Description

Simple

Clinical

Overview

Calanolide A is a new non-nucleoside reverse transcriptase inhibitor (NNRTI) derived from a plant found in the Malaysian rain forest. A related compound, calanolide B, also has anti-HIV activity. Both drugs are being developed by Sarawak Pharmaceuticals. A preliminary dosing study among HIV-infected individuals showed a significant antiviral effect compared with placebo.

Pharmacology

Indication

For use in combination treatment of HIV infection (AIDS).

Pharmacodynamic

Calanolide A is a new non-nucleoside reverse transcriptase inhibitor (NNRTI) derived from a plant found in the Malaysian rain forest. A related compound, calanolide B, also has anti-HIV activity. Both drugs are being developed by Sarawak Pharmaceuticals. The drug is metabolised by cytochrome P450 CY... Read more

Mechanism of action

Viral life-cycle studies indicate that calanolide A acts early in the infection process, similar to the known HIV reverse transcriptase (RT) inhibitor 2', 3'-dideoxycytidine. In enzyme inhibition assays, calanolide A potently and selectively inhibits recombinant HIV type 1 RT but not cellular DNA po... Read more

Absorption

Information currently not available.

Protein binding

Information currently not available.

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

20 hours for 800mg

Route of elimination

Information currently not available.

Toxicity

Information currently not available.

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
Acetohexamide
The therapeutic efficacy of Acetohexamide can be increased when used in combination with Calanolide A.
Adenovirus type 7 vaccine live
The therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Calanolide A.
Anthrax vaccine
The therapeutic efficacy of Anthrax vaccine can be decreased when used in combination with Calanolide A.
Bacillus calmette-guerin substrain connaught live antigen
The therapeutic efficacy of Bacillus calmette-guerin substrain connaught live antigen can be decreased when used in combination with Calanolide A.
Bacillus calmette-guerin substrain danish 1331 live antigen
The therapeutic efficacy of Bacillus calmette-guerin substrain danish 1331 live antigen can be decreased when used in combination with Calanolide A.
Bacillus calmette-guerin substrain tice live antigen
The therapeutic efficacy of Bacillus calmette-guerin substrain tice live antigen can be decreased when used in combination with Calanolide A.
BCG vaccine
The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Calanolide A.
Carbutamide
The therapeutic efficacy of Carbutamide can be increased when used in combination with Calanolide A.
Chlorpropamide
The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Calanolide A.
Dexmethylphenidate
The serum concentration of the active metabolites of Calanolide A can be increased when Calanolide A is used in combination with Dexmethylphenidate.
Glibornuride
The therapeutic efficacy of Glibornuride can be increased when used in combination with Calanolide A.
Gliclazide
The therapeutic efficacy of Gliclazide can be increased when used in combination with Calanolide A.
Glimepiride
The therapeutic efficacy of Glimepiride can be increased when used in combination with Calanolide A.
Glipizide
The therapeutic efficacy of Glipizide can be increased when used in combination with Calanolide A.
Gliquidone
The therapeutic efficacy of Gliquidone can be increased when used in combination with Calanolide A.
Glisoxepide
The therapeutic efficacy of Glisoxepide can be increased when used in combination with Calanolide A.
Glyburide
The therapeutic efficacy of Glyburide can be increased when used in combination with Calanolide A.
Human adenovirus e serotype 4 strain cl-68578 antigen
The therapeutic efficacy of Human adenovirus e serotype 4 strain cl-68578 antigen can be decreased when used in combination with Calanolide A.
Metahexamide
The therapeutic efficacy of Metahexamide can be increased when used in combination with Calanolide A.
Rubella virus vaccine
The therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Calanolide A.
3 References
  1. 1 . Eiznhamer DA, Creagh T, Ruckle JL, Tolbert DT, Giltner J, Dutta B, Flavin MT, Jenta T, Xu ZQ: Safety and pharmacokinetic profile of multiple escalating doses of (+)-calanolide A, a naturally occurring nonnucleoside reverse transcriptase inhibitor, in healthy HIV-negative volunteers. HIV Clin Trials. 2002 Nov-Dec;3(6):435-50.PubMed: 12501127
  2. 2 . Xu ZQ, Barrow WW, Suling WJ, Westbrook L, Barrow E, Lin YM, Flavin MT: Anti-HIV natural product (+)-calanolide A is active against both drug-susceptible and drug-resistant strains of Mycobacterium tuberculosis. Bioorg Med Chem. 2004 Mar 1;12(5):1199-207.PubMed: 14980631
  3. 3 . Sekino E, Kumamoto T, Tanaka T, Ikeda T, Ishikawa T: Concise synthesis of anti-HIV-1 active (+)-inophyllum B and (+)-calanolide A by application of (-)-quinine-catalyzed intramolecular oxo-Michael addition. J Org Chem. 2004 Apr 16;69(8):2760-7.PubMed: 15074925