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Doravirine

Class: HIV Nonnucleoside Reverse Transcriptase Inhibitors
Chemical Name: 3-chloro-5-[1-[(4-methyl-5-oxo-1H-1,2,4-triazol-3-yl)methyl]-2-oxo-4-(trifluoromethyl)pyridin-3-yl]oxybenzonitrile
Molecular Formula: C17H11ClF3N5O3
CAS Number: 1338225-97-0
Brands: Pifeltro

Medically reviewed by Drugs.com on Mar 30, 2020. Written by ASHP.

Introduction

Antiretroviral; HIV nonnucleoside reverse transcriptase inhibitor (NNRTI).

Uses for Doravirine

Treatment of HIV Infection

Treatment of HIV-1 infection in antiretroviral-naive (have not previously received antiretroviral therapy) or antiretroviral-experienced (previously treated) adults.

Single-entity doravirine (Pifeltro) usually used in NNRTI-based regimens that include doravirine and 2 HIV nucleoside reverse transcriptase inhibitors (dual NRTIs).

If an NNRTI-based regimen of doravirine, lamivudine, and tenofovir disoproxil fumarate (tenofovir DF) is used for treatment of HIV-1 infection in adults, a fixed-combination preparation containing all 3 drugs (Delstrigo; doravirine/lamivudine/tenofovir DF) is commercially available and can be used alone as a complete regimen for treatment of HIV-1 infection.

For initial treatment in antiretroviral-naive adults, experts state that doravirine in conjunction with a dual NRTI consisting of emtricitabine and either tenofovir alafenamide fumarate (TAF) or tenofovir DF are recommended NNRTI-based regimens in certain clinical situations.

For antiretroviral-experienced adults, manufacturer states that doravirine in conjunction with other antiretrovirals can be used to replace the current antiretroviral regimen in those with plasma HIV-1 RNA levels <50 copies/mL on a stable antiretroviral regimen who have no history of treatment failure and are infected with HIV-1 with no known substitutions associated with resistance to doravirine.

Most appropriate antiretroviral regimen cannot be defined for every clinical scenario; select regimen based on information regarding antiretroviral potency, potential rate of resistance development, known toxicities, potential for pharmacokinetic interactions, and patient's virologic, immunologic, and clinical characteristics. Guidelines for the management of HIV infection, including specific recommendations for initial treatment in antiretroviral-naive patients and recommendations for changing antiretroviral regimens, are available at [Web].

Doravirine Dosage and Administration

Administration

Oral Administration

Administer orally once daily without regard to food.

Must use single-entity doravirine in conjunction with other antiretrovirals.

Dosage

Adults

Treatment of HIV Infection
Antiretroviral-naive or Antiretroviral-experienced Adults
Oral

100 mg once daily.

Antiretroviral-naive or Antiretroviral-experienced Adults Receiving Rifabutin
Oral

100 mg twice daily (give doses approximately 12 hours apart). (See Specific Drugs under Interactions.)

Special Populations

Hepatic Impairment

Mild or moderate hepatic impairment (Child-Pugh class A or B): Dosage adjustments not needed.

Severe hepatic impairment (Child-Pugh class C): Not studied. (See Hepatic Impairment under Cautions.)

Renal Impairment

Mild, moderate, or severe renal impairment: Dosage adjustments not needed.

Not adequately studied in patients with end-stage renal disease; not studied in those receiving dialysis. (See Renal Impairment under Cautions.)

Geriatric Patients

No specific dosage recommendations; use with caution because of possible age-related decreases in hepatic, renal, and/or cardiac function and potential for concomitant disease and drug therapy. (See Geriatric Use under Cautions.)

Cautions for Doravirine

Contraindications

  • Concomitant use with potent CYP3A inducers (e.g., carbamazepine, oxcarbazepine, phenobarbital, phenytoin, enzalutamide, rifampin, rifapentine, mitotane, St. John’s wort [Hypericum perforatum]). (See Interactions under Cautions.)

Warnings/Precautions

Interactions

Concomitant use with certain drugs may result in known or potentially clinically important drug interactions, some of which may lead to loss of therapeutic effect of doravirine and possible development of resistance.

Consider potential for drug interactions prior to and during doravirine therapy; review concomitant drugs during doravirine therapy and monitor for adverse effects. (See Interactions.)

Immune Reconstitution Syndrome

Immune reconstitution syndrome has been reported in HIV-infected patients receiving multiple-drug antiretroviral therapy. During the initial phase of treatment, HIV-infected patients whose immune systems respond to antiretroviral therapy may develop an inflammatory response to indolent or residual opportunistic infections (e.g., Mycobacterium avium, cytomegalovirus [CMV], Pneumocystis jirovecii [formerly P. carinii], tuberculosis); such responses may necessitate further evaluation and treatment.

Autoimmune disorders (e.g., Graves' disease, polymyositis, Guillain-Barré syndrome, autoimmune hepatitis) also reported in the setting of immune reconstitution; however, time to onset is more variable and can occur many months after initiation of antiretroviral therapy.

Specific Populations

Pregnancy

Antiretroviral Pregnancy Registry at 800-258-4263 or [Web].

Human data not available to establish whether or not doravirine poses a risk to pregnancy outcomes.

In animal reproduction studies, no adverse developmental effects observed in rabbits or rats at exposures 8 or 9 times higher, respectively, than human exposure at recommended human dosage. In pregnant rabbits and rats, doravirine crossed the placenta resulting in fetal plasma concentrations up to 40 and 52%, respectively, of maternal concentrations observed on gestation day 20.

Pharmacokinetics of doravirine not studied in pregnant women.

Lactation

Not known whether doravirine distributes into human milk, affects human milk production, or affects the breast-fed infant.

Distributed into milk of lactating rats following oral administration (milk concentrations approximately 1.5 times higher than maternal plasma concentrations at 2 hours after a dose on lactation day 14).

Instruct HIV-infected women not to breast-feed because of risk of HIV transmission and risk of adverse effects in the infant.

Pediatric Use

Safety and efficacy not established in pediatric patients <18 years of age.

Geriatric Use

Experience in patients ≥65 years of age insufficient to determine whether they respond differently than younger adults.

Use with caution in geriatric patients because of age-related decreases in hepatic, renal, and/or cardiac function and potential for concomitant disease and drug therapy.

Hepatic Impairment

No clinically important differences in doravirine pharmacokinetics in patients with moderate hepatic impairment (Child-Pugh class B); dosage adjustments not needed in those with mild or moderate hepatic impairment (Child-Pugh class A or B).

Not studied in patients with severe hepatic impairment (Child-Pugh class C).

Renal Impairment

Based on population pharmacokinetic analysis, renal function does not have a clinically important effect on doravirine pharmacokinetics; dosage adjustments not needed in those with mild, moderate, or severe renal impairment.

Not adequately studied in patients with end-stage renal disease; not studied in those receiving dialysis.

Common Adverse Effects

Nausea, dizziness, headache, fatigue, diarrhea, abdominal pain, abnormal dreams, insomnia, rash, increased bilirubin concentrations.

Interactions for Doravirine

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Primarily metabolized by CYP3A. In vitro, does not inhibit CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, or 3A4; not likely to induce CYP1A2, 2B6, or 3A4.

Concomitant use with CYP3A inducers may decrease doravirine plasma concentrations and may reduce efficacy of doravirine. Concomitant use with CYP3A inhibitors may increase doravirine concentrations.

Not likely to have a clinically important effect on exposures of drugs metabolized by CYP isoenzymes.

Drugs Affecting or Metabolized by UGT

In vitro, does not inhibit UGT1A1.

Drugs Affecting or Affected by Other Transporters

Based on in vitro studies, not likely to inhibit P-glycoprotein (P-gp) transport system, organic anion transport polypeptide (OATP) 1B1, OATP1B3, bile salt export pump (BSEP), organic anion transporter (OAT) 1, OAT3, organic cation transporter (OCT) 2, multidrug and toxin extrusion transporter (MATE) 1, or MATE2K.

Not a substrate of breast cancer resistance protein (BCRP); unlikely to be a substrate of OATP1B1 or 1B3.

Specific Drugs

Drug

Interaction

Comments

Abacavir

No in vitro evidence of antagonistic antiretroviral effects

α1-Adrenergic blocking agents

Alfuzosin, doxazosin, silodosin, tamsulosin: No effect on α1-adrenergic blocking agent concentrations expected

Dosage adjustments not needed

Antacids

Antacid containing aluminum hydroxide, magnesium hydroxide, and simethicone: No clinically important effect on doravirine concentrations

Dosage adjustments not needed

Anticoagulants

Apixaban, betrixaban, dabigatran, edoxaban, rivaroxaban: No effect on anticoagulant concentrations expected

Warfarin: No effect on warfarin concentrations expected

Apixaban, betrixaban, dabigatran, edoxaban, rivaroxaban: Dosage adjustments not needed

Warfarin: Dosage adjustments not needed

Anticonvulsants

Carbamazepine, oxcarbazepine, phenobarbital, phenytoin: Decreased doravirine concentrations expected; possible decreased doravirine efficacy

Eslicarbazepine: Possible decreased doravirine concentrations

Ethosuximide, lacosamide, lamotrigine, tiagabine, zonisamide: No effect on anticonvulsant concentrations expected

Carbamazepine, oxcarbazepine, phenobarbital, phenytoin: Concomitant use contraindicated; do not initiate doravirine until ≥4 weeks after anticonvulsant discontinued; experts state consider alternative anticonvulsant

Eslicarbazepine: If used concomitantly, experts state monitor virologic outcomes and consider monitoring doravirine plasma concentrations; alternatively, consider different antiretroviral or anticonvulsant

Ethosuximide, lacosamide, lamotrigine, tiagabine, zonisamide: Dosage adjustments not needed

Antidiabetic agents

Canagliflozin, dapagliflozin, empagliflozin: No effect on antidiabetic agent concentrations expected

Linagliptin, saxagliptin, sitagliptin: No effect on antidiabetic agent concentrations expected

Metformin: No clinically important effect on metformin concentrations; possible decreased doravirine concentrations and AUC

Canagliflozin, dapagliflozin, empagliflozin: Dosage adjustments not needed

Linagliptin, saxagliptin, sitagliptin: Dosage adjustments not needed

Metformin: Dosage adjustments not needed

Antifungals, azoles

Fluconazole, isavuconazonium sulfate [prodrug of isavuconazole], itraconazole, voriconazole: Possible increased doravirine concentrations

Ketoconazole: Increased doravirine exposures and peak plasma concentrations; not considered clinically important

Posaconazole: Possible increased doravirine concentrations

Fluconazole, isavuconazonium sulfate, itraconazole, voriconazole: Dosage adjustments not needed

Posaconazole: Experts state monitor for doravirine-associated toxicities

Antimalarial and antiprotozoal agents

Atovaquone: Data not available

Fixed combination of artemether and lumefantrine (artemether/lumefantrine): No effect on antimalarial agent concentrations expected

Fixed combination of atovaquone and proguanil (atovaquone/proguanil): Data not available

Atovaquone: Experts recommend monitoring for antiprotozoal efficacy

Artemether/lumefantrine: Dosage adjustments not needed

Atovaquone/proguanil: Experts recommend monitoring for antimalarial efficacy

Antimycobacterials (bedaquiline, rifamycins)

Bedaquiline: No effect on bedaquiline concentrations expected

Rifabutin: Decreased doravirine AUC and trough plasma concentrations; peak plasma concentrations not affected

Rifampin: Decreased doravirine AUC, peak plasma concentrations, and trough plasma concentrations; possible decreased doravirine efficacy

Rifapentine: Decreased doravirine concentrations expected; possible decreased efficacy of doravirine

Bedaquiline: Dosage adjustments not needed

Rifabutin: Increase dosage of doravirine to 100 mg twice daily

Rifampin, rifapentine: Concomitant use contraindicated; do not initiate doravirine until ≥4 weeks after rifampin or rifapentine discontinued

Antiplatelet agents

Ticagrelor, vorapaxar: No effect on antiplatelet agent concentrations expected

Ticagrelor, vorapaxar: Dosage adjustments not needed

Antipsychotic agents

Aripiprazole, brexpiprazole, cariprazine, lurasidone, pimavanserin, pimozide, quetiapine: No effect on antipsychotic agent concentrations expected

Aripiprazole, brexpiprazole, cariprazine, lurasidone, pimavanserin, pimozide, quetiapine: Dosage adjustments not needed

Atazanavir

Cobicistat-boosted, ritonavir-boosted, or unboosted atazanavir: Increased doravirine concentrations expected; not expected to affect atazanavir concentrations

Cobicistat-boosted, ritonavir-boosted, or unboosted atazanavir: Dosage adjustments not needed

Benzodiazepines

Alprazolam, diazepam, lorazepam, triazolam: No effect on benzodiazepine concentrations expected

Midazolam: No clinically important pharmacokinetic interactions

Alprazolam, diazepam, lorazepam, midazolam, triazolam: Dosage adjustments not needed

Bictegravir

No clinically important effect on pharmacokinetics of either drug expected

Dosage adjustments not needed

Buprenorphine

Buprenorphine (buccal, sublingual, subdermal implant): No effect on buprenorphine concentrations expected

Buprenorphine (buccal, sublingual, subdermal implant): Dosage adjustments not needed

Bupropion

No effect on bupropion concentrations expected

Dosage adjustments not needed

Calcium-channel blocking agents

Dihydropyridine calcium-channel blocking agents: No effect on concentrations of these calcium-channel blocking agents expected

Diltiazem, verapamil: Possible increased doravirine concentrations; no effect on diltiazem or verapamil concentrations expected

Dihydropyridine calcium-channel blocking agents, diltiazem, verapamil: Dosage adjustments not needed

Darunavir

Cobicistat-boosted or ritonavir-boosted darunavir: Increased doravirine concentrations expected; not expected to affect darunavir concentrations

No in vitro evidence of antagonistic antiretroviral effects

Cobicistat-boosted or ritonavir-boosted darunavir: Dosage adjustments not needed

Dasabuvir

Dasabuvir used with the fixed combination of ombitasvir, paritaprevir, and ritonavir (ombitasvir/paritaprevir/ritonavir): Possible increased doravirine concentrations

Dasabuvir used with ombitasvir/paritaprevir/ritonavir: Dosage adjustments not needed

Delavirdine

No in vitro evidence of antagonistic antiretroviral effects

Dexamethasone

Possible decreased doravirine concentrations

Experts state consider alternative corticosteroid for long-term use in patients receiving doravirine; if used concomitantly, monitor virologic response

Didanosine

No in vitro evidence of antagonistic antiretroviral effects

Dolutegravir

Increased dolutegravir AUC, peak plasma concentrations, and trough plasma concentrations; not considered clinically important

No effect on doravirine concentrations

Dosage adjustments not needed

Dutasteride

Pharmacokinetic interactions not expected

Efavirenz

On day 1 of doravirine therapy (and after discontinuance of efavirenz), doravirine exposures and peak plasma concentrations decreased by 62 and 35%, respectively; on day 14 of doravirine therapy (and after discontinuance of efavirenz), doravirine exposures and peak plasma concentrations decreased by 32 and 14%, respectively

No in vitro evidence of antagonistic antiretroviral effects

Concomitant use not recommended

Elbasvir and grazoprevir

Elbasvir and grazoprevir: No clinically important pharmacokinetic interactions

Fixed combination of elbasvir and grazoprevir (elbasvir/grazoprevir): Dosage adjustments not needed

Elvitegravir

Cobicistat-boosted elvitegravir: Increased doravirine concentrations expected; no effect on elvitegravir concentrations expected

Cobicistat-boosted elvitegravir: Dosage adjustments not needed

Emtricitabine

No in vitro evidence of antagonistic antiretroviral effects

Enfuvirtide

No in vitro evidence of antagonistic antiretroviral effects

Enzalutamide

Decreased doravirine concentrations expected; possible decreased doravirine efficacy

Concomitant use contraindicated; do not initiate doravirine until ≥4 weeks after enzalutamide discontinued

Estrogens and progestins

Contraceptives containing ethinyl estradiol and levonorgestrel (oral): No effect on ethinyl estradiol or levonorgestrel concentrations expected

Contraceptives containing etonogestrel or levonorgestrel (transdermal systems) and contraceptives containing ethinyl estradiol and etonogestrel or segesterone (vaginal rings): No effect on concentrations of these hormones expected

Medroxyprogesterone: No effect on concentrations of the hormone expected

Contraceptives containing ethinyl estradiol and levonorgestrel (oral): Dosage adjustments not needed

Contraceptives containing etonogestrel or levonorgestrel (transdermal systems) and contraceptives containing ethinyl estradiol and etonogestrel or segesterone (vaginal rings): Dosage adjustments not needed

Medroxyprogesterone: Dosage adjustments not needed

Etravirine

Decreased doravirine concentrations expected

No in vitro evidence of antagonistic antiretroviral effects

Concomitant use not recommended

Glecaprevir and pibrentasvir

Fixed combination of glecaprevir and pibrentasvir (glecaprevir/pibrentasvir): Possible increased doravirine concentrations

Glecaprevir/pibrentasvir: Dosage adjustments not needed

Histamine H2-receptor antagonists

No effect on doravirine concentrations expected

Dosage adjustments not needed

HMG-CoA reductase inhibitors (statins)

Atorvastatin: No clinically important effect on atorvastatin concentrations

Fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin: No effect on statin concentrations expected

Atorvastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin: Dosage adjustments not needed

Immunosuppressive agents

Cyclosporine: Possible increased doravirine concentrations; no effect on cyclosporine concentrations expected

Everolimus, sirolimus, tacrolimus: No effect on immunosuppressive agent concentrations expected

Cyclosporine, everolimus, sirolimus, tacrolimus: Dosage adjustments not needed

Indinavir

No in vitro evidence of antagonistic antiretroviral effects

Lamivudine

No clinically important pharmacokinetic interactions between doravirine and lamivudine

No in vitro evidence of antagonistic antiretroviral effects between doravirine and lamivudine

Ledipasvir and sofosbuvir

Fixed combination of ledipasvir and sofosbuvir (ledipasvir/sofosbuvir): No clinically important pharmacokinetic interactions

Ledipasvir/sofosbuvir: Dosage adjustments not needed

Lofexidine

No effect on lofexidine concentrations expected

Dosage adjustments not needed

Lopinavir

Fixed combination of lopinavir and ritonavir (lopinavir/ritonavir): Increased doravirine concentrations expected; not expected to affect lopinavir concentrations

Lopinavir/ritonavir: Dosage adjustments not needed

Macrolides

Azithromycin: No effect on azithromycin concentrations expected

Clarithromycin: Possible increased doravirine concentrations; no effect on clarithromycin concentrations expected

Erythromycin: Possible increased doravirine concentrations

Azithromycin: Dosage adjustments not needed

Clarithromycin: Experts state consider alternative (e.g., azithromycin) for prophylaxis or treatment of M. avium complex (MAC) infections in patients receiving doravirine

Erythromycin: Experts state monitor for doravirine tolerability

Maraviroc

No effect on maraviroc pharmacokinetics expected

No in vitro evidence of antagonistic antiretroviral effects

Dosage adjustments not needed

Methadone

No clinically important effect on pharmacokinetics of either drug

Dosage adjustments not needed

Mitotane

Decreased doravirine concentrations expected; possible decreased doravirine efficacy

Concomitant use contraindicated; do not initiate doravirine until ≥4 weeks after mitotane discontinued

Nefazodone

Possible increased doravirine concentrations

Experts state monitor for doravirine-associated adverse effects

Nevirapine

Decreased doravirine concentrations expected

No in vitro evidence of antagonistic antiretroviral effects

Concomitant use not recommended

Olanzapine

No clinically important effect on olanzapine concentrations expected

Dosage adjustments not needed

Phosphodiesterase type 5 (PDE5) inhibitors

Avanafil, sildenafil, tadalafil, vardenafil: No effect on PDE5 inhibitor concentrations expected

Avanafil, sildenafil, tadalafil, vardenafil: Dosage adjustments not needed

Platelet-aggregation inhibitors

Clopidogrel, prasugrel: No effect on platelet-aggregation inhibitor concentrations expected

Clopidogrel, prasugrel: Dosage adjustments not needed

Proton-pump inhibitors

Pantoprazole: No clinically important effect on doravirine concentrations

Other proton-pump inhibitors: No effect on doravirine concentrations expected

Pantoprazole and other proton-pump inhibitors: Dosage adjustments not needed

Raltegravir

No pharmacokinetic interactions expected

No in vitro evidence of antagonistic antiretroviral effects

Dosage adjustments not needed

Rilpivirine

No in vitro evidence of antagonistic antiretroviral effects

Ritonavir

Increased doravirine exposures and peak plasma concentrations; not considered clinically important

St. John's wort (Hypericum perforatum)

Decreased doravirine concentrations expected; possible decreased efficacy of doravirine

Concomitant use contraindicated; do not initiate doravirine until ≥4 weeks after St. John's wort discontinued

Sofosbuvir and velpatasvir

Fixed combination of sofosbuvir and velpatasvir (sofosbuvir/velpatasvir): No clinically important pharmacokinetic interactions expected

Sofosbuvir/velpatasvir: Dosage adjustments not needed

Sofosbuvir, velpatasvir, and voxilaprevir

Fixed combination of sofosbuvir, velpatasvir, and voxilaprevir (sofosbuvir/velpatasvir/voxilaprevir): No clinically important pharmacokinetic interactions expected

Sofosbuvir/velpatasvir/voxilaprevir: Dosage adjustments not needed

SSRIs

Citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, sertraline: No effect on SSRI concentrations expected

Citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, sertraline: Dosage adjustments not needed

Stavudine

No in vitro evidence of antagonistic antiretroviral effects

Tenofovir

Tenofovir DF: No clinically important pharmacokinetic interactions with doravirine

Tenofovir DF: No in vitro evidence of antagonistic antiretroviral effects with doravirine

Tipranavir

Ritonavir-boosted tipranavir: Increased doravirine concentrations expected; not expected to affect tipranavir concentrations

Ritonavir-boosted tipranavir: Dosage adjustments not needed

Trazodone

No effect on trazodone concentrations expected

Dosage adjustments not needed

Zidovudine

No in vitro evidence of antagonistic antiretroviral effects

Doravirine Pharmacokinetics

Absorption

Bioavailability

64%.

Food

Relative to fasting state, administration with high-fat meal increases AUC, peak plasma concentrations, and trough plasma concentrations by 16, 3, and 36%, respectively.

Effect of food not considered clinically important.

Plasma Concentrations

Peak plasma concentrations occur 2 hours after oral administration. Steady-state concentrations achieved after 2 days.

Distribution

Extent

Distributed into milk in rats; not known whether distributed into human milk.

Plasma Protein Binding

76%.

Elimination

Metabolism

Metabolized primarily by CYP3A.

Elimination Route

Approximately 6% of oral dose eliminated in urine as unchanged doravirine; unchanged drug also eliminated to a minor extent by biliary and/or fecal routes.

Half-life

15 hours.

Special Populations

Moderate hepatic impairment (Child-Pugh class B): No clinically important effect on doravirine pharmacokinetics.

Severe renal impairment: Doravirine exposures increased by 43%.

Based on population pharmacokinetic analysis, renal function does not have a clinically important effect on doravirine pharmacokinetics.

No clinically relevant differences in pharmacokinetics based on age (adults), race, body mass index (BMI), or sex.

Stability

Storage

Oral

Tablets

20–25°C (may be exposed to 15–30°C).

Store in original bottle. Protect from moisture; do not remove desiccant and keep bottle tightly closed.

Actions and Spectrum

  • Doravirine is a pyridinone HIV NNRTI antiretroviral. Inhibits replication of HIV-1 by interfering with viral polymerase activities of reverse transcriptase.

  • Inhibits polymerization reaction by noncompetitive, non-active site binding to reverse transcriptase causing conformational changes within active site that result in an inactive conformation.

  • Does not inhibit human cellular α- and β-DNA polymerases or mitochondrial γ-DNA polymerase.

  • Active against wild-type HIV-1, including certain strains resistant to other NNRTIs (i.e., those with K103N and/or Y181C substitutions).

  • HIV-1 strains resistant to doravirine have been produced in vitro and have emerged during doravirine therapy.

  • Cross-resistance occurs among HIV NNRTIs (e.g., efavirenz, etravirine, nevirapine, rilpivirine). Treatment-emergent doravirine resistance-associated substitutions can confer cross-resistance to other NNRTIs; however, treatment-emergent doravirine resistance-associated substitution Y318F does not appear to confer reduced susceptibility to efavirenz, etravirine, or rilpivirine.

Advice to Patients

  • Critical nature of compliance with HIV therapy and importance of remaining under the care of a clinician. Importance of taking as prescribed; do not alter or discontinue antiretroviral regimen without consulting clinician.

  • Antiretroviral therapy is not a cure for HIV infection; opportunistic infections and other complications associated with HIV disease may still occur.

  • Advise patients that early initiation of antiretroviral therapy and sustained decreases in plasma HIV RNA have been associated with reduced risk of progression to acquired immunodeficiency syndrome (AIDS) and death.

  • Advise patients that effective antiretroviral regimens can decrease HIV levels in blood and genital secretions and strict adherence to such regimens in conjunction with risk-reduction measures may decrease, but cannot absolutely eliminate, the risk of secondary transmission of HIV to others. Importance of continuing to practice safer sex (e.g., using latex or polyurethane condoms to minimize sexual contact with body fluids) and reducing high-risk behaviors (e.g., reusing or sharing needles).

  • Importance of reading patient information provided by the manufacturer.

  • Advise patients to take doravirine once every day at a regularly scheduled time with or without food.

  • Advise patients not to miss or skip doses since this can result in development of resistance. If a patient forgets to take doravirine, tell the patient to take the missed dose right away, unless it is almost time for the next dose. Advise the patient not to take 2 doses at one time and to take the next dose at the regularly scheduled time.

  • Advise patients that doravirine may interact with certain other drugs. For patients receiving rifabutin, importance of taking one 100-mg tablet of doravirine twice daily (approximately 12 hours apart).

  • Inform patients that signs and symptoms of inflammation from other previous infections may occur soon after initiation of antiretroviral therapy in some patients with advanced HIV infection (AIDS). These symptoms may be due to an improvement in immune response, enabling the body to fight infections that may have been present with no obvious symptoms. Importance of immediately informing a clinician if any symptoms of infection occur.

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and herbal supplements (e.g., St. John’s wort), as well as any concomitant illnesses.

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. Advise HIV-infected women not to breast-feed.

  • Importance of advising patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Doravirine

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets, film-coated

100 mg

Pifeltro

Merck

AHFS DI Essentials™. © Copyright 2021, Selected Revisions March 30, 2020. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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