Pentamidine

Antiprotozoal — ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS

Key facts

Pentamidine is an ofp drug in the Antiprotozoal class catalogued in DrugCentral. It was first approved by the FDA in 1984. DrugCentral lists 36 molecular targets, including CHRM4, AOC1 and PTP4A2. Recorded indications include African trypanosomiasis, Pneumocystis Carinii Pneumonia Prevention and Pneumocystosis jiroveci pneumonia.

• Approval status: ofp (first approved 1984 by the FDA).
• Drug class: Antiprotozoal.
• Molecular targets: CHRM4, AOC1, PTP4A2 and PTP4A1 (36 listed in DrugCentral).
• Indications: African trypanosomiasis, Pneumocystis Carinii Pneumonia Prevention and Pneumocystosis jiroveci pneumonia.
• ATC code: P01CX01 (Other agents against leishmaniasis and trypanosomiasis).
• Molecular formula: C19H24N4O2; molecular weight 340.43 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (3)

• African trypanosomiasis
• Pneumocystis Carinii Pneumonia Prevention
• Pneumocystosis jiroveci pneumonia

Off-label uses (2)

• Cutaneous leishmaniasis
• Visceral leishmaniasis

Contraindications (20)

• Acute pancreatitis
• Anemia
• Asthma
• Conduction disorder of the heart
• Dehydration
• Diabetes mellitus
• Disease of liver
• Hyperglycemia
• Hyperkalemia
• Hypertensive disorder
• Hypocalcemia
• Hypoglycemic disorder
• Hypomagnesemia
• Kidney disease
• Leukopenia
• Liver function tests abnormal
• Low blood pressure
• Thrombocytopenic disorder
• Torsades de pointes
• Toxic nephropathy

Mechanism & targets

• Established pharmacologic class: Antiprotozoal

Molecular targets (36)

Target	Gene	Action	Activity
Muscarinic acetylcholine receptor M4	CHRM4	unknown	Ki 6.66
Amiloride-sensitive amine oxidase [copper-containing]	AOC1	unknown	Ki 6.54
Protein tyrosine phosphatase type IVA 2	PTP4A2	unknown	IC50 6.52
Protein tyrosine phosphatase type IVA 1	PTP4A1	unknown	IC50 6.52
Multidrug and toxin extrusion protein 1	SLC47A1	unknown	IC50 6.39
5-hydroxytryptamine receptor 2A	HTR2A	unknown	Ki 6.33
Alpha-1D adrenergic receptor	ADRA1D	unknown	Ki 6.31
Muscarinic acetylcholine receptor M2	CHRM2	unknown	Ki 6.29
Alpha-2A adrenergic receptor	ADRA2A	unknown	Ki 6.29
Alpha-1B adrenergic receptor	Adra1b	unknown	Ki 6.27
Glutamate NMDA receptor; GRIN1/GRIN2A	GRIN1|GRIN2A	unknown	IC50 6.14
Amine oxidase [flavin-containing] A	MAOA	unknown	IC50 6.10
Protein S100-B	S100B	unknown	Kd 6.00
Suppressor of tumorigenicity 14 protein	ST14	unknown	Ki 5.94
Transmembrane protease serine 2	TMPRSS2	unknown	IC50 5.92
Solute carrier family 22 member 2	SLC22A2	unknown	IC50 5.92
Alpha-1A adrenergic receptor	Adra1a	unknown	IC50 5.92
Glutamate NMDA receptor	Grin1|Grin2a|Grin2b|Grin2c|Grin2d|Grin3b|Grin3a	unknown	IC50 5.88
D(3) dopamine receptor	DRD3	unknown	Ki 5.87
5-hydroxytryptamine receptor 2C	HTR2C	unknown	Ki 5.76

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1984-10-16	FDA	—	FRESENIUS KABI USA	Yes

ATC classification

ATC code	Therapeutic hierarchy
P01CX01	ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS › ANTIPROTOZOALS › AGENTS AGAINST LEISHMANIASIS AND TRYPANOSOMIASIS › Other agents against leishmaniasis and trypanosomiasis

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Aplastic anaemia	323.4
Pneumocystis jirovecii pneumonia	309.9
Nocardiosis	305.9
Febrile neutropenia	296.0
Toxoplasmosis	293.4
Mucosal inflammation	249.2
Neutropenia	235.0
Graft versus host disease	167.9
Febrile bone marrow aplasia	149.8
Respiratory failure	142.9
Cytokine release syndrome	141.5
Cerebral toxoplasmosis	140.9

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Pentamidine is on its molecule page.

• Molecular formula: C₁₉H₂₄N₄O₂
• Molecular weight: 340.43 g/mol
• CAS number: —
• InChIKey: XDRYMKDFEDOLFX-UHFFFAOYSA-N
• PubChem CID: 4735

NC(=N)C1=CC=C(OCCCCCOC2=CC=C(C=C2)C(N)=N)C=C1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Pentamidine used for?

DrugCentral lists the following indications for Pentamidine: African trypanosomiasis, Pneumocystis Carinii Pneumonia Prevention and Pneumocystosis jiroveci pneumonia.

How does Pentamidine work?

Its molecular targets in DrugCentral include CHRM4, AOC1, PTP4A2 and PTP4A1.

When was Pentamidine first approved?

Pentamidine was first approved by the FDA in 1984.

What drug class does Pentamidine belong to?

Pentamidine is in the Antiprotozoal class.

What is the chemical formula of Pentamidine?

Pentamidine has the molecular formula C19H24N4O2 and a molecular weight of 340.43 g/mol.

Sources

• DrugCentral drug card 2090 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL361506 — compound record and bioactivity
• PubChem CID 4735 — chemical identifiers
• DrugBank DB00738 — drug record
• FDA UNII 673LC5J4LQ — substance identity
• DailyMed: FDA labels for Pentamidine — current prescribing information (label search)
• UniProt P08173 (CHRM4) — target protein
• UniProt P19801 (AOC1) — target protein
• UniProt Q12974 (PTP4A2) — target protein
• UniProt Q93096 (PTP4A1) — target protein
• UniProt Q96FL8 (SLC47A1) — target protein
• UniProt P28223 (HTR2A) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.