Drugs for HIV & AIDS Protease Inhibitors (PIs)

What are they? http://www ai!s"e!s #o"/PIs ht" What are Protease Inhibitors (PIs)? Protease Inhibitors (PIs) are a class of anti-HIV drugs. When one PI is used in combination with other anti-HIV drugs usually a total of 3 drugs then this combination thera y can bloc! the re lication of HIV in a erson"s blood. #he first $ PIs listed abo%e are currently a ro%ed by the &'( for use in these combination thera ies. Protease inhibitors re%ent #-cells that ha%e been infected with HIV from roducing new co ies of the %irus. When HIV infects a cell in a erson"s body) it co ies it"s own genetic code into the cell"s '*(. In this way) the cell is then + rogrammed+ to create new co ies of HIV. ,nce HIV"s genetic material (-*() is inside a #-cell"s '*() the cell roduces a long strand of genetic material that must be cut u and ut together correctly to form new co ies of the %irus. .utting u this strand re/uires a scissorli!e en0yme called rotease. PIs bloc! this en0yme and re%ent the cell from roducing new %iruses. #o learn more on how HIV infects a #-cell and begins to create more %iruses) and where each class of anti-HIV drugs bloc!s this rocess) clic! on the following lesson lin!1 ($%peri"enta& !rugs are italicized' an! appro(e! !rugs are in regu&ar' non) ita&i#i*e! type) +ran! ,a"e In%irase2 &orto%ase2 -eneri# ,a"e Abbre(iation sa/uina%ir 45V (H3.) (Hard 3el .a ) sa/uina%ir (4oft 45V (43.) 3el .a ) $%peri"enta& .o!e -o-36-7898 Phar"a#euti#a& .o"pany -oche :aboratories -oche :aboratories

*or%ir2 .ri<i%an2 Virace t2

ritona%ir indina%ir nelfina%ir

-#V I'V *&V (PV :PV

(;#-937 =>-?38 (3-63A3

(bbott :aboratories =erc! @ .o. Pfi0er

(generase2 am rena%ir >aletra2 lo ina%ir C ritona%ir

6A6W8A or VB3la<o4mith>line A$7 (;#-3$7Dr (bbott :aboratories

GW-433908 or GlaxoSmithKline VX-175 tipranavir &riva'a( ata)anavir mo)enavir TPV P !-140"90 #*S-+3+"3+ 1*P-450 #oehrin$er %n$elheim #ri,tol-*-er, S./i00 Trian$le Pharma2e/ti2al,

I""une)+ase! /herapies
What are they? htt 1DDwww.aidsmeds.comDI;#.htm ($%peri"enta& !rugs are italicized' an! appro(e! !rugs are in regu&ar' non) ita&i#i*e! type) +ran! ,a"e -eneri# ,a"e Abbre(iati $%peri"ent Phar"a#euti#a& on a& .o!e .o"pany %5-+ :G1""1 6hiron 6orporation The %mm/ne 7e,pon,e 6orporation

Prole/3in al'e,le/3in4 or ( %nterle/3in-+ 7em/ne 9%V-1 %mm/no$en4 or 8 Sal3 va22ine

What are I""une)+ase! /herapies?

(I'4 researchers ha%e rimarily concentrated on finding drugs that re%ent HIV from re licating (creating more %irus) inside the body. #hese drugs are often referred to as +anti%irals+. =ore recently) many researchers ha%e been trying to find ways to hel a erson"s immune system fight the %irus on its own. .alled +immunebased thera ies+) some of these treatments are now being studied in large clinical trials. ,ne a roach is to re roduce im ortant roteins) called +cyto!ines+) that hel regulate a erson"s immune system) then use them to stimulate or inhibit the growth and acti%ity of %arious immune cells. #he most tested treatment using this a roach is Proleu!in() a high-tech recreation of Interleu!in-E (I:-E)) a naturally occurring cyto!ine that stimulates the roduction of #A-cells. (nother a roach is the use of +thera eutic %accines+. While traditional %accines are used to + rime+ a erson"s immune system before a ossible infection occurs) thera eutic %accines attem t to +teach+ a erson"s immune system to fight a %irus long after it has infected them. #he leading candidate for this !ind of thera y is -emuneF) also !nown as the 4al! %accine. While these and other immune-based thera ies are being intensi%ely researched) it is im ortant to note that no studies ha%e yet been com leted that ha%e ro%en a clinical benefit (the ability to rolong a erson"s life).

0pportunisti# Infe#tions (0Is)

htt 1DDwww.aidsmeds.comDlessonsD4tartHere7.htm -emember our re%ious section titled +What is (I'4 @ HIVG+1 (I'4 (ac/uired immune deficiency syndrome) is a condition caused by a %irus called HIV. #his %irus attac!s the immune system) the body"s +security force+ that fights off infections. When the immune system brea!s down) you lose this rotection and can de%elo many serious) often deadly infections and cancers. #hese are called +o ortunistic infections+ (,Is) because they ta!e ad%antage of the body"s wea!ened defenses. Hou ha%e heard it said that someone +died of (I'4.+ #his is not entirely accurate) since it is the o ortunistic infections that cause death. (I'4 is the condition that lets them ta!e hold. In the I4) the .enters for 'isease .ontrol (.'.) is res onsible for collecting data on the number of eo le with (I'4. #his is not the same thing as the number of eo le li%ing with HIV. -emember) (I'4 includes the words +immune deficiency+. 4ince eo le can li%e with HIV

an a%erage of 6J years before their immune systems become seriously im aired) (I'4 is really Kust the last stage of an HIV infection. #he .'. uses s ecific criteria for determining when a erson li%ing with HIV rogresses to (I'4. ,ne thing they loo! at is #-cell counts1 if a erson falls below EJJ #A cells) then they ha%e officially rogressed to (I'4. (nother thing they loo! for are ,Is1 if an HIVC indi%idual is diagnosed with an o ortunistic infection that"s included on the .'."s list of o%er two do0en ossible HIV-related ,Is) then they are diagnosed with (I'4. =any ,Is can be re%ented andDor treated. In fact) a lot of the (I'4 research you here about has been done to find treatments or cures for s ecific ,Is) and not Kust loo!ing for drugs to sto HIV. 1iste! be&ow are &essons about ea#h of the "a2or 0Is & #an#ers that #an o##ur !uring &ate)stage HIV !isease' a&ong with possib&e treat"ents:

+a#teria& Infe#tions

4unga& Infe#tions

=ycobacterium (%ium .om le< (=(.) 4almonellosis - 2omin$ ,oon 4y hilis @ *eurosy hilis 2omin$ ,oon

(s ergillosis - 2omin$ ,oon .andidiasis (thrush) yeast infection) .occidioidomycosis - 2omin$

,oon

#uberculosis (#;) (nal 'ys lasiaD.ancer .er%ical 'ys lasiaD.ancer >a osi"s 4arcoma (>4) :ym homas .ytomegalo%irus (.=V) He atitis - 2omin$ ,oon

.ry tococcal =eningitis Histo lasmosis - 2omin$ ,oon .ry tos oridiosis =icros oridiosis Pneumocystis .arinii Pneumonia (P.P) #o<o lasmosis (I'4 'ementia .om le< -

3a&ignan#ies (.an#ers)

Proto*oa& Infe#tions

Vira& Infe#tions

,euro&ogi#a& .on!itions

Her es 4im le< Virus (oral @ genital her es) Her es Loster Virus (shingles)
- 2omin$ ,oon

2omin$ ,oon

Peri heral *euro athy

Human Pa iloma Virus (HPV) genital warts) analDcer%ical dys lasiaDcancer) =olluscum .ontagiosum 2omin$ ,oon

0ther .on!itions an! .o"p&i#ations

( thous Ilcers - 2omin$ ,oon 'e ression &atigue and (nemia *ausea @ 'iarrhea #hrombocyto enia - 2omin$ ,oon Wasting 4yndrome @ :i odystro hy

,ral Hairy :eu!o la!ia (,H:)

- 2omin$ ,oon

Progressi%e =ultifocal :eu!oence halo athy (P=:)

http://www ai!s"e!s #o"/S$s ht"

/reat"ents for Si!e $ffe#ts

($%peri"enta& !rugs are italicized' an! appro(e! !rugs are in regu&ar' non) ita&i#i*e! type) Ane"ia (low le%els of red blood cells) which can cause fatigue1 learn more) +ran! ,a"e Procrit2 -eneri# ,a"e e oetin alfa (erythro oietin) Abbre(iation $%peri"enta& Phar"a#euti#a& .o!e .o"pany ,rtho ;iotech

1ipo!ystrophy (learn more) +ran! ,a"e -eneri# ,a"e Abbre(iation $%peri"enta& Phar"a#euti#a& .o!e .o"pany Serono 5a0oratorie,

,omatropin4 or Sero,tim( h/man $ro;th hormone

Under Construction -- other side effect treatments will be listed soon

http://www ai!s"e!s #o"/0ther.&asses ht"

0ther .&asses of Anti)HIV Drugs

($%peri"enta& !rugs are italicized' an! appro(e! !rugs are in regu&ar' non)

ita&i#i*e! type) ,u#&eotide 5e(erse /rans#riptase Inhibitors +ran! ,a"e VireadF -eneri# ,a"e Abbre(iation tenofo%ir diso ro<il fumarate ('&) -eneri# ,a"e #'& or ;is(P,.) P=P( $%peri"enta& Phar"a#euti#a& .o!e .o"pany 3ilead 4ciences

.e&&u&ar Inhibitors +ran! ,a"e 'ro<ia2 +ran! ,a"e Abbre(iation $%peri"enta& .o!e Phar"a#euti#a& .o"pany ;ristol-=yers 4/uibb $%peri"enta& .o!e T-+0 T-1+49 :*1-3100 Phar"a#euti#a& .o"pany Trimeri, Trimeri, :nor*=14 %n2>

hydro<yurea HI -eneri# ,a"e en</virti'e

$ntry Inhibitors (in#&u!ing 4usion Inhibitors) Abbre(iation

,on),u#&eosi!e 5e(erse /rans#riptase Inhibitors (,,5/Is)

What are they? htt 1DDwww.aidsmeds.comD**-#Is.htm ($%peri"enta& !rugs are italicized' an! appro(e! !rugs are in regu&ar' non) ita&i#i*e! type) +ran! ,a"e Viramune2 -eneri# ,a"e ne%ira ine Abbre(iation *VP ':V M&V =*V $%peri"enta& .o!e ;I--3-97$ I-8J69E4D# '=P-E?? *K6-44+ Phar"a#euti#a& .o"pany ;oehringer Ingelheim Pfi0er ;ristol-=yers 4/uibb Trian$le

-escri tor2 dela%irdine 4usti%aF efa%iren0 6oa2tinon( emivirine

Pharma2e/ti2al, ?@A2alanoli'e : 2apravirine 6PV :G-1549 or S1153 1P6-083 T*6-1+0 T*6-1+5 Sara;a3 *e'i2hem P<i)er #ri,tol-*-er, S./i00 Ti0ote2-Vir2o Gro/p Ti0ote2-Vir2o Gro/p

What are ,on),u#&eosi!e 5e(erse /rans#riptase Inhibitors (,,5/Is)? **-#Is are a class of anti-HIV drugs. When one **-#I is used in combination with other anti-HIV drugs usually a total of 3 drugs then this combination thera y can bloc! the re lication of HIV in a erson"s blood. #he first 3 **-#Is listed abo%e are currently a ro%ed by the &'( for use in these combination thera ies. **-#Is) sometimes referred to as +*on-*ucleoside (nalogues+ or +non-nu!es+ for short re%ent healthy #-cells in the body from becoming infected with HIV. When HIV infects a cell in a erson"s body) it co ies it"s own genetic code into the cell"s '*(. In this way) the cell is then + rogrammed+ to create new co ies of HIV. HIV"s genetic material is in the form of -*(. In order for it to infect #-cells) it must first con%ert its -*( into '*(. HIV"s re%erse transcri tase en0yme is needed to erform this rocess. **-#Is attach themsel%es to re%erse transcri tase and re%ent the en0yme from con%erting -*( to '*(. In turn) HIV"s genetic material cannot be incor orated into the healthy genetic material of the cell) and re%ents the cell from roducing new %irus. #o learn more on how HIV infects a #-cell and begins to create more %iruses) and where each class of anti-HIV drugs bloc!s this rocess) clic! on the following lesson lin!1

,u#&eosi!e/,u#&eoti!e 5e(erse /rans#riptase Inhibitors (,5/Is)

What are they? htt 1DDwww.aidsmeds.comD*-#Is.htm ($%peri"enta& !rugs are italicized' an! appro(e! !rugs are in regu&ar' non)ita&i#i*e! type) +ran! ,a"e -eneri# ,a"e -etro%ir2 M i%ir2 .ombi%ir2 #ri0i%irF LiagenF Hi%id
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Abbre(iation (L# or L'V 3#. (L# C 3#.

$%peri"enta& .o!e

Phar"a#euti#a& .o"pany 3la<o4mith>line 3la<o4mith>line 3la<o4mith>line 3la<o4mith>line

0ido%udine lami%udine 0ido%udine C lami%udine

abaca%ir C 0ido%udine (;. C (L# C 3#. C lami%udine abaca%ir 0alcitabine didanosine1 buffered %ersions didanosine1 delayedrelease ca sules sta%udine tenofo%ir diso ro<il fumarate ('&) emtri2ita0ine am'oxovir (;. dd. ddI ddI dA# #'& or ;is(P,.) P=P( BT6 1:P1 ;=H-E$79$ ;=H-AJ8JJ 698EI78

3la<o4mith>line -oche :aboratories ;ristol-=yers 4/uibb ;ristol-=yers 4/uibb ;ristol-=yers 4/uibb 3ilead 4ciences Trian$le Pharma2e/ti2al, Trian$le Pharma2e/ti2al,

Vide<2 Vide<2 M. Lerit2 VireadF 6ovira2il8

What are ,u#&eosi!e/,u#&eoti!e 5e(erse /rans#riptase Inhibitors (,5/Is)? *-#Is are a class of anti-HIV drugs. When *-#Is are used in combination with other anti-HIV drugs usually a total of 3 drugs then this combination thera y can bloc! the re lication of HIV in a erson"s blood. #he first 6J *-#Is listed abo%e are currently a ro%ed by the &'( for use in these combination thera ies. *-#Is) sometimes referred to as +*ucleoside (nalogues+ or +nu!es+ for short re%ent healthy #-cells in the body from becoming infected with HIV. When HIV infects a cell in a erson"s body) it co ies it"s own genetic code into the cell"s '*(. In this way) the cell is then + rogrammed+ to

create new co ies of HIV. HIV"s genetic material is in the form of -*(. In order for it to infect #-cells) it must first con%ert its -*( into '*(. HIV"s re%erse transcri tase en0yme is needed to erform this rocess. *-#Is contain faulty %ersions of the building bloc!s (nucleotides) used by re%erse transcri tase to con%ert -*( to '*(. When re%erse transcri tase uses these faulty building bloc!s) the new '*( cannot be build correctly. In turn) HIV"s genetic material cannot be incor orated into the healthy genetic material of the cell and re%ents the cell from roducing new %irus. While nucleotide analogues (Viread is the only nucleotide analogue a ro%ed at this time) are technically different than nucleoside analogues) they act %ery much the same way. In order for nucleoside analogues to wor!) they must undergo chemical changes ( hos horylation) to become acti%e in the body. *ucleotide analogues by ass this ste ) gi%en that they are already chemically acti%ated. #o learn more on how HIV infects a #-cell and begins to create more %iruses) and where each class of anti-HIV drugs bloc!s this rocess) clic! on the following lesson lin!1