781-3420	INJECTION	20 mg	SUBCUTANEOUS	ANDA	26 sections

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